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DNA topoisomerase II inhibitor 1 (compound 8ed) is a potent DNA topoisomerase II inhibitor. DNA topoisomerase II inhibitor 1 shows anti-proliferative activity. DNA topoisomerase II inhibitor 1 induces apoptosis and cell cycle arrest at sub G1 phase .
SUB1 Human Pre-designed siRNA Set A contains three designed siRNAs for SUB1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Tricaprilin-d15(Trioctanoin-d15 is the deuterium labeled Tricaprilin (HY-B1804). Tricaprilin is an orally active and well tolerated ketogenic agent that safely induces ketosis. Tricaprilin restores brain electrical activity and metabolism to help counteract neuroinflammation in migraine. Tricaprilin is promising for research of migraine prevention and Alzheimer’s disease (AD). Tricaprilin is a pure C8 medium chain triglyceride (MCT) [3].
Tricaprilin-d50(Trioctanoin-d50 is the deuterium labeled Tricaprilin (HY-B1804). Tricaprilin is an orally active and well tolerated ketogenic agent that safely induces ketosis. Tricaprilin restores brain electrical activity and metabolism to help counteract neuroinflammation in migraine. Tricaprilin is promising for research of migraine prevention and Alzheimer’s disease (AD). Tricaprilin is a pure C8 medium chain triglyceride (MCT) [3].
Pretomanid-d5 is deuterated labeled Pretomanid (HY-10844). Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL.
Ac-{Cpg}-Thr-Ala-{Ala(CO)}-Asp-{Cpg}-NH2 (compound 40) is a potent Plasmodium subtilisin-like protease 1 (SUB1) inhibitor. SUB1-IN-1 shows IC50 values of 12 nM and 10 nM against P. vivax and P. falciparumSUB1 (Pv- and PfSUB1), respectively .
IMPDH-IN-2 (compound 2) is an inhibitor of inosine monophosphate dehydrogenase (IMPDH) with IC50 for IMPDH I and IMPDH II >Values are 0.15 and 0.17 μM, respectively. IMPDH-IN-2 has antitumor activity .
Zidovudine-d3 is the deuterium labeled Zidovudine. Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection.
Alpha-Naphthoflavone is an orally active flavonoid that is a potent, competitive inhibitor of aromatase< b>aromatase. < b > IC < sub > 50 < / sub > < / b > and < b > K < sub > I < / sub > < / b > value were 0.5 and 0.2 microns. Alpha-Naphthoflavone can inhibit cell proliferation and induce apoptosis[3] .
Omeprazole-d3 is deuterium labeled Omeprazole. Omeprazole, a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].
Deutenzalutamide (Enzalutamide-d3) is a developed deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells .
Clomipramine-d3 is the deuterium labeled Clomipramine. Clomipramine is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively[1][2].
Acetaminophen-d3 is the deuterium labeled Acetaminophen. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent[1][2][3]. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor[4].
Alpha-Estradiol-d3 is the deuterium labeled Alpha-Estradiol. Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia.
Normetanephrine-d3 (hydrochloride) is the deuterium labeled Normetanephrine hydrochloride. Normetanephrine ((±)-Normetanephrine) hydrochloride is the O-methylated metabolite of norepinephrine (NE)[1].
Methoxsalen-d3 is the deuterium labeled Methoxsalen[1]. Methoxsalen (8-Methoxypsoralen) is a potent tricyclic furocoumarin suicide inhibitor of CYP (cytochrome P-450), is an agent used to treat psoriasis, eczema, vitiligo and some cutaneous Lymphomas in conjunction with exposing the skin to sunlight[2].
Liothyronine-d3 is deuterated labeled Liothyronine (HY-A0070A). Liothyronine is an active form of thyroid hormone. Liothyronine is a potent thyroid hormone receptors TRα and TRβ agonist with Kis of 2.33 nM for hTRα and hTRβ, respectively [3].
Butylphthalide-d3 is the deuterium labeled Butylphthalide. Butylphthalide(3-n-Butylphthalide), an anti-cerebral-ischemia agent, is first isolated from the seeds of celery and showes efficacy in animal models of stroke.
Tamoxifen-d3 hydrochloride is deuterated labeled Tamoxifen (Citrate) (HY-13757). Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells [3].Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen Citrate activates autophagy and induces apoptosis .Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse .
Frovatriptan-d3 (hydrochloride) is the deuterium labeled Frovatriptan[1]. Frovatriptan is a potent 5-HT1B//D receptor agonist and has the highest 5-HT1B potency in the triptan class. Frovatriptan is apparently cerebroselective. Frovatriptan is efficacious and even superior in some endpoints also when taken during the headache phase in migraine attacks with aura[2].
5-Aminosalicylic acid-d3 is the deuterium labeled 5-Aminosalicylic Acid. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB[1][2][3][4].
N,N-Dimethylglycine-d3(Dimethylglycine-d3) hydrochloride is the deuterium labeled N,N-Dimethylglycine hydrochloride (HY-W001158). N,N-Dimethylglycine (Dimethylglycine) is a natural N-methylated glycine, is a nutrient supplement and acts as an NMDAR glycine site partial agonist. N,N-Dimethylglycine is a methyl donor, could improve immunity, function as an antioxidant to prevent oxidative stress, and scavenge excess of free radicals. N,N-Dimethylglycine exhibits antidepressant-like and surfactant effects [3].
Fulvestrant-d3 is the deuterium labeled Fulvestrant. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy[1].
Deracoxib-d3 is the deuterium labeled Deracoxib. Deracoxib, a selective cyclooxygenase-2 inhibitor, is a non-narcotic, non-steroidal anti-inflammatory drug (NSAID).
Guaifenesin-d3 is the deuterium labeled Guaifenesin. Guaifenesin (Guaiacol glyceryl ether), a constituent of guaiac resin from the wood of Guajacum officinale Linné, is an expectorant. Guaifenesin can alleviate cough discomfortby increasing sputum volume and decreasing its viscosity, thereby promoting effective cough[1][2].
Tamoxifen-d3 is the deuterium labeled Tamoxifen . Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells [3] . Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen activates autophagy and induces apoptosis . Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse .
Binimetinib-d3(MEK162-d3) is deuterium labeled Binimetinib. Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM .
Gatifloxacin-d3 (hydrochloride) is the deuterium labeled Gatifloxacin (hydrochloride). Gatifloxacin hydrochloride (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin hydrochloride can be used to treat bacterial conjunctivitis in vivo.
5-Aminosalicylic Acid-d3 (hydrochloride) is the deuterium labeled 5-Aminosalicylic Acid. 5-Aminosalicylic acid (Mesalamine) hydrochloride acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
Thiamphenicol-d3 is a deuterium labeled Thiamphenicol. Thiamphenicol, a methyl-sulfonyl derivative of Chloramphenicol, is a broad-spectrum antimicrobial antibiotic. Thiamphenicol acts by binding to the 50S ribosomal subunit, leading to inhibition of protein synthesis and bacteriostatic effect (against Gram-negative, Gram-positive aerobic and anaerobic bacteria)[1][2].
Physcion-d3(Parietin-d3) is the deuterium labeled Physcion (HY-N0108). Physcion acts as an inhibitor of 6-phosphogluconate dehydrogenase, with an IC50 and a Kd of 38.5 μM and 26.0 μM, respectively. Physcion exhibits laxative, hepatoprotective, anti-inflammatory, anti-microbial, anti-proliferative and anti-tumor effects [3].
Antipyrine-d3 is the deuterium labeled Antipyrine. Antipyrine (Phenazone) is an antipyretic and analgesic. Antipyrine can be used as a probe agent for oxidative agent metabolism. Antipyrine has been widely used in assessment of hepatic oxidative capacity[1][2].
Taxifolin-d3 is deuterium labeled Taxifolin. Taxifolin ((+)-Dihydroquercetin) exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM[1]. Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity[2].
Nomifensine-d3((±)-Nomifensine-d3) maleate is the deuterium labeled Nomifensine maleate (HY-B1110A). Nomifensine ((±)-Nomifensine) is a potent norepinephrine (NE) and dopamine (DA) reuptake inhibitor. Nomifensine inhibits uptake of NE, DA and 5-HT in rat brain synaptosomes, with IC50 values of 6.6 nM, 48 nM and 830 nM, and Ki values of 4.7 nM, 26 nM and 4000 nM, respectively. Nomifensine shows low or ineffective binding activity to dopamine D2, α1-adrenergic, 5-HT2, and muscarinic receptors. Nomifensine has antidepressive effects [3].
Roflumilast-d3 is deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells.
Acetylcysteine-d3 is the deuterium labeled Acetylcysteine. Acetylcysteine (N-Acetylcysteine) is a mucolytic agent which reduces the thickness of the mucus. Acetylcysteine is a ROS inhibitor. Acetylcysteine is a cysteine precursor, prevents hemin-induced ferroptosis by neutralizing toxic lipids generated by arachidonate-dependent activity of 5-lipoxygenases. Acetylcysteine induces cell apoptosis. Acetylcysteine also has anti-influenza virus activities. In addition, Acetylcysteine is the most stable form of cysteine during drug delivery and can be used in disulfidptosis studies [3] .
Esomeprazole-d3 potassium is deuterated labeled Esomeprazole (HY-17021). Esomeprazole ((S)-Omeprazole) is a potent and orally active proton pump inhibitor and reduces acid secretion through inhibition of the H +, K +-ATPase in gastric parietal cells. Esomeprazole has the potential for symptomatic gastroesophageal reflux disease research [3].
L-Tryptophan-d3 is the deuterium labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3[1].
Meldonium-d3 is the deuterated form of Meldonium. Meldonium is a cardiovascular protective agent that competitively inhibits BBOX1 and OCTN2. The IC50 value of Mildronate against human recombinant BBOX is 34-62 μM, and the EC50 value against human OCTN2 is 21 μM. Meldonium is a fatty acid oxidation inhibitor [3].
Pizotyline-d3 is deuterated labeled Pizotifen (HY-B0115). Pizotifen (Pizotyline) is a potent 5-HT2 receptor antagonist, with a high affinity for 5-HT1C binding site.
Cefotaxime-d3 is the deuterium labeled Cefotaxime (HY-A0088A). Cefotaxime is the β-lactamase stable cephalosporin and the third-generation cephalosporin antibiotic. Cefotaxime possesses broad-spectrum antibiotic activity against numerous Gram-positive and Gram-negative bacteria [3] .
Rapamycin-d3 is the deuterium labeled Rapamycin. Rapamycin is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant .
Florfenicol-d3 is the deuterium labeled Florfenicol. Florfenicol, a commonly used veterinary antibiotic, is currently indicated for bovine respiratory disease, and also used in aquaculture for the control of enteric septicemia in catfish. Florfenicol can induce early embryonic death in eggs, with an LC50 of 1.07 μg/g.
Pyrazinamide-d3 is deuterium labeled Pyrazinamide. Pyrazinamide (Pyrazinecarboxamide; Pyrazinoic acid amide) is a potent and orally active antitubercular antibiotic. Pyrazinamide is a proagent that is converted to the active form pyrazinoic acid (POA) by PZase/nicotinamidase encoded by the pncA gene in M. tuberculosis[1][2].
Salbutamol-d3 is the deuterium labeled Salbutamol. Salbutamol is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease (COPD).
Tetrahydrouridine-d3 is the deuterium labeled Tetrahydrouridine[1]. Tetrahydrouridine dihydrate is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine[2][3].
Esomeprazole-d3 is deuterium labeled Esomeprazole. Esomeprazole ((S)-Omeprazole) is a potent and orally active proton pump inhibitor and reduces acid secretion through inhibition of the H+, K+-ATPase in gastric parietal cells. Esomeprazole has the potential for symptomatic gastroesophageal reflux disease research[1][2][3].
Doxorubicinone-d3 is the deuterium labeled Doxorubicinone. Doxorubicinone is a metabolite of an anti-cancer chemotherapy agent Doxorubicin[1]. Doxorubicin is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively.
Rifampicin-d3 is the deuterium labeled Rifampicin. Rifampicin is a potent and broad spectrum antibiotic against bacterial pathogens. Rifampicin has anti-influenza virus activities[1][2].
Stearoylethanolamide-d3(Ceamid-d3) is deuterium labeled Stearoylethanolamide. Stearoylethanolamide is an endocannabinoid-like compound with pro-apoptotic activity .
(-)-Ketoconazole-d3 is deuterium labeled (-)-Ketoconazole. (-)-Ketoconazole ((-)-R 41400) is one of the enantiomer of Ketoconazole. Ketoconazole is a racemic mixture of two enantiomers, levoketoconazole ((2S,4R)-(−)-ketoconazole) and dextroketoconazole ((2R,4S)-(+)-ketoconazole).
Sarcosine-d3 is the deuterium labeled Sarcosine. Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia[1][2].
Thymidine-d3 is the deuterium labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[1][2][3].
Cefotaxime-d3 (sodium) is the deuterium labeled Cefotaxime (sodium salt). Cefotaxime sodium salt, a β-lactamase stable cephalosporin and a third-generation cephalosporin antibiotic, possesses broad-spectrum antibiotic activity against numerous Gram-positive and Gram-negative bacteria[1][2][3][4][5].
Exemestane-d3 is the deuterium labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research[1][2].
DL-Mevalonolactone-d3 is the deuterium labeled DL-Mevalonolactone[1]. DL-Mevalonolactone ((±)-Mevalonolactone;Mevalolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone (Mevalonolactone) decreases mitochondrial membrane potential ( Ψm), NAD(P)H content and the capacity to retain Ca2+ in the brain, besides inducing mitochondrial swelling[2][3].
Artemisinin-d3 is the deuterium labeled Artemisinin. Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants[1]. Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects[2].
Esomeprazole-d3 (sodium) is the deuterium labeled Esomeprazole. Esomeprazole ((S)-Omeprazole) is a potent and orally active proton pump inhibitor and reduces acid secretion through inhibition of the H+, K+-ATPase in gastric parietal cells. Esomeprazole has the potential for symptomatic gastroesophageal reflux disease research[1][2][3].
Fmoc-leucine-d3 is the deuterium labeled Fmoc-leucine. Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-induced glucose-intolerant, and in diabetic db/db mice. Fmoc-leucine has a lower adipogenic activity[1].
D-Alanine-d3 is the deuterium labeled D-Alanine. D-Alanine is a weak GlyR (inhibitory glycine receptor) and PMBA agonist, with an EC50 of 9 mM for GlyR.
Oseltamivir acid-d3 is a deuterium labeled Oseltamivir acid. Oseltamivir acid, the active metabolite of Oseltamivir phosphate, is an orally bioavailable, potent and selective inhibitor of influenza virus neuraminidase (IC50=2 nM) with activity against both influenza A and B viruses[1][2].
N-Acetyl-5-hydroxytryptamine-d3 is the deuterium labeled N-Acetyl-5-hydroxytryptamine. N-Acetyl-5-hydroxytryptamine is a Melatonin precursor, and that it can potently activate TrkB receptor[1][2].
Clomipramine-d3 (hydrochloride) is a deuterium labeled Clomipramine hydrochloride. Clomipramine hydrochloride is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively[1][2].
S-Adenosyl-L-methionine-d3 (S-Adenosyl methionine-d3) is the deuterated product of S-Adenosyl-L-methionine (HY-B0617). S-Adenosyl-L-methionine (S-Adenosyl methionine) is an orally active methyl group donor. S-Adenosyl-L-methionine is a dietary supplement with potent antidepressant effects. S-Adenosyl-L-methionine also has anti‑proliferative, pro‑apoptotic and anti‑metastatic roles in cancers. S-Adenosyl-L-methionine has the potential for, cancer, liver disease and osteoarthritis research [3].
(R)-Pyrrolidine-2-carboxylic acid-d3 is the deuterium labeled (R)-pyrrolidine-2-carboxylic acid. (R)-pyrrolidine-2-carboxylic acid is an endogenous metabolite.
Lamotrigine- 13C3,d3 is the 13C-labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al[1][2].
Rosuvastatin- 13C,d3 sodium is 13C and deuterated labeled Rosuvastatin sodium (HY-17504B). Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels [3].
Skatole-d3 is the deuterium labeled Skatole. Skatole is produced by intestinal bacteria, regulates intestinal epithelial cellular functions through activating aryl hydrocarbon receptors and p38[1].
Meglutol-d3 is the deuterium labeled Meglutol[1]. Meglutol is an antilipemic agent which lowers cholesterol, triglycerides, serum beta-lipoproteins and phospholipids, and inhibits the activity of hydroxymethylglutarryl CoA reductases, which is the rate limiting enzyme in the biosynthesis of cholesterol.
Estradiol-d3 is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.
D-Glucose-d-33 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
Methylacetylacetate-d3 (Acetoacetate methylester-d3) is a deuterium labeled Methyl acetylacetate (HY-Y1298). Methyl acetylacetate is an endogenous metabolite .
Vincristine-d3 (sulfate)is the deuterium labeled Vincristine sulfate. Vincristine sulfate is an antitumor vinca alkaloid which inhibits microtubule formation in mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. It binds to microtubule with a Ki of 85 nM[1][2].
Doxifluridine-d3 is deuterated labeled Doxifluridine (HY-B0021). Doxifluridine has anticancer activity. Doxifluidine is a 5-FU prodrug. Doxifluridine is a thymidinesynthase inhibitor. Doxifluridine can enhance tumor inhibition by synergizing with a variety of drugs [3].
Retinoic acid-d3 is the deuterium labeled Retinoic acid (HY-14649). Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha [3].
Vincristine-d3-ester (sulfate) is the deuterium labeled Vincristine sulfate. Vincristine sulfate is an antitumor vinca alkaloid which inhibits microtubule formation in mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. It binds to microtubule with a Ki of 85 nM[1].
Lurbinectedin-d3 is deuterium labeled Lurbinectedin. Lurbinectedin (PM01183) is a DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively[1].
L-Serine-d3 is the deuterium labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
Ondansetron-d3 is the deuterium labeled Ondansetron[1]. Ondansetron(GR 38032;SN 307) is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy[2].
Mifepristone-d3 is the deuterium labeled Mifepristone. Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay[1].
Levosulpiride-d3 is the deuterium labeled Levosulpiride. Levosulpiride (RV-12309) is the (S)-enantiomer of sulpiride, which is a D2 receptor a antagonist, an atypical antipsychotic agent of the benzamide class[1][2].
Etoricoxib-d3 is the deuterium labeled Etoricoxib[1]. Etoricoxib (MK-0663) is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood[2][3][4].
Mirtazapine-d3 is a deuterium labeled Mirtazapine. Mirtazapine is a 5-HT receptor inhibitor. Mirtazapine is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent by blocking 5-HT2 and 5-HT3 receptors[1].
Dioxybenzone-d3 is deuterium labeled Dioxybenzone. Dioxybenzone (Benzophenone-8; UV-24) is an organic compound used to block UVB and short-wave UVA (ultraviolet) radiation. Dioxybenzone has orally activity. Dioxybenzone exhibits estrogenic disrupting effect. Dioxybenzone up-regulates inflammatory cytokines. Dioxybenzone can be used for cancer, reproductive system disease and inflammatory disease study [3] .
Pantoprazole-d3 is deuterium labeled Pantoprazole. Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI)[1]. Pantoprazole, a substituted benzimidazole, is a potent H+/K+-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142)[3][4].
Oltipraz-d3 is the deuterium labeled Oltipraz. Oltipraz has an inhibitory effect on HIF-1α activation in a time-dependent manner, completely abrogating HIF-1α induction at ≥10 μM concentrations, the IC50 of Oltipraz for HIF-1α inhibition is 10 μM. Oltipraz is a potent Nrf2 activator.
Tilmicosin-d3 is the deuterium labeled Tilmicosin. Tilmicosin (LY-177370) is an orally active calcium channel antagonist and macrolide antibiotic with antimicrobial activity. Tilmicosin mainly acts on the 50S subunit of bacterial ribosomes, inhibiting protein synthesis. Tilmicosin is effective in the treatment of respiratory diseases in livestock such as cattle, sheep and pigs. In addition, Tilmicosin has immunomodulatory and anti-inflammatory effects .
Pocapavir-d3(SCH-48973-d3;V-073-d3) is the deuterium labeled Pocapavir (HY-104074) . Pocapavir (SCH-48973) is an orally active capsid inhibitor. Pocapavir prevents virion uncoating upon entry into the cell. Pocapavir has antiviral activity against polioviruses. Pocapavir also inhibits enterovirus infections .
Fexofenadine-d3 is the deuterium labeled Fexofenadine[1]. Fexofenadine (MDL-16455) is an orally active and nonsedative H1 receptor antagonist. Fexofenadine can be used in allergic rhinitis and chronic idiopathic urticarial research[2][3][4].
Medroxyprogesterone acetate-d3 is deuterium labeled Medroxyprogesterone acetate. Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors[1].
Brequinar-d3(DUP785-d3) is deuterium labeled Brequinar. Brequinar (DUP785) is a potent inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 of 5.2 nM for human DHODH. Brequinar has potent activities against a broad spectrum of viruses. Brequinar also has an anti-SARS2 activity .
Verapamil-d3 (hydrochloride) is the deuterium labeled Verapamil hydrochloride. Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research[1][2][3].
Trabectedin D3 (Ecteinascidin 743 D3) is deuterium labeled Trabectedin. Trabectedin is a tetrahydroisoquinoline alkaloid with potent antitumor activity. Trabectedin binds to the minor groove of DNA, blocks transcription of stress-induced proteins, induces DNA backbone cleavage and cancer cells apoptosis, and increases the generation of ROS in MCF-7 and MDA-MB-453 cells. Trabectedin has tje potential for soft tissue sarcoma and ovarian cancer treatment [3].
Oleanolic acid-d3 is the deuterium labeled Oleanolic Acid[1]. Oleanolic acid (Caryophyllin) is a natural compound from plants with anti-tumor activities[2].
Vitamin D3-d3 is the deuterium labeled Vitamin D3. Vitamin D3 (Cholecalciferol; Colecalciferol) is a naturally occuring form of vitamin D. Vitamin D3 induces cell differentiation and prevents proliferation of cancer cells.
Nortriptyline-d3 (hydrochloride) is the deuterium labeled Nortriptyline hydrochloride. Nortriptyline hydrochloride (Desmethylamitriptyline hydrochloride) is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and used to relieve the symptoms of depression[1].
Methylmalonic acid-d3 is the deuterium labeled Methylmalonic acid. Methylmalonic acid (Methylmalonate) is an indicator of Vitamin B-12 deficiency in cancer[1][2].
Benserazide-d3 (hydrochloride) is the deuterium labeled Benserazide hydrochloride. Benserazide hydrochloride (Serazide) is commonly used in Parkinson's disease and is an inhibitor of peripheral aromatic L-amino acid decarboxylase (AADC)[1].
Lamotrigine-d3 is the deuterium labeled Lamotrigine[1]. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al[2][3].
Diazoxide-d3 is deuterium labeled Diazoxide. Diazoxide (Sch-6783) is an ATP-sensitive potassium channel activator, has the potential for hyperinsulinism treatment.
Methionine-d3 is the deuterium labeled Methionine. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
Undecanoic acid-d3 is the deuterium labeled Undecanoic acid. Undecanoic acid (Undecanoate) is a monocarboxylic acid with antimycotic property, which inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum[1].
Dorzolamide-d3 hydrochloride is deuterated labeled Dorzolamide hydrochloride (HY-B0109A). Dorzolamide (L671152) hydrochloride is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity .
Pyridoxine-d3 (hydrochloride) is the deuterium labeled Pyridoxine hydrochloride. Pyridoxine hydrochloride (Pyridoxol; Vitamin B6) is a pyridine derivative. Pyridoxine (Pyridoxol; Vitamin B6) exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
Orlistat-d3 is a deuterated labeled Orlistat . Orlistat (Tetrahydrolipstatin) is a well-known irreversible inhibitor of pancreatic and gastric lipases. Orlistat is also an inhibitor of fatty acid synthase (FASN), is used orally for long-term research of obesity .?Anti-atherosclerotic?effect [3].
Baricitinib-d3 is the deuterium labeled Baricitinib. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
3-O-Methyldopa-d3(3-Methoxy-L-tyrosine-d3) is deuterium labeled 3-O-Methyldopa (HY-113468A). 3-O-Methyldopa is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of l-DOPA and dopamine .
3,4,5-Trimethoxybenzoic acid-d3 is the deuterium labeled 3,4,5-Trimethoxybenzoic acid[1]. 3,4,5-Trimethoxybenzoic acid (Eudesmic acid;Trimethylgallic Acid) is a benzoic acid derivative. A building block in medicine and organic synthesis.
Daunorubicin- 13C,d3 is 13C and deuterium labeled Daunorubicin. Daunorubicin (Daunomycin) is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin inhibits DNA and RNA synthesis. Daunorubicin is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin is also an anthracycline antibiotic. Daunorubicin can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor .
Frovatriptan-d3 (succinate) is deuterium labeled Frovatriptan (succinate). Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research[1][2].
5-Aminosalicylic acid-d3 disodium is deuterated labeled 5-Aminosalicylic Acid (HY-15027). 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).
Hexacosanoic acid methylester-d3 (C26:0 methylester-d3) is deuterium labeled Methyl hexacosanoate. Methyl hexacosanoate is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Dabigatran-d3 is the deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
Malic acid-d3 is the deuterium labeled Malic acid. Malic acid (Hydroxybutanedioic acid) is a dicarboxylic acid that is naturally found in fruits such as apples and pears. It plays a role in many sour or tart foods[1][2].
Infigratinib-d3 is a deuterated analog of infigratinib. Infigratinib is an effective inhibitor of the FGFR family, with IC50 values of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively .
Vinorelbine-d3 (ditartrate) is the deuterium labeled Vinorelbine ditartrate. Vinorelbine (ditartrate) is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC50 of 1.25 nM.
Rivastigmine-d3 hydrochloride is deuterated labeled Rivastigmine (HY-17368). Rivastigmine (ENA 713 free base) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease .
Thiamine-d3 (hydrochloride) is the deuterium labeled Thiamine hydrochloride. Thiamine hydrochloride (Thiamine chloride hydrochloride) is an essential micronutrient needed as a cofactor for many central metabolic enzymes.
Theophylline-d3 is deuterated labeled Theophylline (HY-B0809). Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research [3] .
4-Hydroxyantipyrine-d3 is the deuterium labeled 4-Hydroxyantipyrine. 4-Hydroxyantipyrine is the major metabolite of Antipyrine, can be as a biodistribution promoter. 4-Hydroxyantipyrine can increase distribution of concentration ratio of Antipyrine in the brain[1][2][3].
Cabotegravir-d3 (sodium) is the deuterium labeled Cabotegravir sodium. Cabotegravir sodium is a highly potent HIV integrase inhibitor with an IC50 value of 2.5 nM for HIVADA. Cabotegravir sodium is primarily metabolized by uridine diphosphate glucuronosyltr
Methyldopa-d3 (hydrochloride) is deuterium labeled Methyldopa (hydrochloride). Methyldopa hydrochloride (L-(-)-α-Methyldopa hydrochloride) hydrochloride, a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa hydrochloride is a proagent and is metabolized (α-Methylepinephrine) in the central nervous system[1][2].
Omeprazole metabolite Omeprazole sulfone-d3 is the deuterium labeled Omeprazole metabolite Omeprazole sulfone. Omeprazole sulfone is a metabolite of Omeprazole, which is a proton pump inhibitor.
Etoposide-d3 (VP-16-d3) is the deuterium labeled Etoposide (HY-13629). Etoposide (VP-16) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy .
Licarbazepine-d3 is the deuterium labeled Licarbazepine (HY-108506). Licarbazepine is a voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects[1][2].
Vildagliptin-d3 is the deuterium labeled Vildagliptin. Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity[1][2].
Ulipristal-d3(CDB-3236-d3) is deuterium labeled Ulipristal. Ulipristal (CDB 3236) is a selective progesterone receptor modulator (SPRM). Ulipristal binds to the progesteron receptor, thereby inhibiting PR-mediated gene expression, and interfering with progesterone activity in the reproductive system .
Imatinib-d3 (hydrochloride) is the deuterium labeled Imatinib. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
Riboflavin-d3 is the deuterium labeled Riboflavin. Riboflavin is an easily absorbed micronutrient with a key role in maintaining health in humans and other animals.
N-Desmethyl Clomipramine-d3 (hydrochloride) is the deuterium labeled N-Desmethyl Clomipramine. N-Desmethyl Clomipramine hydrochloride (Desmethylclomipramine hydrochloride) is a primary plasma N-desmethyl metabolite of Clomipramine[1]
Thiamphenicol-d3-1(Thiophenicol-d3-1;Dextrosulphenidol-d3-1) is the deuterium-labeled Thiamphenicol (HY-B0479) . Thiamphenicol (Thiophenicol)，a methyl-sulfonyl derivative of Chloramphenicol，is a broad-spectrum antimicrobial antibiotic. Thiamphenicol acts by binding to the 50S ribosomal subunit，leading to inhibition of protein synthesis and bacteriostatic effect (against Gram-negative，Gram-positive aerobic and anaerobic bacteria) [3].
(S)-Malic acid-d3 is the deuterium labeled (S)-Malic acid. (S)-Malic acid ((S)-2-Hydroxysuccinic acid) is a dicarboxylic acid in naturally occurring form, contributes to the pleasantly sour taste of fruits and is used as a food additive[1][2].
AChE/Aβ-IN-3 (compound AM5) is a dual inhibitor of AChE and Amyloid-β aggregation with IC50<.sub> values of 1.29 and 4.93 μM, respectively. AChE/Aβ-IN-3 has antioxidant properties that scavenge ROS and restore their normal levels. AChE/Aβ-IN-3 can be used in the study of neurological diseases, such as Alzheimer's disease .
Duloxetine-d3 (hydrochloride) is a deuterium labeled Duloxetine hydrochloride. Duloxetine hydrochloride is a serotonin-norepinephrine reuptake inhibitor (SNRI) with a Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD)[1][2].
N6-Methyladenosine-d3(6-Methyladenosine-d3;N-Methyladenosine-d3) is a deuterium labeled N6-Methyladenosine (HY-N0086). N6-Methyladenosine is the most prevalent internal (non-cap) modification present in the messenger RNA (mRNA) of all higher eukaryotes. N6-Methyladenosine can modifies viral RNAs and has antiviral activities.
Dexamethasone-d3-1(Hexadecadrol-d3-1; Prednisolone F-d3-1) is a deuterium labeled Dexamethasone (HY-14648). Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
Levocarnitine propionate-d3 (hydrochloride) is the deuterium labeled Levocarnitine propionate hydrochloride. Levocarnitine propionate hydrochloride (L-Propionylcarnitine chloride; ST-261) is used to treat the deterioration of renal function, congestive heart failure, intermittent claudication, and other diseases.
N-Methylpyrrolidone-d3 is the deuterium labeled N-Methylpyrrolidone [1]. N-Methylpyrrolidone (1-Methyl-2-pyrrolidinone), a five-membered cyclic amide, is an organic polar solvent. N-Methylpyrrolidone is extensively used in the manufacture of adhesives, paints, fuels, and pharmaceuticals[2][3].
Phenylephrine-d3 (hydrochloride) is the deuterium labeled Phenylephrine hydrochloride. (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
Tofacitinib-d3 (citrate) is deuterium labeled Tofacitinib (citrate). Tofacitinib citrate is an orally available JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.
13-cis Acitretin-d3 is a deuterium labeled 13-cis Acitretin. 13-cis Acitretin is the metabolite of Acitretin after chronic administration. Acitretin(Ro 10-1670) is a second-generation, systemic retinoid that has been used in the treatment of psoriasis[1][2].
L-5-Hydroxytryptophan-d3 is the deuterium labeled L-5-Hydroxytryptophan. L-5-Hydroxytryptophan (L-5-HTP), a naturally occurring amino acid and a dietary supplement for use as an antidepressant, appetite suppressant, and sleep aid, is the immediate precursor of the neurotransmitter serotonin and a reserpine antagonist[1]. L-5-Hydroxytryptophan (L-5-HTP) is used to treat fibromyalgia, myoclonus, migraine, and cerebellar ataxia[2][3][4][5].
Citalopram-d3((±)-Citalopram-d3) hydrobromide is deuterium labeled Citalopram (hydrobromide). Citalopram hydrobromide is a selective serotonin reuptake inhibitor (SSRI). Citalopram hydrobromide inhibits 5-HT uptake into synaptosomes with an IC50 of 1.8 nM. Citalopram hydrobromideinhibits the 5-HT uptake in rabbit blood platelets with an IC50 of 14 nM. Antidepressant effect .
Hydroxytyrosol-d5 is the deuterium labeled Hydroxytyrosol. Hydroxytyrosol (DOPET) is a phenolic compound drawn from the olive tree and its leaves with anti-oxidant, anti-atherogenic, anti-thrombotic, antimicrobial, anti-inflammatory and anti-tumour effects[1][2].
Hydroxytyrosol-d4 is the deuterium labeled Hydroxytyrosol. Hydroxytyrosol (DOPET) is a phenolic compound drawn from the olive tree and its leaves with anti-oxidant, anti-atherogenic, anti-thrombotic, antimicrobial, anti-inflammatory and anti-tumour effects[1][2].
Clindamycin hydrochloride monohydrate is an oral protein synthesis inhibitory agent that has the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin hydrochloride monohydrate resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin hydrochloride monohydrate decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla) .
Retinoic acid-d3-1 is the deuterium labeled Retinoic acid (HY-14649). Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha [3].
Perindopril-d3 (erbumine) is deuterated labeled Perindopril (erbumine) (HY-B0130A). Perindopril erbumine is an angiotensin-converting enzyme inhibitor. Perindopril erbumine modulates NF-κB and STAT3 signaling and inhibits glial activation and neuroinflammation. Perindopril erbumine can be used for the research of Chronic Kidney Disease and high blood pressure [3] .
(R)-Mirtazapine-d3 is a deuterium labeled (R)-Mirtazapine. (R)-Mirtazapine is a R(−)-enantiomer of Mirtazapine with antinociceptive properties in an animal model of acute thermal nociception. (R)-Mirtazapine is a 5-HT3 receptor antagonist. (R)-Mirtazapine is mainly metabolized by CYP3A4[1].
(S)-Mirtazapine-d3 is a deuterium labeled (S)-Mirtazapine. (S)-Mirtazapine is a S(+)-enantiomer of Mirtazapine with pronociceptive properties in an animal model of acute thermal nociception.(S)-Mirtazapine is a stereoselective 5-HT2 receptor antagonist. (S)-Mirtazapine is metabolized by CYP2D6 and CYP1A2[1].
Fexofenadine-d3-1 fumarate is deuterated labeled Fexofenadine (HY-B0801). Fexofenadine (MDL-16455) is an orally active and nonsedative H1 receptor antagonist. Fexofenadine can be used in allergic rhinitis and chronic idiopathic urticarial research [3].
L-741671 is a selective and brain-permeable antagonist of neurokininl (hNKI) receptor, with Kis of 64 nM, 0.03 nM and 0.7 nM in rat, human and ferret, respectively .
ML307 is a potent, sub-micromolar, first-in-class Ubc13 enzyme activity inhibitor with an IC50 of 781 nM. ML307 has the potential for immunomodulation and inflammation research .
Neochilenin (3-O-Methylquercetin 4 '-O-glucoside) is a glycoside of 3-O-methylquercetin, which can be isolated from the sub-family Cereoideae (Cactaceae). .
5'-Methylthioadenosine-d3 is the deuterium labeled 5'-Methylthioadenosine[1]. 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis. 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis[2][3][4].
3-Indoleacetic acid-d7 is the deuterium labeled 3-Indoleacetic acid (HY-18569). 3-Indoleacetic acid (Indole-3-acetic acid) is the most common natural plant growth hormone of the auxin class. It can be added to cell culture medium to induce plant cell elongation and division .
Medroxyprogesterone-d3 is the deuterium labeled Medroxyprogesterone. Medroxyprogesterone is a progestin, a synthetic variant of the human hormone progesterone and a potent progesterone receptor agonist.
N1-Methylpseudouridine-d3 is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc .
3-Indoleacetic acid-d4 (Indole-3-acetic acid-d4; 3-IAA-d4) is the deuterium labeled 3-Indoleacetic acid (HY-18569) . 3-Indoleacetic acid (Indole-3-acetic acid) is the most common natural plant growth hormone of the auxin class. It can be added to cell culture medium to induce plant cell elongation and division .
3-Indoleacetic acid-d5 is the deuterium labeled 3-Indoleacetic acid (HY-18569). 3-Indoleacetic acid-d5 can be used as internal standard for assay of IAA releases by alkaline hydrolysis of ester and amide conjugates .
Retinyl acetate-d3 (ALK-001) is a deuterated Vitamin A. Retinyl acetate-d3 can be used for research of geographic atrophy (GA) secondary to age-related macular degeneration (AMD) .
(S)-Indoximod-d3 is the deuterium labeled (S)-Indoximod. (S)-Indoximod (1-Methyl-L-tryptophan) is an inhibitor of indoleamine 2,3-dioxygenase (IDO). (S)-Indoximod can be used for the research of cancer[1][2][3].
L-Serine- 13C3, 15N,d3 is the deuterium, 13C-, and 15-labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
3-Methoxybenzeneboronic acid-d3 is the deuterium labeled 3-Methoxybenzeneboronic acid (HY-W000854). 3-Methoxybenzeneboronic acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
2'-Deoxycytidine- 15N3 is the 15N labeled 2'-Deoxycytidine[1]. 2'-Deoxycytidine, a deoxyribonucleoside, could inhibit biological effects of Bromodeoxyuridine (Brdu)[2].
Physostigmine-d3 is the deuterium labeled Physostigmine. Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning[1][2][3][4].
Ibuprofen-d3((±)-Ibuprofen-d3) sodium is the deuterium labeled Ibuprofen sodium (HY-78131C). Ibuprofen sodium is an orally active, selective COX-1 inhibitor with an IC50 value of 13 μM. Ibuprofen sodium inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen sodium is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen sodium can be used in the research of pain, swelling, inflammation, infection, immunology, cancers [3] .
Betulin-d3(Trochol-d3) is deuterium labeled Betulin. Betulin (Trochol), is a sterol regulatory element-binding protein (SREBP) inhibitor with an IC50 of 14.5 μM in K562 cell line .
Sulfadoxine-d3 is a deuterium labeled Sulfadoxine (HY-B0439). Sulfadoxine is a sulfonamide that is used, usually in combination with Pyrimethamine (HY-18062), for multidrug-resistant Plasmodium falciparum and P. vivax inhibition. Unlike PYR, Sulfadoxine has no impact on HIV replication or MT-2 cell cycle progression. But also Sulfadoxine exhibits suppression on respiratory, and urinary tract infections[1][2][3][4].
Nefopam-d3 (hydrochloride) is the deuterium labeled Nefopam hydrochloride. Nefopam hydrochloride (Fenazoxine hydrochloride) is a centrally-acting but non-opioid analgesic drug, for the relief of moderate to severe pain. Nefopam hydrochloride targets β-catenin protein level in mesenchymal cells in-vitro and in-vivo[1][2].
Levofloxacin-d3((-)-Ofloxacin-d3) hydrochlorideis deuterium labeled Levofloxacin (hydrochloride). Levofloxacin ((-)-Ofloxacin) hydrochloride is an orally active antibiotic and is active against both Gram-positive and Gram-negative bacteria. Levofloxacin hydrochloride inhibits the DNA gyrase and topoisomerase IV. Levofloxacin hydrochloride can be used for chronic periodontitis, airway inflammation and BK Viremia research. Levofloxacin hydrochloride shows anti-orthopoxvirus activity [3] .
Pyridoxine-d3 is a deuterium labeled Pyridoxine. Pyridoxine (Pyridoxol) is a pyridine derivative. Pyridoxine exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway .
Hydrocortisone-d3 is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex[1].
Eplerenone-d3 is the deuterium labeled Eplerenone. Eplerenone (Epoxymexrenone) is a selective, competitive and oreally active aldosterone antagonist with an IC50 of 138 nM. Eplerenone has low affinity for progesterone, androgen, estrogen and glucocorticoid receptors. Eplerenone can be used for hypertension and heart failure after myocardial infarction reserch[1][2].
Trigonelline-d3 (chloride) is the deuterium labeled Trigonelline chloride. Trigonelline chloride, an alkaloid with potential antidiabetic activity, is present in considerable amounts in coffee. Trigonelline chloride has anti-HSV-1 , antibacterial, and antifungal activities.
Glyburide-d3 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity[1]. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability[4]. Glibenclamide can induce autophagy[5].
Pefloxacin-d3 is the deuterium labeled Pefloxacin. Pefloxacin is a an antibacterial agent and prevents bacterial DNA replication by inhibiting DNA gyrase (topoisomerse).
Metamizole-d3 sodium is the deuterium labeled Metamizole sodium. Metamizole sodium is a non-opioid compound with excellent analgesic and antipyretic effects. Metamizole sodium is a cyclooxygenase-3(COX-3) inhibitor .
Mianserin-d3 is the deuterium labeled Mianserin (HY-B0188). Mianserin? is a Histamine 1 receptor inverse agonist and is a psychoactive agent of the tetracyclic antidepressant .
Nefopam-d3 is a deuterium labeled Nefopam (Fenazoxine). Nefopam is a centrally-acting but non-opioid analgesic drug, and Nefopam targets β-catenin protein level in mesenchymal cells[1][2].
Imidaprilat-d3(6366A-d3) is deuterium labeled Imidaprilate. Imidaprilate is an active metabolite of TA-6366, acts as a potent angiotensin converting enzyme (ACE) inhibitor, with an IC50 of 2.6 nM, and is used in the research of hypertensive disease .
DTAC-d3(Dodecyltrimethylammonium-d3 chloride) is the deuterium labeled DTAC (HY-W096983). DTAC is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
GSK345931A is an EP1 receptor antagonist. GSK345931A shows measurable CNS penetration in the mouse and rat and potent analgesic efficacy in acute and sub-chronic models of inflammatory pain .
11-Ketodihydrotestosterone-d3 is the deuterium labeled 11-Ketodihydrotestosterone. 11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells[1][2].
Sapropterin-d3((6R)-BH4-d3) is deuterium labeled Sapropterin. Sapropterin ((6R)-BH4) is an orally active phenylalanine hydroxylase (PAH) cofactor, which is effective in reducing blood phenylalanine concentrations. Sapropterin can be used in study of phenylketonuria (PKU) .
L-5-Hydroxytryptophan-d3-1 is the deuterium labeled L-5-Hydroxytryptophan[1]. L-5-Hydroxytryptophan (L-5-HTP), a naturally occurring amino acid and a dietary supplement for use as an antidepressant, appetite suppressant, and sleep aid, is the immediate precursor of the neurotransmitter serotonin and a reserpine antagonist[2]. L-5-Hydroxytryptophan (L-5-HTP) is used to treat fibromyalgia, myoclonus, migraine, and cerebellar ataxia[3][4][5][6].
Clopidogrel-d3 (hydrogen sulfate) is the deuterium labeled Clopidogrel hydrogen sulfate[1]. Clopidogrel hydrogen sulfate is an antiplatelet agent to prevent blood clots. Clopidogrel hydrogen sulfate inhibits CYP2B6 and CYP2C19 with IC50s of 18.2 nM and 524 nM, respectively. Clopidogrel hydrogen sulfate is a potent antithrombotic agent that inhibits ADP-induced platelet aggregation．Clopidogrel hydrogen sulfate also is an orally active P2Y(12) inhibitor[2][3][4][5][6].
Zidovudine- 13C,d3 is the 13C- and deuterium labeled Zidovudine. Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection.
3-Epiglycyrrhetinic acid-d3 (3α-Glycyrrhetic acid-d3) is the deuterium-labeled 3-Epiglycyrrhetinic acid. 3-Epiglycyrrhetinic acid is a derivative of glycyrrhetic acid. Glycyrrhetic acid and its derivative are considered to have anti-inflammatory, anti-ulcer, and antiviral activities .
Clindamycin (hydrochloride monohydrate) (Standard) is the analytical standard of Clindamycin (hydrochloride monohydrate). This product is intended for research and analytical applications. Clindamycin hydrochloride monohydrate is an oral protein synthesis inhibitory agent that has the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin hydrochloride monohydrate resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin hydrochloride monohydrate decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla) .
Hydrocinnamic acid-d5 is the deuterium labeled Hydrocinnamic acid[1]. Hydrocinnamic acid is the major rhizospheric compound with known growth regulatory activities[2].
Hydrocinnamic acid-d9 is the deuterium labeled Hydrocinnamic acid[1]. Hydrocinnamic acid is the major rhizospheric compound with known growth regulatory activitie[2]s.
Tricaprilin- 13C3 (Trioctanoin- 13C3) is a 13C-labeled Tricaprilin (HY-B1804) . Tricaprilin is an orally active and well tolerated ketogenic agent that safely induces ketosis. Tricaprilin restores brain electrical activity and metabolism to help counteract neuroinflammation in migraine. Tricaprilin is promising for research of migraine prevention and Alzheimer’s disease (AD). Tricaprilin is a pure C8 medium chain triglyceride (MCT) [3].
Estrone- 13C3 is the 13C-labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells[1][2].
Ritonavir- 13C3 is 13C labeled Ritonavir. Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.61 μM .
Omeprazole metabolite Omeprazole sulfone (methoxy-d3) is the deuterium labeled Omeprazole metabolite Omeprazole sulfone. Omeprazole sulfone is a metabolite of Omeprazole, which is a proton pump inhibitor.
Pyrroloquinoline quinone-13C3 (sodium) is an isotope of Pyrroloquinoline quinone. Pyrroloquinoline quinone (PQQ), a redox co-factor, is an anionic, redox-cycling orthoquinone. Pyrroloquinoline quinone is isolated from cultures of methylotropic bacteria and tissues of mammals. Pyrroloquinoline quinone is an essential nutrient for mammals and is important for immune function .
Cyromazine- 13C3 is the 13C3 labeled Cyromazine. Cyromazine is a triazine insect growth regulator used as an insecticide and an acaricide. It is a cyclopropyl derivative of melamine. Cyromazine works by affecting the nervous system of the immature larval stages of certain insects.
D-Glucose- 13C3-2 is the 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
Clomipramine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled Clomipramine (hydrochloride). Clomipramine (Chlorimipramine) hydrochloride is a potent 5-HT reuptake blocker with the IC50 value of 1.5 nM. Clomipramine hydrochloride is a tricyclic antidepressant that can be used for the research of depression and obsessive compulsive disorder (OCD)[1].
D-Glucose- 13C3-1 is the 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
Tedizolid- 13C,d3 is the 13C- and deuterium labeled Tedizolid. Tedizolid (TR 700; Torezolid; DA-7157) is a novel oxazolidinone, acting through inhibition of bacterial protein synthesis by binding to 23S ribosomal RNA (rRNA) of the 50S subunit of the ribosome.
Omeprazole sulfide-d3 is the deuterium labeled Omeprazole sulfide. Omeprazole metabolite Omeprazole sulfide (Ufiprazole) is a metabolite of Omeprazole, which is a proton pump inhibitor.
Methotrexate metabolite-d3 is the deuterium labeled Methotrexate metabolite. Methotrexate metabolite (DAMPA), the active metabolite of Methotrexate. Methotrexate is a folic acid antagonist that is widely used as an immunosuppressant and chemotherapeutic agent[1].
Trilostane-d3 is the deuterium-labeled Trilostane (HY-14281). Trilostane-d3 (Win 24540) is a competitive and orally active 3-β-hydroxysteroiddehydrogenase (3β-HSD) inhibitor. Trilostane-d3 is a synthetic nonhormonal steroid. Trilostane-d3 can be used for the research of breast cancer and prostate cancer .
Dinotefuran-d3 is the deuterium labeled Dinotefuran[1]. Dinotefuran is an insecticide of the neonicotinoid class, its mechanism of action involves disruption of the insect's nervous system by inhibiting nicotinic acetylcholine receptors[2].
Mexiletine-d3 (hydrochloride) is deuterium labeled Mexiletine (hydrochloride). Mexiletine hydrochloride (KOE-1173 hydrochloride), a Class IB antianhythmic, is a non-selective voltage-gated sodium channel blocker[1][2].
Flunixin-d3 is the deuterium labeled Flunixin. Flunixin Meglumine is a potent inhibitor of COX used as analgesic agent with anti-inflammatory and antipyretic activity[1][2].
Flumatinib-d3 is deuterium labeled Flumatinib. Flumatinib (HHGV678) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib inhibits c-Abl, PDGFRβ and c-Kit with IC50s of 1.2 nM, 307.6 nM and 665.5 nM, respectively[1].
Parbendazole-d3 is the deuterium labeled Parbendazole. Parbendazole is a potent inhibitor of microtubule assembly, destabilizes tubulin, with an EC50 of 530 nM, and exhibits a broad-spectrum anthelmintic activity.
Acalabrutinib-d3(ACP-196-d3) is the deuterated form of Acalabrutinib (HY-17600). Acalabrutinib (ACP-196) is an orally active, irreversible, highly selective second-generation BTK inhibitor. Acalabrutinib covalently binds to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib shows strong targeting and efficacy in mouse models of chronic lymphocytic leukemia (CLL).
Ritodrine-d3 (hydrochloride) is the deuterium labeled Ritodrine (hydrochloride). Ritodrine hydrochloride (DU21220 hydrochloride) is a β-2 adrenergic receptor agonist.
Elimusertib-d3 (BAY 1895344-d3) is the deuterium labeled Elimusertib (BAY 1895344). Elimusertib is a potent, orally active and selective ATR inhibitor and has anti-tumor activity .
Ozenoxacin-d3 is the deuterium-labeled Ozenoxacin (HY-14957). Ozenoxacin-d3 is a nonfluorinated quinolone antibacterial, which shows potent activities against the main microorganisms isolated from skin and soft tissue infections.
Cinacalcet-d3 is the deuterium labeled Cinacalcet. Cinacalcet (AMG 073) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.
Sulindac-d3 is deuterium labeled Sulindac. Sulindac (MK-231) is a non-steroidal antiinflammatory agent, acts as a COX-2 inhibitor, and inhibits overexpression of COX-2.
Nordoxepin-d3 (hydrochloride) is the deuterium labeled Nordoxepin hydrochloride. Nordoxepin hydrochloride is an active metabolite of Doxepin hydrochloride (HY-B0725), which is an orally active tricyclic antidepressant[1].
Pazopanib-d3(GW786034-d3) is deuterium labeled Pazopanib. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively .
Fluorofenidone-d3 is deuterium labeled Fluorofenidone. Fluorofenidone (AKF-PD), an analogue of AMR69, shows equivalent antifibrotic activity, lower toxicity and longer half-life. Fluorofenidone (AKF-PD) attenuates the progression of renal interstitial fibrosis partly by suppressing NADPH oxidase and extracellular matrix (ECM) deposition via the PI3K/Akt signalling pathway[1][2].
Methoxyamine-d3 (O-Methylhydroxylamine-d3) hydrochloride is the deuterium labeled Methoxyamine hydrochloride. Methoxyamine hydrochloride is an orally active and potent base excision repair (BER) inhibitor .
Amitraz-d3 is the deuterium labeled Amitraz. Amitraz is a non-systemic acaricide and insecticide, with alpha-adrenergic agonist activity, interaction with octopamine receptors of the central nervous system and inhibition of monoamine oxidases and prostaglandin synthesis.
Albendazole-d3 is the deuterium labeled Albendazole, which is a member of the benzimidazole compounds used as a agent indicated for the treatment of a variety of worm infestations[1].
Capsaicin-d3 is the deuterium labeled Capsaicin. Capsaicin ((E)-Capsaicin), an active component of chili peppers, is a TRPV1 agonist. Capsaicin has pain relief, antioxidant, anti-inflammatory, neuroprotection and anti-cancer effects[1][2].
Apalutamide-d3 is the deuterium labeled Apalutamide[1]. Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM[2].
Celecoxib-d3 is the deuterium labeled Celecoxib. Celecoxib,a selective non-steroidal anti-inflammatory drug (NSAID), is a selective COX-2 inhibitor with an IC50 of 40 nM[1][2].
Tadalafil-d3 is the deuterium labeled Nortadalafil. Nortadalafil is demethyl Tadalafil, which is a PDE5 inhibitor, currently marketed in pill form for treating erectile dysfunction (ED) under the name Cialis; and under the name Adcirca for the treatment of pulmonary arterial hypertension.
Glycyrrhizic acid-d3(Glycyrrhizin-d3) is deuterium labeled Glycyrrhizic acid. Glycyrrhizic acid is a triterpenoid saponinl, acting as a direct HMGB1 antagonist, with anti-tumor, anti-diabetic activities .
Parecoxib-d3 is the deuterium labeled Parecoxib. Parecoxib (SC 69124) is a highly selective and orally active COX-2 inhibitor, the proagent of Valdecoxib (HY-15762). Parecoxib Sodium is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits prostaglandin (PG) synthesis. Parecoxib can be used for the relief of acute postoperative pain and symptoms of chronic inflammatory conditions such as osteoarthritis and rheumatoid arthritis in vivo.
Eprinomectin-d3(MK-397-d3) is the deuterium-labeled Eprinomectin (HY-12643). Eprinomectin is a type of avermectin. Eprinomectin，as a broad-spectrum fungicide，has insecticidal，insecticidal and acaricidal activities. Eprinomectin induces apoptosis and autophagy in prostate cancer cells and has antitumor activity .
Flurbiprofen-d3 is the deuterium labeled Flurbiprofen. Flurbiprofen (dl-Flurbiprofen) is a potent, orally active nonsteroidal anti-inflammatory agent (NSAIA/NSAID), with antipyretic and analgesic activities. Flurbiprofen is commonly used for the research of inflammatory diseases, including osteoarthritis and rheumatoid arthritis. Flurbiprofen is a non-selective cyclooxygenase (COX) inhibitor that can be used for the research of colorectal cancer[1][2][3].
Puromycin-d3 (dihydrochloride) is the deuterium labeled Puromycin dihydrochloride. Puromycin dihydrochloride (CL13900 dihydrochloride), an aminonucleoside antibiotic, inhibits protein synthesis[1].
Aspartame-d3 is the deuterium labeled Aspartame. Aspartame (SC-18862) is a methyl ester of a dipeptide. Aspartame can be used as a synthetic nonnutritive sweetener. Aspartame is composed of phenylalanine (50%), aspartic acid (40%) and methanol (10%)[1][2].
Cimetidine-d3 is the deuterium labeled Cimetidine. Cimetidine (SKF-92334) is an orally active and inverse histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine is an inverse agonist. Cimetidine has anti-cancer and anti-inflammatory activity[1][2][5].
Spironolactone-d3 is the deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC50 of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes[1][2][3].
Captopril-d3 is deuterium labeled Captopril. Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM[1][2][3].
Valsartan-d3 is the deuterium labeled Valsartan[1]. Valsartan (CGP 48933) is an angiotensin II receptor antagonist and has the potential for high blood pressure and heart failure research[2].
Guaiacol-d3 is the deuterium labeled Guaiacol. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Guaiacol has an anti-inflammatory activity[1].
Nintedanib-d3 is the deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
Bergapten-d3 is deuterium labeled Bergapten. Bergapten is a natural anti-inflammatory and anti-tumor agent. Bergapten is inhibitory towards mouse and human CYP isoforms.
Olanzapine-d3 is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic[1][2].
Oseltamivir-d3 (phosphate)eis the deuterium labeled Oseltamivir phosphate. Oseltamivir phosphate (GS 4104) is a neuraminidase inhibitor recommended for the treatment and prophylaxis of influenza A and B.
Nemonoxacin-d3 is the deuterium labeled Nemonoxacin. Nemonoxacin (TG-873870) is an orally active and potent broad-spectrum antibiotic. Nemonoxacin shows good inhibitory activity against different species of staphylococci, streptococci, and enterococci, Neisseria gonorrhoeae, and Haemophilus influenza. Nemonoxacin can be used in the study of bacterial infections and community-acquired pneumonia[1][2][3].
Ampyrone-d3 is the deuterium labeled Ampyrone. Ampyrone is a metabolite of Metamizole sodium (HY-B1279A). Ampyrone is a PGE2-dependent blocker and inhibitor of COX .
Piroxicam-d3 is deuterium labeled Piroxicam. Piroxicam is a non-steroidal anti-inflammatory drugs, acts as a COX inhibitor, with IC50s of 47, 25 μM for human monocyte COX-1 and COX-2, respectively [1].
L-Hyoscyamine-d3 is the deuterium labeled L-Hyoscyamine. L-Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine is a levo-isomer to Atropine (HY-B1205)[1][2].
Prasugrel-d3 is the deuterium labeled Prasugrel. Prasugrel (PCR 4099), a thienopyridine and proagent, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation[1].
Saracatinib-d3 (AZD0530-d3) (ZG5129) is the deuterium-labeled analog of Saracatinib (HY-10234). Saracatinib-d3 is an inhibitor of the Src kinase, which can inhibit severe sepsis caused by bacterial or various microbial infections .
Sarpogrelate-d3 (hydrochloride) is the deuterium labeled Sarpogrelate hydrochloride. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis[1][2][3].
Agomelatine-d3 is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively[1]. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively[2].
Naproxen-d3 is the deuterium labeled Naproxen. Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Ergothioneine-d3 is the deuterium labeled Ergothioneine. Ergothioneine, an imidazole-2-thione derivative of histidine betaine, is synthesized by certain bacteria and fungi. Ergothioneine is generally considered an antioxidant[1].
Diflunisal-d3 is the deuterium labeled Diflunisal. Diflunisal (MK-647) is a salicylate derivative with nonsteroidal anti-inflammatory and uricosuric properties, which is used alone as an analgesic and in rheumatoid arthritis patients. The mechanism of action of diflunisal is as a Cyclooxygenase (COX) Inhibitor.
Methylprednisolone-d3 is the deuterium labeled Methylprednisolone. Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels[3].
Linezolid-d3 is a deuterium labeled Linezolid (PNU-100766). Linezolid is a synthetic antibiotic that acts by inhibiting the initiation of bacterial protein synthesis[1].
Valdecoxib-d3 is the deuterium labeled Valdecoxib. Valdecoxib is a highly potent and selective inhibitor of COX-2, with IC50s of 5 nM and 140 μM for COX-2 and COX-1, respeceively. Valdecoxib can be used in the research of arthritis and pain[1][2].
(±)-Duloxetine-d3 (hydrochloride) is deuterium labeled (±)-Duloxetine (hydrochloride). (±)-Duloxetine ((Rac)-Duloxetine) hydrochloride is the racemate of Duloxetine hydrochloride. Duloxetine hydrochloride, a serotonin-norepinephrine reuptake inhibitor, can be used for diabetic neuropathic pain and fibromyalgia as well as major depressive disorder research[1].
Tasquinimod-d3 (ABR-215050-d3) is the deuterium labeled Tasquinimod (HY-10528). Tasquinimod is an oral antiangiogenic agent, which plays an important role in castration-resistant prostate cancer. Tasquinimod binds to the regulatory Zn 2+ binding domain of HDAC4 with Kd of 10-30 nM. Tasquinimod also is a S100A9 inhibitor [3].
Ozenoxacin-d3 (hydrochloride) is the deuterium labeled Ozenoxacin hydrochloride. Ozenoxacin hydrochloride is a nonfluorinated quinolone antibacterial, which shows potent activities against the main microorganisms isolated from skin and soft tissue infections[1][2][3].
Penicillamine-d3 is the deuterium labeled Penicillamine. Penicillamine (D-(-)-Penicillamine) is the most characteristic degradation product of the penicillin antibiotics. It is used as an antirheumatic and as a chelating agent in Wilson's disease.
Pomalidomide-d3 is the deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors[1][2].
Isoeugenol-d3 is deuterated labeled Sterigmatocystine (HY-N6725). Sterigmatocystine is a precursor of aflatoxins and a mycotoxin produced by common mold strains from Aspergillus versicolor . Sterigmatocystine, a inhibitor of G1 Phase and DNA synthesis, is used to inhibit p21 activity. Sterigmatocystine has teratogenic, and carcinogenic effects in animals [3].
Eugenol acetate-d3 is deuterated labeled Decyl aldehyde (HY-W012570). Decyl aldehyde is a simple ten-carbon aldehyde. Decyl aldehyde is a bacterial luciferase substrate.
Axitinib-d3 (AG-013736-d3) is deuterium labeled Axitinib. Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively[1].
Ropinirole-d3 (hydrochloride) is the deuterium labeled Ropinirole hydrochloride[1]. Ropinirole (SKF 101468) hydrochloride is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease[2][3].
Nabumetone-d3 is the deuterium labeled Nabumetone. Nabumetone is an orally active non-acidic anti-inflammatory agent, acts as a potent and selective COX-2 inhibitor, and is the proagent of the active metabolite 6MNA.
Eletriptan-d3 is the deuterium labeled Eletriptan hydrobromide. Eletriptan hydrobromide is a selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively[1][2].
Vericiguat-d3 (BAY1021189-d3) hydrochloride is a deuterated Vericiguat with tracer functionality. Vericiguat is an orally available stimulator of guanylate cyclase .
Voriconazole-d3 is the deuterium labeled Voriconazole. Voriconazole (UK-109496) is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes[1][2].
Triptolide-d3 is the deuterium labeled Triptolide. Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory, antiproliferative and antitumour effects. Triptolide is a NF-κB activation inhibitor[1][2][3][4][5][6].
Tenidap-d3 is the deuterium labeled Tenidap. Tenidap, a non-steroidal anti-inflammatory drug, is a selective COX-1 inhibitor, with IC50 values of 0.03 μM and 1.2 μM for COX-1 and COX-2, respectively. Tenidap has anti-inflammatory and antirheumatic properties[1][2]. Tenidap is also a specific SLC26A3inhibitor[3].
Etiracetam-d3 is the deuterium labeled Etiracetam. Etiracetam (UCB 6474) is an acetylcholine agonist and a nootropic drug of the racetam family. Less active than its S-enantiomer Levetiracetam (UCB L059)[1].
Medetomidine-d3 (hydrochloride) is the deuterium labeled Medetomidine hydrochloride. Medetomidine hydrochloride is an agonist of adrenergic alpha-2 receptor[1][2].
Nicardipine-d3 (hydrochloride) (YC-93 D3) is the deuterium labeled Nicardipine hydrochloride. Nicardipine hydrochloride is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine hydrochloride acts as an agent for chronic stable angina and for controlling blood pressure[1].
Raltegravir-d3 (potassium) is the deuterium labeled Raltegravir potassium. Raltegravir (MK 0518) potassium is a potent integrase (IN) inhibitor, used to treat HIV infection[1][2].
Sodium 2-oxopropanoate-d3 is the deuterium labeled Sodium 2-oxopropanoate[1]. Sodium 2-oxopropanoate (Sodium pyruvate), a three-carbon metabolite of Glucose, is a compound produced in the glycolytic pathway. Sodium 2-oxopropanoate is a free radical scavenger that can scavenge ROS[2][3].
Terbinafine-d3 (hydrochloride) is the deuterium labeled Terbinafine hydrochloride. Terbinafine hydrochloride (TDT 067 hydrochloride) is an antifungal medication used to treat fungal infections. It is a potent non-competitive inhibitor of squalene epoxidase from Candida with a Ki of 30 nM[1][2]. Terbinafine hydrochloride also antibacterial activity against certain Gram-positive and Gram-negative bacteria[3].
Acetohydrazide-d3 (Ethanehydrazonic acid-d3) is deuterium labeled Acetohydrazide. Acethydrazide is an organic building that undergo catalytic hydrogenation to produce N′-methyl acethydrazide (MAH) .
Omeprazole-d3 sodium is deuterated labeled Omeprazole (HY-B0113). Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) [3].
Acetylpyrazine-d3 is deuterated labeled Linalyl acetate (HY-N6948). Linalyl acetate is the principal components of many plant essential oils with potentially anti-inflammatory activity .
HMMNI-d3 is deuterium labeled HMMNI. HMMNI (Hydroxy dimetridazole) is a hydroxy metabolite of Dimetridazole. Dimetridazole is a nitroimidazole class agent that combats protozoan infections[1].
Clozapine-d3 (HF 1854-d3) is deuterium labeled Clozapine. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively [3]. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) [3] .
Moxidectin-d3(CL-301423-d3) is deuterium labeled Moxidectin. Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk [3] .
Ketoprofen-d3 is the deuterium labeled Ketoprofen. Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC50s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively[1].
Apremilast-d3(CC-10004-d3) is deuterium labeled Apremilast. Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM .
Regadenoson-d3 is the deuterium labeled Regadenoson. Regadenoson (CVT-3146) is a potent and selective A2A adenosine receptor agonist, with Kis of 290 and 1120 nM for rat and pig adenosine A2A receptor, respectively. Regadenoson is selective for the adenosine A2A receptor over adenosine A1 and A2B receptors, and shows 13-fold selectivity over the human adenosine A1 receptor. Regadenoson is a vasodilator stress agent has shifted the landscape of vasodilator myocardial perfusion imaging. Regadenoson increases blood-brain barrier (BBB) permeability in rodents[1][2][3].
Puromycin-d3 is the deuterium labeled Puromycin. Puromycin dihydrochloride is the dihydrochloride salt of puromycin. Puromycin is an aminoglycoside antibiotic that inhibits protein synthesis.
Rabeprazole-d3 (sodium)mis the deuterium labeled Rabeprazole sodium. Rabeprazole sodium (LY307640 sodium) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H+/K+-ATPase. Rabeprazole sodium induces apoptosis. Rabeprazole sodium acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole sodium can be used for the research of gastric ulcerations and gastroesophageal reflux[1][2][3].
Cinacalcet-d3 (hydrochloride) is the deuterium labeled Cinacalcet (hydrochloride). Cinacalcet hydrochloride (AMG-073 hydrochloride) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.
Estradiol benzoate-d3 is the deuterium labeled Estradiol benzoate. Estradiol Benzoate (β-Estradiol 3-benzoate), a proagent of estradiol, acts as a steroid sex hormone. It exhibits mild anabolic and metabolic properties, and increases blood coagulability[1][2][3][4].
L-Serine- 13C3 is the 13C-labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
Lamotrigine- 13C3 is the 13C-labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al[1][2].
3-O-Methyldopa-d3 (hydrate) is the deuterium labeled 3-O-Methyldopa. 3-O-Methyldopa (3-Methoxy-L-tyrosine) is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of l-DOPA and dopamine[1].
8-CPT-Cyclic AMP (8-CPT-cAMP) sodium is a selective activator of cyclic AMP-dependent protein kinase (PKA). 8-CPT-Cyclic AMP sodium is also a potent inhibitor of the cyclic GMP-specific phosphodiesterase (PDE VA) with an IC50 of 0.9 μM. 8-CPT-Cyclic AMP sodium also inhibits PDE III and PDE IV with IC50 s of 24 and 25 μM, respectively. 8-CPT-Cyclic AMP sodium is a very high affinity for Epac and is a potent Epac activator .
Clindamycin is an orally active and broad-spectrum bacteriostatic lincosamide antibiotic. Clindamycin can inhibit bacterial protein synthesis, possessing the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla). Clindamycin also can be used for researching malaria .
1,2-Cyclohexylenedinitrilotetraacetic acid (CDTA) is a chelating agent. 1,2-Cyclohexylenedinitrilotetraacetic acid has an ability to remove manganese from brain and liver (in vivo) and their sub-cellular fractions (in vitro), of rats pretreated with manganese sulphate .
IPR-803 is a potent inhibitor of the uPAR·uPA protein-protein interaction (PPI). IPR-803 binds directly to uPAR with sub-micromolar affinity. IPR-803 displays anti-tumor activity .
Ecopladib is a sub-micromolar inhibitor of cytosolic phospholipase A2α (cPLA2α), with IC50s of 0.15 μM and 0.11 μM in the GLU micelle and rat whole blood assays, respectively.
Thiamine- 13C3 (hydrochloride) is the 13C-labeled Thiamine (hydrochloride). Thiamine hydrochloride (Thiamine chloride hydrochloride) is an essential micronutrient needed as a cofactor for many central metabolic enzymes.
AalphaC- 15N3 (2-Amino-α-carboline- 15N3) is 15N labeled AalphaC. AalphaC (AαC) is a potential carcinogen with carcinogenic activity. AalphaC is an important biomarker in tobacco smoke and is associated with tobacco smoke exposure. Urinary concentrations of AalphaC are significantly higher in dedicated smokers than in non-smokers, indicating its importance in monitoring tobacco exposure. AalphaC levels increase significantly with increasing serum nicotine levels, indicating its close relationship with tobacco use. In addition, consuming high-temperature cooked beef significantly increases the amount of AalphaC in urine, while consuming vegetables is associated with a decrease in AalphaC concentrations. Smoking half a pack of cigarettes is associated with a significant increase in the amount of AalphaC, which further confirms the biological activity of AalphaC and its association with dietary habits .
Rasagiline- 13C3 ((R)-AGN1135- 13C3; TVP1012- 13C3) mesylate is the deuterium labeled Rasagiline (mesylate) (HY-14605) . Rasagiline (R-AGN1135) mesylate is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively .
Sildenafil-d3-1 (UK-92480-d3-1) is deuterium labeled Sildenafil-d3. Sildenafil (UK-92480) is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM.
L-DOPA-d6 is the deuterium labeled L-DOPA. L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease[1][2][3].
Butylphthalide-d9(3-n-Butylphthalide-d9) is deuterium labeled Butylphthalide. Butylphthalide (3-n-Butylphthalide) is an active molecule against cerebral ischemia. It was originally isolated from celery species and has been shown to be effective in stroke animal models .
Etonogestrel-d6 is deuterium labeled Etonogestrel. Etonogestrel (3-Oxodesogestrel), a biologically active metabolite of progestin Desogestrel, binds with high affinity to progesterone receptors and estrogen receptors in the target organs[1]. Etonogestrel induce FKBP51 mRNA and protein expression in cultured human endometrial stromal cells (HESCs)[2].
(±)-1,2-Propanediol- 13C3 is 13C labeled (±)-1,2-Propanediol (HY-Y0921). (±)-1, 2-propanediol (1,2-(RS)-Propanediol) is an aliphatic alcohol that is often used as an excipient in many active molecular preparations to increase the solubility and stability of the active molecule. (±)-1, 2-propanediol can affect the neurobehavior of zebrafish .
Oseltamivir acid-13C,d3 (GS 4071-13C,d3; Ro 64-0802-13C,d3) is a 13C- and deuterium-labeled Oseltamivir acid (HY-13318). Oseltamivir acid is the active metabolite of Oseltamivir phosphate and inhibits influenza virus neuraminidase (IC50=2 nM). Oseltamivir acid is orally active and can be used to study influenza A/B infections [3] .
Docosanoic acid-d3 (Behenic acid-d3) is the deuterium labeled Docosanoic acid (HY-W013049). Docosanoic acid (Behenic acid) is a long-chain saturated fatty acid. Docosanoic acid inhibits the double-stranded DNA (dsDNA) binding activity of p53 DNA binding domain, with a Kd of 12 nM. Docosanoic acid has low bioavailability and can increase cholesterol in humans [3].
(Rac)-Levomepromazine-d3 (hydrochloride) is a labelled racemic Methotrimeprazine, which is a phenothiazine which has antagonist actions at multiple neurotransmitter receptor sites, including dopaminergic, cholinergic, serotonin and histamine receptors[1][2].
Lignoceric acid-d3 is the deuterium labeled Lignoceric acid[1]. Lignoceric acid (Tetracosanoic acid) is a 24-carbon saturated (24:0) fatty acid, which is synthesized in the developing brain. Lignoceric acid is also a by-product of lignin production. Lignoceric acid can be used for Zellweger cerebro‐hepato‐renal syndrome and adrenoleukodystrophy research[2][3].
Ipratropium-d3 (bromide) is the deuterium labeled Ipratropium bromide. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with binding IC50 values of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma[1][2][3].
Galanthamine-d3 (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD)[1][2][3].
Nonanoic acid-d3 is the deuterium labeled Nonanoic acid. Nonanoic acid is a naturally-occurring saturated fatty acid with nine carbon atoms. Nonanoic acid significantly reduces bacterial translocation, enhances antibacterial activity, and remarkably increases the secretion of porcine β-defensins 1 (pBD-1) and pBD-2[1].
(Rac)-Rotigotine-d3 hydrochloride is a deuterium labeled (Rac)-Rotigotine (hydrochloride) (HY-15394). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
Triclabendazole sulfoxide-d3 is the deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP[1][2].
(R)-(-)-Ibuprofen-d3 is the deuterium labeled (R)-(-)-Ibuprofen. (R)-(-)-Ibuprofen is the R enantiomer of Ibuprofen, inactive on COX, inhibits NF-κB activation; (R)-(-)-Ibuprofen exhibits anti-inflammatory and antinociceptive effects.
Apixaban-d3(BMS-562247-01-d3) is the deuterium labeled Apixaban (HY-50667) . Apixaban (BMS-562247-01) is a highly selective, reversible and orally active inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively . Apixaban is in development for the prevention and treatment of various thromboembolic diseases [3].
Tetrahydrodeoxycorticosterone-d3 is the deuterium labeled Tetrahydrodeoxycorticosterone. Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties[1][2][3].
(S)-(+)-Ibuprofen-d3 is a deuterium labeled (S)-(+)-Ibuprofen. (S)-(+)-Ibuprofen is the S(+)-enantiomer of Ibuprofen that inhibits COX-1 and COX-2 activity with IC50s of 2.1 μM and 1.6 μM. (S)-(+)-Ibuprofen has analgesic, antiinflammatory and antipyretic effects[1][2].
Decanoyl-L-carnitine-d3((-)-Decanoylcarnitine-d3) is deuterium labeled Decanoyl-L-carnitine. Decanoyl-L-carnitine has stimulatory effect on the formation of desaturated fatty acid metabolites from both [1- 14C]-22:4 (n-6) and [1- 14C]-22:5 (n-3) [3].
Homovanillic acid-d3 is the deuterium labeled Homovanillic acid. Homovanillic acid is a dopamine metabolite found to be associated with aromatic L-amino acid decarboxylase deficiency, celiac disease, growth hormone deficiency, and sepiapterin reductase deficiency.
4-Hydroxynonenal-d3 is the deuterium labeled 4-Hydroxynonenal. 4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal and an oxidative/nitrosative stress biomarker. 4-Hydroxynonenal is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2). 4-Hydroxynonenal can modulate a number of signaling processes mainly through forming covalent adducts with nucleophilic functional groups in proteins, nucleic acids, and membrane lipids. 4-Hydroxynonenal plays an important role in cancer through mitochondria[1][2][3].
Octanoic acid-d3 is the deuterium labeled Octanoic acid. Octanoic acid (Caprylic acid) is an oily liquid with a slightly unpleasant rancid taste and used commercially in the production of esters used in perfumery and also in the manufacture of dyes.
Triciribine phosphate-d3 (TCN-P-d3) is a deuterated compound of Triciribine phosphate (TCN-P). TCN-P inhibits adenosine monophosphate (AMP)-activated protein kinase through an allosteric mechanism, affecting the first key step in de novo purine biosynthesis. Triciribine phosphate also inhibits inosine monophosphate dehydrogenase, which is the first key step in guanosine nucleotide synthesis. Triciribine phosphate does not affect ligase activity .
Mometasone furoate-d3 is a deuterium labeled Mometasone furoate. Mometasone furoate (Sch32088) is a glucocorticoid receptor agonist with anti-inflammatory and anti-allergic activity[1].
Cyclobenzaprine-d3 (hydrochloride) is the deuterium labeled Cyclobenzaprine hydrochloride. Cyclobenzaprine hydrochloride (MK130 hydrochloride) is a skeletal muscle relaxant and a central nervous system (CNS) depressant.
Prednisone acetate-d3 is the deuterium labeled Prednisone acetate. Prednisone acetate (Prednisone 21-acetate), the acetate salt form of prednisolone, is a glucocorticoid receptor agonist with anti-inflammatory and immunomodulating properties[1].
Exatecan-d3(DX8951f-d3) mesylate is deuterium-labeled Exatecan mesylate (HY-13631A). Exatecan mesylate is a DNA topoisomerase I inhibitor, with an IC50 of 0.975 μg/mL .
Ulipristal acetate-d3(CDB-2914-d3) is deuterium labeled Ulipristal acetate. Ulipristal acetate (CDB-2914) is an orally active, selective progesterone receptor modulator (SPRM). Ulipristal acetate stimulates the autophagic response selectively in leiomyoma cells. Ulipristal acetate has the potential for benign gynecological conditions treatment, such as uterine myoma [3].
Carbidopa-d3-1 is the deuterium labeled Carbidopa (HY-B0311). Carbidopa, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa inhibits pancreatic cancer cell and tumor growth .
N,N-Dimethylacetamide-d3 is the deuterium labeled N,N-Dimethylacetamide[1]. N,N-Dimethylacetamide (DMAc) is an inexpensive, common aprotic organic solvent[2].
ar-Turmerone-d3 is the deuterium labeled ar-Turmerone. ar-Turmerone ((+)-ar-Turmerone) is a major bioactive compound of the herb Curcuma longa with anti-tumorigenesis and anti-inflammatory activities. ar-Turmerone induces apoptosis in U937 cells. ar-Turmerone exerts positive modulation on murine DCs. ar-Turmerone induces NSC proliferation in vitro and in vivo, and can be used for various neurologic disorders study [3] .
Arachidic acid-d3) is the deuterium labeled Arachidic acid. Arachidonic acid (Icosanoic acid), a long-chain fatty acid, is present in all mammalian cells, typically esterified to membrane phospholipids, and is one of the most abundant polyunsaturated fatty acids present in human tissue[1][2].
D-Serine-d3((R)-Serine-d3) is a deuterium labeled D-Serine (HY-100808). D-Serine ((R)-Serine), an endogenous amino acid involved in glia-synapse interactions that has unique neurotransmitter characteristics, is a potent co-agonist at the NMDA glutamate receptor. D-Serinee has a cardinal modulatory role in major NMDAR-dependent processes including NMDAR-mediated neurotransmission, neurotoxicity, synaptic plasticity, and cell migration [3].
Velpatasvir-d3(GS-5816-d3) is deuterium labeled Velpatasvir. Velpatasvir (VEL, GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons. Velpatasvir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 2.16 μM [3].
Glycopyrrolate-d3 (bromide) is deuterium labeled Glycopyrrolate. Glycopyrrolate (Glycopyrronium bromide), a quaternary ammonium derivative, is a muscarinic receptor antagonist. Glycopyrrolate has bronchoprotective effect and produces a beneficial effect on blood pressure. Glycopyrrolate can be used for the research of bronchial diseases [3] .
Alfuzosin-d3 hydrochloride is the deuterium labeled Alfuzosin hydrochloride. Alfuzosin hydrochloride is an α1 adrenergic receptor antagonist used to treat benign prostatic hyperplasia (BPH).
Abiraterone acetate-d3(CB7630-d3) is deuterium labeled Abiraterone acetate. Abiraterone acetate (CB7630) is an oral, potent, selective, and irreversible inhibitor of CYP17A1 with antiandrogen activity. Abiraterone acetate is a proagent form of Abiraterone (CB7598) .
SN-38-d3 is the deuterium labeled SN-38. SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively[1][2][3][4].
Tropicamide-d3 is the deuterium labeled Tropicamide[1]. Tropicamide (Ro 1-7683) is a selective M4 muscarinic acetylcholine receptor antagonist. Tropicamide produces short acting mydriasis (dilation of the pupil) and cycloplegia when applied as eye drops[2][3].
Trans-Anethole-d3 is deuterated labeled α-Terpineol (HY-N5142). α-Terpineol is isolated from Eucalyptus globulus Labill, exhibits strong antimicrobial activity against periodontopathic and cariogenic bacteria .
α-Terpineol possesses antifungal activity against T. mentagrophytes, and the activity might lead to irreversible cellular disruption .
2-Methoxybenzaldehyde-d3 is the deuterium labeled 2-Methoxybenzaldehyde[1]. 2-Methoxybenzaldehyde (o-Anisaldehyde), isolated from cinnamon essential oil (CEO), exists antibacterial and antifungal activity[2].
Finerenone-d3 is the deuterium labeled finerenone (HY-111372). Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
TRIA-662-d3 is the deuterium labeled TRIA-662[1]. TRIA-662 (1-Methylnicotinamide chloride) is an endogenous metabolite. TRIA-662 shows antithrombotic and anti-inflammatory activities[2].
Nisoldipine-d3 is deuterated labeled Nisoldipine (HY-17402). Nisoldipine (BAY-k 5552; Sular) is a highly efficient and specific L-type Cav1.2 channel blocker with an IC50 of 10 nM.
Carbidopa-d3 (monohydrate) is the deuterium labeled Carbidopa monohydrate. Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa monohydrate is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa monohydrate inhibits pancreatic cancer cell and tumor growth[1][2].
Dolutegravir-d3 is the deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2].
4-Methylanisole-d3 is the deuterium labeled 4-Methylanisole[1]. 4-Methylanisole (4-Methoxytoluene) is food flavoring agent and can be naturally found in Ylang Ylang fragrance oil[2].
Mianserin-d3 (hydrochloride) is the deuterium labeled Mianserin hydrochloride. Mianserin hydrochloride (Org GB 94) is a H1 receptor inverse agonist and is a psychoactive agent of the tetracyclic antidepressant.
Theobromine-d3 is the deuterium labeled Theobromine. Theobromine is a methylxanthine found in cacao beans which can inhibit adenosine receptor A1 (AR1) signaling.
Moxifloxacin-d3 (hydrochloride) is the deuterium labeled Moxifloxacin hydrochloride. Moxifloxacin hydrochloride is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia[1][2][3].
Geranylgeraniol is an orally acitve vitamin K2sub-type, an intermediate of the mevalonate pathway. Geranylgeraniol targets NF-kB signaling pathway and could alleviate LPS-induced microglial inflammation in animal model [3] .
Antibacterial agent 268 (Compound 10e) is an antibacterial agent with antimycobacterial properties. Antibacterial agent 268 shows high anti-bacterial properties at sub-micromolar values (MIC=0.44-0.07 μM) .
N6-Methyladenosine- 13C3 (6-Methyladenosine- 13C3) is 13C-labeled N6-Methyladenosine (HY-N0086). N6-Methyladenosine is the most prevalent internal (non-cap) modification present in the messenger RNA (mRNA) of all higher eukaryotes. N6-Methyladenosine can modifies viral RNAs and has antiviral activities [3].
Imazamox- 13C,d3 is the 13C- and deuterium labeled Imazamox. Imazamox (CL29926) is a systemic herbicide that inhibits the production of acetolactate synthase (ALS) in plants with high selectivity, high activity, safety and broadspectrum activity, which would then inhibit plant growth and ultimately lead to plant death[1][2].
Rapamycin- 13C,d3 (Sirolimus- 13C,d3; AY-22989- 13C,d3) is the 13C and deuterium labeled Rapamycin (HY-10219) .Rapamycin is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant .
Ritonavir- 13C,d3 is the 13C- and deuterium labeled Ritonavir. Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.61 μM.
Rasagiline- 13C3 (mesylate racemic) is a 13C-labeled Rasagiline mesylate racemic. Rasagiline mesylate racemic is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor[1]. Rasagiline-13C3 (mesylate racemic) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
17α-Hydroxyprogesterone- 13C3 is the 13C-labeled 17α-Hydroxyprogesterone. 17α-Hydroxyprogesterone (17-Hydroxyprogesterone) is an endogenous progestogen as well as chemical intermediate in the biosynthesis of other steroid hormones, including the corticosteroids and the androgens and the estrogens.
Dexmedetomidine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled Dexmedetomidine (hydrochloride). Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine hydrochloride shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine hydrochloride exhibits anxiolysis, sedation, and modest analgesia effects[1][2][3].
Osimertinib- 13C,d3 is the deuterium and 13C labeled Osimertinib. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively.
Cytidine-5'-triphosphate- 15N3,d14 (Cytidine triphosphate- 15N3,d14 dilithium; 5'-CTP- 15N3,d14) dilithium is deuterium and 15N labeled Cytidine-5'-triphosphate (HY-125818). Cytidine 5′-triphosphate (Cytidine triphosphate; 5'-CTP) is a nucleoside triphosphate and serves as a building block for nucleotides and nucleic acids, lipid biosynthesis. Cytidine triphosphate synthase can catalyze the formation of cytidine 5′-triphosphate from uridine 5′-triphosphate (UTP). Cytidine 5′-triphosphate is an essential biomolecule?in the de novo?pyrimidine biosynthetic pathway in?T. gondii.
Deoxycytidine triphosphate- 15N3,d14 (dCTP- 15N3,d14 dilithium; 2′-Deoxycytidine-5′-triphosphate- 15N3,d14) dilithium is deuterium and 15N labeled Deoxycytidine triphosphate (HY-101400). Deoxycytidine triphosphate (dCTP) is a nucleoside triphosphate that can be used for DNA synthesis. Deoxycytidine triphosphate has many applications, such as real-time PCR, cDNA synthesis, and DNA sequencing.
PD 407824 is a checkpoint kinase Chk1 and WEE1 inhibitor with IC50s of 47 and 97 nM, respectively. PD 407824 is a chemical BMP sensitizer and increases the sensitivity of cells to sub-threshold amounts of BMP4 .
Tramiprosate-d6 is the deuterium labeled Tramiprosate. Tramiprosate (Homotaurine), an orally active and brain-penetrant natural amino acid found in various species of red marine algae. Tramiprosate binds to soluble Aβ and maintains Aβ in a non-fibrillar form. Tramiprosate is also a GABA analog and possess neuroprotection, anticonvulsion and antihypertension effects[1][2][3].
Cytidine 5′-monophosphate- 15N3,d12 (5'-Cytidylic acid- 15N3,d12 dilithium; 5'-CMP- 15N3,d12) dilithium is deuterium and 15N labeled Cytidine 5'-monophosphate (HY-W009162). Cytidine 5'-monophosphate (5'-Cytidylic acid) is a nucleotide which is used as a monomer in RNA. Cytidine 5'-monophosphate consists of the nucleobase cytosine, the pentose sugar ribose, and the phosphate group.
Vanillin- 13C,d3 is the 13C and deuterium labeled Vanillin[1]. Vanillin (p-Vanillin) is a single molecule extracted from vanilla beans and also a popular odor used widely in perfume, food and medicine[2][3].
PSI-6206- 13C,d3 is the deuterium labeled PSI-6206. PSI-6206 is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase. PSI-6206 low potently inhibits HCV replicon with EC90 of >100 μM.
Mifepristone- 13C,d3 is the 13C- and deuterium labeled Mifepristone. Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay[1]. Mifepristone-13C,d3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Etoricoxib- 13C,d3 is the 13C- and deuterium labeled Etoricoxib. Etoricoxib (MK-0663) is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.
Simeprevir- 13C,d3 is the 13C- and deuterium labeled Simeprevir. Simeprevir is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir inhibits HCV replication with an EC50 of 7.8 nM. Simeprevir also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir inhibits the main protease (Mpro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses[1][2][5].
L-Serine- 15N,d3 is the deuterium and 15N-labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
3-Indoleacetic acid-2,2-d2 is the deuterium labeled 3-Indoleacetic acid (HY-18569). 3-Indoleacetic acid (Indole-3-acetic acid) is the most common natural plant growth hormone of the auxin class. It can be added to cell culture medium to induce plant cell elongation and division .
cis-Urocanic acid- 13C3 is the 13C-labeled cis-Urocanic acid. cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor[1].
Trametinib- 13C,d3 is the 13C- and deuterium labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis[1][2].
Lamotrigine- 13C,d3 is the 13C- and deuterium labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al[1][2].
SJ-3366 (IQP-0410) is a potent inhibitor of HIV nonnucleoside reverse transcriptase . SJ-3366 (IQP-0410) inhibits HIV at sub-nanomolar concentrations primarily through a typical non-nucleoside mechanism .
Anticancer agent 67 (Compound 13g) is an anti-cancer agent. Anticancer agent 67 induces apoptosis and increases sub-G1 cell population in MCF-7 cells. Anticancer agent 67 is a ciprofloxacin analog .
Anticancer agent 66 (Compound 13e) is an anti-cancer agent. Anticancer agent 66 induces apoptosis and increases sub-G1 cell population in MCF-7 cells. Anticancer agent 66 is a ciprofloxacin analog .
Clindamycin-d3 (hydrochloride) is the deuterium labeled Clindamycin. Clindamycin is an orally active and broad-spectrum bacteriostatic lincosamide antibiotic. Clindamycin can inhibit bacterial protein synthesis, possessing the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla). Clindamycin also can be used for researching malaria[1][2].
Clindamycin (Standard) is the analytical standard of Clindamycin. This product is intended for research and analytical applications. Clindamycin is an orally active and broad-spectrum bacteriostatic lincosamide antibiotic. Clindamycin can inhibit bacterial protein synthesis, possessing the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla). Clindamycin also can be used for researching malaria .
3α,21-Dihydroxy-5α-pregnan-20-one-d3 is the deuterium labeled 3α,21-Dihydroxy-5α-pregnan-20-one. 3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.
3-Amino-2-oxazolidinone-d4 is a deuterium labeled 3-Amino-2-oxazolidinone. 3-Amino-2-oxazolidinone (AOZ) is the metabolite of Furazolidone (HY-B1336). 3-Amino-2-oxazolidinone is always be detected as an indicator of furazolidone residues[1][2].
1-Methylguanosine-d3 is deuterium labeled 1-Methylguanosine (HY-113136). 1-Methylguanosine is a methylated nucleoside originating from RNA degradation. 1-Methylguanosine is a tumour marker.
Idasanutlin-d3-1(RG7388-d3-1) is the deuterium labeled Idasanutlin. Idasanutlin is a potent antagonist of MDM2/p53. Idasanutlin inhibits relapsed or refractory acute myeloid leukemia .
2,5-Dimethylpyrazine-d3 is deuterated labeled γ-Terpinene (HY-W020183). γ-Terpinene, a monoterpene, is an orally active antioxidant compound which can scavenge radicals directly. γ-Terpinene has potent antinociception activity .
Oxaceprol-d3(N-Acetyl-L-hydroxyproline-d3) is deuterium labeled Oxaceprol. Oxaceprol (N-Acetyl-L-hydroxyproline), an orally active derivative of L-proline, possesses distinct anti-inflammatory activity. Oxaceprol is usually used for the research of osteoarthritis and rheumatoid arthritis [3].
Rosuvastatin-d3 is a deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM[1]. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals[2].
Ceramide 3-d3 (N-Stearoyl phytosphingosine-d3) is deuterium labeled Ceramide 3. C18 Phytoceramide (t18:0/18:0) (Cer(t18:0/18:0)) is a bioactive sphingolipid found in the stratum corneum of Saccharomyces cerevisiae, wheat grain, and mammalian epidermis. Cer(t18:0/18:0) consists of a phytosphingosine backbone amine linked to a C18 fatty acid chain. Cer(t18:0/18:0) has the function of regulating apoptosis, cell differentiation, proliferation of smooth muscle cells and inhibition of mitochondrial respiratory chain. It also suppresses the expression of allergic cytokines IL-4, TNF-α, and transcription factors c-Jun and NF-κB in histone-stimulated mouse skin tissue. Formulations containing cer(t18:0/18:0) have been used as skin protectants in cosmetics as they reduce water loss and prevent epidermal dehydration and irritation .
Sorafenib-d3 (Donafenib) tosylate is the 13C- and deuterium labeled Sorafenib. Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator .
Tiotropium-d3 (bromide) is the deuterium labeled Tiotropium (Bromide). Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
1-Methylinosine-d3 is the deuterium labeled 1-Methylinosine. 1-Methylinosine is a modified nucleotide found at position 37 in tRNA 3' to the anticodon of eukaryotic tRNA[1].
Isovanillin-d3 is the deuterium labeled Isovanillin[1]. Isovanillin is an aldehyde oxidase inhibitor[2]. Antispasmodic activities[3]. Antidiarrheal activities[4].
2-Methylcitric acid-d3 is the deuterium labeled 2-Methylcitric acid. 2-Methylcitric acid (Methylcitric acid) is an endogenous metabolite in the 2-methylcitric acid cycle. 2-Methylcitric acid accumulates in methylmalonic and propionic acidemias and acts as a marker metabolite. 2-Methylcitric acid markedly inhibits ADP-stimulated and uncoupled respiration in mitochondria supported by glutamate[1].
Omeprazole-d3-1 is the deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
Spironolactone-d3-1 is deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC50 of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes[1][2][3].
Sorafenib-d3 (Donafenib), a deuterated compound of Sorafenib, is the first deuterium-generation tumor suppressor small molecule. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively .
16α-Hydroxyprednisolone-d3 is the deuterium labeled 16α-Hydroxyprednisolone. 16α-Hydroxyprednisolone is a stereoselective metabolite of the 22(R) epimer of the glucocorticoid budesonide via cytochrome P450 3A (CYP3A) enzymes[1][2].
Cyclobenzaprine-d3-1 hydrochloride (MK130-d3-1 hydrochloride) is the deuterium labeled Cyclobenzaprine hydrochloride (HY-B0740). Cyclobenzaprine (MK130) hydrochloride is an orally active 5-HT2 receptor antagonist. Cyclobenzaprine hydrochloride acts centrally, providing skeletal muscle relaxation, alleviating muscle spasms, and reducing pain. Additionally, Cyclobenzaprine hydrochloride has antiprotozoal activity. Additionally, Cyclobenzaprine hydrochloride also possesses antiparasitic activity. Cyclobenzaprine hydrochloride holds promise for research in the fields of acute, painful skeletal muscle disorders and infectious diseases [3]
2-Hydroxymethyl olanzapine-d3 (LY-290411-d3) is a deuterium labeled 2-Hydroxymethyl olanzapine. 2-Hydroxymethyl olanzapine is a metabolite of Olanzapine. .
3-Hydroxy Midostaurin-d5 is a deuterium labeled 3-Hydroxy Midostaurin. 3-Hydroxy Midostaurin is a metabolite of PKC412, which effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively[1].
Sulindac sulfide-d3 is deuterium labeled Sulindac sulfide. Sulindac sulfide is a noncompetitive γ-secretase inhibitor, with an IC50 of 20.2 μM for γ42-secretase activity.
Nemonoxacin-d3-1 is the deuterium labeled Nemonoxacin. Nemonoxacin (TG-873870) is an orally active and potent broad-spectrum antibiotic. Nemonoxacin shows good inhibitory activity against different species of staphylococci, streptococci, and enterococci, Neisseria gonorrhoeae, and Haemophilus influenza. Nemonoxacin can be used in the study of bacterial infections and community-acquired pneumonia[1][2][3].
Perindoprilat-d3 disodium is deuterated labeled Perindoprilat (HY-B1433). Perindoprilat (S 9780) is an angiotensin-converting enzyme (ACE) inhibitor with the IC50 value ranging from 1.5 to 3.2 nM. Perindoprilat can be used in hypertension research .
Voriconazole N-oxide-d3 (Voriconazole oxynitride-d3) is deuterium labeled Voriconazole N-oxide. Voriconazole N-oxide (Voriconazole oxynitride) is a potent antifungal agent. Voriconazole N-oxide has phototoxicity and photocarcinogenicity. Voriconazole N-oxide does not sensitize keratinocytes to ultraviolet B (UVB) .
Linagliptin-d3-1 (BI 1356-d3-1) is the deuterium labeled Linagliptin (HY-10284). Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM .
rac-Vofopitant-d3 (rac-GR 205171-d3) is the deuterium labeled Vofopitant (HY-12142) . Vofopitant is potent tachykinin NK1 receptor antagonist, with pKis of 10.6, 9.5, and 9.8 for human, rat and ferret NK1 receptor, respectively .
Alogliptin-d3 is the deuterium labeled Alogliptin. Alogliptin (SYR-322 free base) is a potent, selective and orally active inhibitor of DPP-4 with an IC50 of <10 nM, and exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9. Alogliptin can be used for the research of type 2 diabetes[1][2][3].
Melatonin-d3 is the deuterium labeled Melatonin. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties [3]. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation . Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress .
Skatole-d8 is the deuterium labeled Skatole. Skatole is produced by intestinal bacteria, regulates intestinal epithelial cellular functions through activating aryl hydrocarbon receptors and p38[1].
β-Alanine-d4 is the deuterium labeled β-Alanine. β-Alanine is a non-essential amino acid that is shown to be metabolized into carnosine, which functions as an intracellular buffer.
Kobusine derivative-2, a kobusine derivative, has antiproliferative activity against cancer cells. Kobusine derivative-2 can induce the arrest of MDA-MB-231 cells in the sub-G1 phase. Anticancer activity .
TP3011 (CH0793011) is an active metabolite of CH-0793076 and is a potent topoisomerase I inhibitor equipotent as SN38 . TP3011 is against cancer cell lines growth with IC50s at the range sub-nanomolar in vitro .
Tegaserod- 13C,d3 (maleate) is the 13C- and deuterium labeled Tegaserod (maleate). Tegaserod maleate is a selective 5-HT4 receptor partial agonist and a 5-HT2B receptor antagonist. Tegaserod maleate exhibits a promotile effect throughout the gastrointestinal (GI) tract[1][2][5].
Erythromycin ethylsuccinate- 13C,d3 is the 13C- and deuterium labeled Erythromycin Ethylsuccinate. Erythromycin Ethylsuccinate is an antibiotic useful for the treatment of a number of bacterial infections, has an antimicrobial spectrum similar to or slightly wider than that of penicillin. Erythromycin Ethylsuccinate has antiviral activity against HIV-1.
Phenylephrine-2,4,6-d3 (hydrochloride) is the deuterium labeled Phenylephrine hydrochloride. (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
Etoposide- 13C,d3 is the 13C- and deuterium labeled Etoposide. Etoposide (VP-16; VP-16-213) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy[1].
Cinnamic acid- 13C3 (3-Phenylacrylic acid- 13C3) is the 13C labeled Cinnamic acid (HY-N0610A). Cinnamic acid has potential use in cancer intervention, with IC50s of 1-4.5 mM in glioblastoma, melanoma, prostate and lung carcinoma cells .
3-Indoleacetic acid- 13C6 is the 13C labeled 3-Indoleacetic acid (HY-18569). 3-Indoleacetic acid (Indole-3-acetic acid) is the most common natural plant growth hormone of the auxin class. It can be added to cell culture medium to induce plant cell elongation and division .
Dabigatran- 13C,d3 is the 13C- and deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
Sofosbuvir- 13C,d3 is the deuterium labeled Sofosbuvir. Sofosbuvir (PSI-7977) is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.
Lumateperone- 13C,d3 (ITI-007- 13C,d3) tosylate is 13C and deuterium labeled Lumateperone (tosylate). Lumateperone (ITI-007) tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia [3] .
NPEC- caged-(S)-AMPA, a caged neurotransmitter analog, is a NPEC photoprotecting group caged the (S)-AMPA (HY-100815A) to make caged ligands specific for glutamate receptor sub-types. NPEC- caged-(S)-AMPA selectively activates AMPA receptor .
Clindamycin- 13C,d3 is the 13C- and deuterium labeled Clindamycin. Clindamycin is an orally active and broad-spectrum bacteriostatic lincosamide antibiotic. Clindamycin can inhibit bacterial protein synthesis, possessing the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla). Clindamycin also can be used for researching malaria[1][2][3].
Cytidine-5'-triphosphate- 15N3 (Cytidine triphosphate- 15N3 dilithium; 5'-CTP- 15N3) dilithium is 15N labeled Cytidine-5'-triphosphate (HY-125818). Cytidine 5′-triphosphate (Cytidine triphosphate; 5'-CTP) is a nucleoside triphosphate and serves as a building block for nucleotides and nucleic acids, lipid biosynthesis. Cytidine triphosphate synthase can catalyze the formation of cytidine 5′-triphosphate from uridine 5′-triphosphate (UTP). Cytidine 5′-triphosphate is an essential biomolecule?in the de novo?pyrimidine biosynthetic pathway in?T. gondii.
Deoxycytidine triphosphate- 15N3 (dCTP- 15N3 dilithium; 2′-Deoxycytidine-5′-triphosphate- 15N3) dilithium is 15N labeled Deoxycytidine triphosphate (HY-101400). Deoxycytidine triphosphate (dCTP) is a nucleoside triphosphate that can be used for DNA synthesis. Deoxycytidine triphosphate has many applications, such as real-time PCR, cDNA synthesis, and DNA sequencing.
Fluralaner- 13C2, 15N,d3 is the deuterium, 13C-, and 15-labeled Fluralaner. Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels.
3,4-Dehydro Cilostazol-d11 is deuterated labeled 3,4-Dehydro Cilostazol (HY-135910). 3,4-Dehydro Cilostazol (OPC-13015) is an active metabolite of Cilostazol (CLZ; HY-17464). 3,4-Dehydro Cilostazol is used for pharmacokinetic study .
1,3,5-Trimethoxybenzene-d3 (Trimethyl phloroglucinol-d3) is the deuterium labeled 1,3,5-Trimethoxybenzene (HY-Y0678). 1,3,5-Trimethoxybenzene is a key component of the Chinese rose odor. 1,3,5-Trimethoxybenzene is synthesized in three successive methylation steps from phloroglucinol, the initial precursor .
4-Acetamidobutanoic acid-d3 is the deuterated analog of 4-Acetamidobutanoic acid (HY-101411). 4-Acetamidobutanoic acid (N-acetyl GABA), the main metabolite of GABA, exhibits antioxidant and antibacterial activities .
N-Acetyl-L-methionine-d3 is the deuterium labeled N-Acetyl-L-methionine. N-Acetyl-L-methionine, a human metabolite, is nutritionally and metabolically equivalent to L-methionine. L-methionine is an indispensable amino acid required for normal growth and development[1].
6β-Naltrexol-d3(6β-Hydroxynaltrexone-d3) is deuterium labeled 6β-Naltrexol. 6β-Naltrexol (6β-Hydroxynaltrexone), the primary metabolite of Naltrexone, is a peripherally selective opioid antagonist. 6β-Naltrexol selectively inhibits gastrointestinal opioid effects in human subjects and inhibits Morphine-induced slowing of gastrointestinal transit .
3-O-Methyltolcapone-d7 is a deuterium labeled 3-O-Methyltolcapone. 3-O-Methyltolcapone is a metabolite of Tolcapone. Tolcapone is an orally active, reversible, selective and potent COMT inhibitor. Tolcapone crosses the blood-brain barrier, and can be used for treatment of Parkinson's disease[1][2].
2-Acetylfuran-d3 is deuterated labeled Citreoviridin (HY-N6745). Citreoviridin, a toxin from Penicillium citreoviride NRRL 2579, inhibits brain synaptosomal Na +/K +-ATPase whereas in microsomes, both Na +/K +-ATPase and Mg 2+-ATPase activities are significantly stimulated in a dose-dependent manner . Citreoviridin inhibits cell proliferation and enhances apoptosis of human umbilical vein endothelial cells .
Ceftriaxone-d3 (disodium) is the deuterium labeled Ceftriaxone. Ceftriaxone is a third-generation cephalosporin antibiotic with excellent activity against many gram-negative, and reasonable activity against most gram-positive microorganisms. Anti-inflammatory and antioxidant characteristics[1][2].
L-Alanine-d3 is the deuterium labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
Calcifediol-d3 is a deuterium labeled Calcifediol. Calcifediol, is an effective VDR ligand and VD supplement. Calcifediol is a prohormone of the vitamin D endocrine system (VDES) and is hydroxylated in the liver to produce the active form, calcitriol. Calcifediol can rapidly increase serum VD levels [3].
Glycerol- 13C3 is the 13C labeled Glycerol[1]. Glycerol is used in sample preparation and gel formation for polyacrylamide gel electrophoresis[2][3][4].
Salmeterol-d3 (xinafoate) is the deuterium labeled Salmeterol xinafoate. Salmeterol (GR 33343X) xinafoate is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively[1].
Ercalcidiol-d3 is the deuterium labeled Ercalcidiol. Ercalcidiol is a metabolite of Vitamins D2. Ercalcidiol can be used as an indicator of vitamins D status .
Estriol- 13C3 is the 13C-labeled Estriol. Estriol is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.
DL-Alanine-d3 is the deuterium labeled DL-Alanine. DL-alanine, an amino acid, is the racemic compound of L- and D-alanine. DL-alanine is employed both as a reducing and a capping agent, used with silver nitrate aqueous solutions for the production of nanoparticles. DL-alanine can be used for the research of transition metals chelation, such as Cu(II), Zn(II), Cd(11). DL-alanine, a sweetener, is classed together with glycine, and sodium saccharin. DL-alanine plays a key role in the glucose-alanine cycle between tissues and liver[1][2][3][4][5][6].
2-Sec-butyl-3-methoxypyrazine-d3 is deuterated labeled cis-?Jasmone (HY-N7058). Cis-Jasmone is a plant-derived natural product. Cis-Jasmone is constitutively released by many flowers and sometimes by leaves as an attractant for pollinators or as a chemical cue for host location by insect flower herbivores. Cis-Jasmone treatment of crop plants not only induces direct defense against herbivores, but also induces indirect defense by releasing VOCs that attract natural enemies .
p-Toluic acid-d3 is the deuterium labeled p-Toluic acid[1]. p-Toluic acid (4-Methylbenzoic acid) is a substituted benzoic acid and can be used as an intermediate for the synthesis of para-aminomethylbenzoic acid (PAMBA), p-tolunitrile, etc.
(±)-Taxifolin-13C3 ((±)-Dihydroquercetin-13C3) is a derivative of (±)-Taxifolin, labeled with 13C3. (±)-Taxifolin is the racemate of Taxifolin. Taxifolin exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM . Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity .
Calcitriol-d3 is the deuterium labeled Calcitriol[1]. Calcitriol is the most active metabolite of vitamin D and also a vitamin D receptor (VDR) agonist[2][3][4][5].
3-Methyl-2-quinoxalinecarboxylic acid-d4 is the deuterium labeled 3-Methyl-2-quinoxalinecarboxylic acid. 3-Methyl-2-quinoxalinecarboxylic acid (MQCA), an important N-oxide reductive metabolite of Quinocetone or Olaquindox, potently inhibits the growth of Chang liver cells through S phase arrest of the cell cycle[1].
1,3-Dimethoxybenzene-d3 (Resorcinol dimethyl ether-d3) is the deuterium labeled 1,3-Dimethoxybenzene (HY-34487). 1,3-Dimethoxybenzene belongs to the class of organic compounds known as dimethoxybenzenes. 1,3-Dimethoxybenzene is an intermediate in synthesis of organic compounds .
3-O-Methyltolcapone-d4 is the deuterium labeled 3-O-Methyltolcapone. 3-O-Methyltolcapone (Ro 40-7591) is a metabolite of Tolcapone. Tolcapone is an orally active, reversible, selective and potent COMT inhibitor. Tolcapone crosses the blood-brain barrier, and can be used for treatment of Parkinson's disease[1][2].
Histamine- 15N3 is the 15N3-labeled Histamine (HY-B1204). Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter .
(E)-Ferulic acid-d3 is the deuterium labeled (E)-Ferulic acid. (E)-Ferulic acid is a isomer of Ferulic acid which is an aromatic compound, abundant in plant cell walls. (E)-Ferulic acid causes the phosphorylation of β-catenin, resulting in proteasomal degradation of β-catenin and increases the expression of pro-apoptotic factor Bax and decreases the expression of pro-survival factor survivin. (E)-Ferulic acid shows a potent ability to remove reactive oxygen species (ROS) and inhibits lipid peroxidation. (E)-Ferulic acid exerts both anti-proliferation and anti-migration effects in the human lung cancer cell line H1299[1].
Moxifloxacin-d3-1 hydrochloride (BAY 12-8039-d3-1) is a deuterium labeled Moxifloxacin (HY-66011A). Moxifloxacin is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia [3].
Fmoc-Asp(OtBu)-OH-d3 (4-tert-Butyl N-(fluoren-9-ylmethoxycarbonyl)-L-aspartate-d3) is deuterium labeled Fmoc-Asp(OtBu)-OH. Fmoc-Asp(OtBu)-OH (4-tert-Butyl N-(fluoren-9-ylmethoxycarbonyl)-L-aspartate) is a aspartate derivative containing amine protecting group Fmoc. Fmoc-Asp(OtBu)-OH can be used for peptide synthesis .
Cytidine- 15N3 is the 15N labeled Cytidine[1]. Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catecholamine synthesis, and mitochondrial function[2][3][4].
Cytidine 5′-monophosphate- 15N3 (5'-Cytidylic acid- 15N3 dilithium; 5'-CMP- 15N3) dilithium is 15N labeled Cytidine 5'-monophosphate (HY-W009162). Cytidine 5'-monophosphate (5'-Cytidylic acid) is a nucleotide which is used as a monomer in RNA. Cytidine 5'-monophosphate consists of the nucleobase cytosine, the pentose sugar ribose, and the phosphate group.
NLRP3/aim2-in-2 (compound 8) is a new potent inhibitor with different species-specific effects on NLRP3 and AIM2 inflammasome dependent cell death. Its < b > IC < sub > 50 < / sub > < / b > value is 0.2392 μ M。
Deoxycytidine triphosphate- 13C9, 15N3 (dCTP- 13C9, 15N3 dilithium; 2′-Deoxycytidine-5′-triphosphate- 13C9, 15N3) dilithium is 13C and 15N-labeled Deoxycytidine triphosphate (HY-101400). Deoxycytidine triphosphate (dCTP) is a nucleoside triphosphate that can be used for DNA synthesis. Deoxycytidine triphosphate has many applications, such as real-time PCR, cDNA synthesis, and DNA sequencing.
Cytidine 5′-monophosphate- 13C9, 15N3 (5'-Cytidylic acid- 13C9, 15N3 dilithium; 5'-CMP- 13C9, 15N3) dilithium is 13C and 15N-labeled Cytidine 5'-monophosphate (HY-W009162). Cytidine 5'-monophosphate (5'-Cytidylic acid) is a nucleotide which is used as a monomer in RNA. Cytidine 5'-monophosphate consists of the nucleobase cytosine, the pentose sugar ribose, and the phosphate group.
Cytidine- 13C9, 15N3 is the 13C and 15N labeled Cytidine[1]. Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catecholamine synthesis, and mitochondrial function[2][3][4].
p-Tolylmaleimide (compound 9) is a naphthalimide derivative that has cytotoxic effects on cancer cells. p-Tolylmaleimide can arrest the cell cycle of human acute myeloid leukemia cells K562 in the sub-G0/G1 phase and induce apoptosis .
Sodium 2-oxopropanoate- 13C3 is the 13C-labeled Sodium 2-oxopropanoate. Sodium 2-oxopropanoate (Sodium pyruvate), a three-carbon metabolite of Glucose, is a compound produced in the glycolytic pathway. Sodium 2-oxopropanoate is a free radical scavenger that can scavenge ROS[1][2].
(E)-10-Hydroxynortriptyline-d3 is a deuterium labeled (E)-10-Hydroxy Nortriptyline. (E)-10-Hydroxy Nortriptyline is a metabolite of Nortriptyline. Nortriptyline is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and is used to relieve the symptoms of depression[1].
5-Methyl-1H-benzotriazole-d3(5-Methylbenzotriazole-d3) is the deuterium labeled 5-Methyl-1H-benzotriazole (HY-W086988). 5-Methyl-1H-benzotriazole is a biological material or organic compound that can be used in life science research .
3-Epiglycyrrhetinic acid-d2 (3α-Glycyrrhetic acid-d2) is the deuterium-labeled 3-Epiglycyrrhetinic acid. 3-Epiglycyrrhetinic acid is a derivative of glycyrrhetic acid. Glycyrrhetic acid and its derivative are considered to have anti-inflammatory, anti-ulcer, and antiviral activities .
Dantrolene- 13C3 is the 13C3 labeled Dantrolene. Dantrolene (F368), a muscle relaxant, non-competitively inhibits human erythrocyte glutathione reductase. Ki and IC50 values are 111.6 μM and 52.3 μM, respectively. Dantrolene is a ryanodine receptor antagonist and Ca2+ signaling stabilizer. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome.
Amiloride- 15N3 (hydrochloride) is the 15N labeled Amiloride hydrochloride[1]. Amiloride hydrochloride (MK-870 hydrochloride) is an inhibitor of both epithelial sodium channel (ENaC[2]) and urokinase-type plasminogen activator receptor (uTPA[3]). Amiloride hydrochloride is a blocker of polycystin-2 (PC2;TRPP2[4]) channel.
1-Bromo-3-methoxybenzene-d3 is the deuterium labeled 1-Bromo-3-methoxybenzene. Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Etbicyphat- 13C3 is the 13C labeled Etbicyphat (HY-139145). Etbicyphat is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors[1][2].
Varenicline-15N3 Hydrochloride (CP 526555-15N3 Hydrochloride) is the 15N labeled isotope of Varenicline hydrochloride (HY-10020). Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation [3] .
Favipiravir- 13C3 is the 13C labeled isotope of Favipiravir- 13C3(HY-14768 ).Favipiravir (T-705) is a potent viral RNA polymerase inhibitor, it is phosphoribosylated by cellular enzymes to its active form, Favipiravir-ribofuranosyl-5′-triphosphate (RTP). Favipiravir-RTP inhibits the influenza viral RNA-dependent RNA polymerase (RdRP) activity with an IC50 of 341 nM.
Trifluoperazine N-glucuronide-d3 is deuterium labeled Trifluoperazine N-Glucuronide. Trifluoperazine N-Glucuronide (UGT1A4), as one of the human UGT1A isoforms, is expressed in the liver. Trifluoperazine N-Glucuronide catalyzes the imipramine and trifluoperazine Nglucuronide formation[1].
Lactate-d3 sodium (60% in water) is the deuterium labeled Lactate sodium (60% in water). Lactate sodium (60% in water) is the product of glycogenolysis and glycolysis. Lactate sodium (60% in water) functions in a variety of biochemical processes .
Argifin is a sub-nanomolar chitinase inhibitor produced by soil microorganisms, with IC50s of 0.025 μM, 6.4 μM , 1.1 μM and 4.5 μM for SmChiA (Serratia marcescens chitinaese A), SmChiB, Aspergillus fumigatus chitinase B1 and human chitotriosidase, respectively .
MtTMPK-IN-8 (compound 27) is a moderate M. tuberculosis thymidylate kinase (MtbTMPK) inhibitor. MtTMPK-IN-8 has sub-micromolar activity against mycobacteria (MICs = 0.78~9.4 μM) without significant cytotoxicity. MtTMPK-IN-8 can be used for researching tuberculosis .
BK50164 is a potent CD73 inhibitor with an IC50 value of 13.089 µM. BK50164 binds to CD99 with a KD value of 1.5 µM. BK50164 shows antiproliferative activity. BK50164 induced Apoptosis and cell cycle arrest at Sub-G1 phase .
Histamine- 13C5, 15N3 (Ergamine- 13C5, 15N3) is the 13C and 15N labeled isotope of Histamine (HY-B1204). Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter .
Ceftriaxone- 13C2,d3 triethylammonium salt is 13C and deuterated labeled Ceftriaxone (HY-B0712). Ceftriaxone (Ro 13-9904 free acid) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone is a covalent inhibitor of GSK3β with IC50 value of 0.78 mM. Ceftriaxone is an inhibitor of Aurora B. Ceftriaxone has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone can be used in the study of bacterial infections and meningitis [3] .
Nicotinamide- 15N, 13C3 is the 13C-labeled and 15N-labeled Nicotinamide. Nicotinamide is a form of vitamin B3 that plays essential roles in cell physiology through facilitating NAD+ redox homeostasis and providing NAD+ as a substrate to a class of enzymes that catalyze non-redox reactions. Nicotinamide is an inhibitor of SIRT1.
Geranylgeraniol (Standard) is the analytical standard of Geranylgeraniol. This product is intended for research and analytical applications. Geranylgeraniol is an orally acitve vitamin K2 sub-type, an intermediate of the mevalonate pathway. Geranylgeraniol targets NF-kB signaling pathway and could alleviate LPS-induced microglial inflammation in animal model [3][4].
Aculene D, a fungal metabolite, shows quorum sensing (QS) inhibitory activity against Chromobacterium violaceum CV026, and could significantly reduce violacein production in N-hexanoyl-l-homoserine lactone (C6-HSL) induced C. violaceum CV026 cultures at sub-inhibitory concentrations .
N-Hexanoyl-L-Homoserine lactone-d3(C6-HSL-d3) is deuterium labeled N-Hexanoyl-L-homoserine lactone. N-Hexanoyl-L-homoserine lactone is a short-chained N-acyl homoserine lactone (AHL). Diatoms are frequently found in association with Proteobacteria, many members of which employ cell-to-cell communication via AHLs in aquatic habitats .
Ibuprofen- 13C,d3 is the 13C- and deuterium labeled Ibuprofen. Ibuprofen is an anti-inflammatory agent targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively .
Indole-3-carboxaldehyde- 13C (3-Formylindole- 13C) is a 13C labeled Indole-3-carboxaldehyde (HY-W007376). Indole-3-carboxaldehyde (3-Formylindole), a banlangen extract, is the product of the oxidative degradation of indole-3-acetic acid (IAA) by crude enzyme preparations from etiolated pea seedlings. Indole-3-carboxaldehyde (3-Formylindole) is a biochemical used to prepare analogs of the indole phytoalexin cyclobrassinin .
Acetyl-L-carnitine-d3 (hydrochloride) is the deuterium labeled Acetyl-L-carnitine hydrochloride. Acetyl-L-carnitine hydrochloride is a blood-brain permeable acetyl ester of the amino acid L-carnitine found in the body. Acetyl-L-carnitine hydrochloride is often used as a dietary supplement, and exibits anti-stress-related psychiatric disorders[1].
Myrcene- 13C3 is 13C labeled trans-2-Decenal (HY-W015551). trans-2-Decenal is an important raw material and intermediate used in organic synthesis, medicine, pesticides and dyes.
Ercalcitriol-d3 is the deuterium labeled Ercalcitriol. Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Pyruvic acid-13C is isotype-labeled compound of Pyruvic acid. Pyruvic acid is an intermediate metabolite in the metabolism of carbohydrates, proteins, and fats .
Guanidine- 13C, 15N3 (hydrochloride)is the 13C-labeled and 15N-labeled Guanidine hydrochloride. Guanidine hydrochloride (Guanidinium chloride) a strong chaotrope, is also a strong denaturant of proteins[1][2].
L-Serine- 13C3, 15N is the 13C- and 15N-labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
L-DOPA- 13C6 is the 13C-labled L-DOPA . L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease [3] .
Amentoflavone (Didemethyl-ginkgetin) is a potent and orally active GABA(A) negative modulator. Amentoflavone also shows anti-inflammatory, antioxidative, anti-viral, anti-tumor, anti-radiation, anti-fungal, antibacterial activity. Amentoflavone induces apoptosis and cell cycle arrest at sub-G1 phase [3] .
Antibacterial agent 182 (compound 8c) is an antibacterial agent that shows antibacterial activity against various Gram-positive bacteria, particularly against Vancomycin-resistant Enterococcus faecalis (MIC ≤0.125 μg/mL). Antibacterial agent 182 inhibits biofilm formation of Staphylococcus aureus and Pseudomonas aeruginosa at sub-MIC doses .
JNK-1-IN-5 (Compound 14) is a potent JNK1 inhibitor with sub-nanomolar efficacy. JNK-1-IN-5 suppresses TGF-β-induced epithelial-mesenchymal transition. JNK-1-IN-5 is promising for research of anti-pulmonary fibrosis agent targeting JNK1 .
L-Histidine- 13C6, 15N3,d5 (hydrochloride hydrate) is the deuterium, 13C-, and 15-labeled L-Histidine hydrochloride hydrate. L-Histidine hydrochloride hydrate (H-His-OH.HCl.H2O) is an endogenous metabolite.
Nur77 modulator 1 is a good Nur77 binder (KD = 3.58 μM). Nur77 modulator 1 up-regulates Nur77 expression, mediates sub-cellular localization of Nur77, induces Nur77-dependent ER stress and autophagy, and results in cell apoptosis. Anti-hepatoma activity .
MtTMPK-IN-7 (compound 26) is a moderate M. tuberculosis thymidylate kinase (MtbTMPK) inhibitor with an IC50 value of 47 μM. MtTMPK-IN-7 has sub-micromolar activity against mycobacteria (MICs = 2.3~4.7 μM) without significant cytotoxicity. MtTMPK-IN-7 can be used for researching tuberculosis .
MtTMPK-IN-9 (compound 28) is a moderate M. tuberculosis thymidylate kinase (MtbTMPK) inhibitor with an IC50 value of 48 μM. MtTMPK-IN-9 has sub-micromolar activity against mycobacteria (MICs = 6.25~9.4 μM) without significant cytotoxicity. MtTMPK-IN-9 can be used for researching tuberculosis .
Doravirine-13C,d3 (MK-1439-13C,d3) is the deuterium labeled Doravirine (HY-16767). Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181Creverse transcriptase mutants, respectively .
5-Methylcytidine 5′-triphosphate-d3 trisodium is the deuterium labeled 5-Methylcytidine 5’-triphosphate trisodium (HY-147338A). 5-Methylcytidine 5′-triphosphate (5-Methyl-CTP) trisodium is a modified nucleoside triphosphate. 5-Methylcytidine 5′-triphosphate trisodium can apply in replacing unmodified mRNA, resulting in the increase of translational properties and stability, as well as the reduction of innate immune responses in human and other mammalian cells .
Chlortetracycline-13C,d3 hydrochloride (7-Chlorotetracycline-13C,d3 hydrochloride) is the 13C- and deuterium labeled Chlortetracycline hydrochloride (HY-B1327). Chlortetracycline hydrochloride is an orally active, selective antibiotic, that inhibits methanogenic bacteria through inhibition of bacterial protein synthesis. Chlortetracycline hydrochloride is a specific and potent calcium ionophore antibiotic, that inhibits binding of aminoacyl-tRNA to ribosomes [3] .
Apalutamide- 13C,d3 is the 13C- and deuterium labeled Apalutamide. Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM[1].
Axitinib- 13C,d3 is a 13C-labeled and deuterium labeled Axitinib. Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50 values of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively .
Pazopanib- 13C,d3 (hydrochloride) is the deuterium and 13C labeled Pazopanib hydrochloride[1]. Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively[2][3].
Sulfasalazine-d3,15N is 15N and deuterated labeled Sulfasalazine (HY-14655). Sulfasalazine (NSC 667219) is an anti-rheumatic agent for the research of rheumatoid arthritis and ulcerative colitis. Sulfasalazine can suppress NF-κB activity. Sulfasalazine is a type 1 ferroptosis inducer [3] .
Istradefylline- 13C,d3 is the 13C- and deuterium labeled Istradefylline. Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.
Medetomidine-13C,d3 (hydrochloride) is a deuterated labeled Medetomidine (hydrochloride) . Medetomidine hydrochloride is an orally active α2-adrenoceptor agonist (Ki: 1.08 nM). Medetomidine hydrochloride has sedative and analgesic effects. Medetomidine hydrochloride can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels [3] .
Moxonidine- 13C,d3 hydrochloride is 13C and deuterated labeled Moxonidine hydrochloride (HY-B0374A). Moxonidine (BDF5895) hydrochloride is an imidazoline type 1 receptor (I1-R) selective agonist and antihypertensive agent.
Pazopanib- 13C,d3 is the deuterium and 13C labeled Pazopanib[1]. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively[2][3].
Elagolix- 13C,d3 (sodium) is the 13C- and deuterium labeled Elagolix sodium. Elagolix sodium is a human GnRH receptor (GnRHR) antagonist with an IC50 and Ki of 0.25 and 3.7 nM, respectively.
Linagliptin- 13C,d3 is the 13C- and deuterium labeled Linagliptin. Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM. Linagliptin-13C,d3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Cilastatin- 15N,d3 is a 15N-labeled and deuterium labeled Cilastatin. Cilastatin (MK0791) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin is an antibacterial adjunct[1][2][3].
Raltegravir- 13C,d3 potassium is 13C labeled Raltegravir potassium (HY-10353A). Raltegravir (MK 0518) potassium is a potent integrase (IN) inhibitor, used to treat HIV infection.
Pravastatin- 13C,d3 (sodium) is the 13C- and deuterium labeled Pravastatin (sodium). Pravastatin sodium (CS-514 sodium) is an HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM.
Omeprazole- 13C,d3 is a 13C-labeled and deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
Flurbiprofen- 13C,d3 is the 13C- and deuterium labeled Flurbiprofen. Flurbiprofen (dl-Flurbiprofen) is a potent, orally active nonsteroidal anti-inflammatory agent (NSAIA/NSAID), with antipyretic and analgesic activities. Flurbiprofen is commonly used for the research of inflammatory diseases, including osteoarthritis and rheumatoid arthritis. Flurbiprofen is a non-selective cyclooxygenase (COX) inhibitor that can be used for the research of colorectal cancer[1][2][3].
Fluvoxamine- 13C, d3 maleate is 13C and deuterated labeled Fluvoxamine maleate (HY-B0103A). Fluvoxamine maleate (DU-23000 maleate) is an antidepressant which functions pharmacologically as a selective serotonin reuptake inhibitor.
Taltirelin- 13C,d3 (TA-0910- 13C,d3) is 13C and deuterated labeled Taltirelin (HY-B0596). Taltirelin (TA0910) is a superagonist at thyrotropin-releasing hormone receptor (TRH-R) with an IC50 of 910 nM and EC50 of 36 nM for stimulating an increase in cytosolic Ca 2+ concentration (Ca 2+ release).
Encorafenib- 13C,d3 is the 13C- and deuterium labeled Encorafenib. Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).
Velpatasvir- 13C,d3 (GS-5816- 13C,d3) is 13C and deuterium labeled Velpatasvir. Velpatasvir (VEL, GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons. Velpatasvir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 2.16 μM [3].
Zafirlukast- 13C,d3 is the 13C- and deuterium labeled Zafirlukast. Zafirlukast (ICI 204219) is a potent orally active leukotriene D4 (LTD4) receptor antagonist. Zafirlukast shows anti-asthmatic, anti-inflammatory and anti-bacterial effects.
L-Histidine- 15N3 (hydrochloride hydrate) is the 15N-labeled L-Histidine hydrochloride hydrate. L-Histidine hydrochloride hydrate (H-His-OH.HCl.H2O) is an endogenous metabolite.
Almorexant- 13C,d3 is the 13C- and deuterium labeled Almorexant. Almorexant (ACT 078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM, respectively.
Trelagliptin-13C,d3 is a deuterated labeled Trelagliptin . Trelagliptin (SYR-472) is a potent, orally active and highly selective DPP-4 inhibitor with an IC50 of 4 nM. Trelagliptin succinate improves glycemic control in vivo and can be used for the study of type 2 diabetes mellitus (T2DM) .
Trimegestone- 13C,d3 is 13C and deuterated labeled Trimegestone (HY-106827). Trimegestone (RU 27987) is an orally active 19-norpregnane progestin. Trimegestone binds to progesterone receptor (PR) with an IC50 value of 3.3 nM (rat PR). Trimegestone increases alkaline phosphatase activity (EC50=0.1 nM) but not luciferase activity. Trimegestone also shows a weak antiandrogenic activity (weak androgen receptor affinity). Trimegestone can be used in studies of contraception or menopausal syndromes .
Butenafine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled. Butenafine Hydrochloride (KP363 Hydrochloride) is a synthetic benzylamine antifungal, works by inhibiting the synthesis of sterols by inhibiting squalene epoxidase.
Nintedanib- 13C,d3 is the 13C- and deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
Rabeprazole-13C,d3 is a deuterated labeled Rabeprazole . Rabeprazole (LY307640) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H +/K +-ATPase. Rabeprazole induces apoptosis. Rabeprazole acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole can be used for the research of gastric ulcerations and gastroesophageal reflux [3] .
2,3-Diphosphoglyceric acid-d3 ammonium (2,3-DPG-d3 ammonium) is the deuterium labeled 2,3-Diphosphoglyceric acid (HY-113050). 2,3-Diphosphoglyceric acid (2,3-DPG) is an intermediate of the glycolytic pathway. 2,3-Diphosphoglyceric acid stabilizes the deoxygenated form of hemoglobin by allosteric binding and facilitates oxygen release at tissue sites. 2, 3-diphosphoglyceric acid has antiparasitic activity. 2,3-Diphosphoglyceric acid can be used in the study of Alzheimer's disease (AD) [3] .
Ketoprofen- 13C,d3 is the 13C- and deuterium labeled Ketoprofen. Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC50s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively[1].
Telmisartan- 13C,d3 is the 13C- and deuterium labeled Telmisartan. Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
Hydrocinnamic acid-2,3- 13C2 is the 13C-labeled Hydrocinnamic acid. Hydrocinnamic acid is the major rhizospheric compound with known growth regulatory activities.
L-Histidine- 13C6, 15N3 (hydrochloride hydrate) is the 13C- and 15N-labeled L-Histidine hydrochloride hydrate. L-Histidine hydrochloride hydrate (H-His-OH.HCl.H2O) is an endogenous metabolite.
β-Alanine- 13C3, 15N is the 13C- and 15N-labeled β-Alanine. β-Alanine is a non-essential amino acid that is shown to be metabolized into carnosine, which functions as an intracellular buffer.
1,2-Cyclohexylenedinitrilotetraacetic acid (Standard) is the analytical standard of 1,2-Cyclohexylenedinitrilotetraacetic acid. This product is intended for research and analytical applications. 1,2-Cyclohexylenedinitrilotetraacetic acid (CDTA) is a chelating agent. 1,2-Cyclohexylenedinitrilotetraacetic acid has an ability to remove manganese from brain and liver (in vivo) and their sub-cellular fractions (in vitro), of rats pretreated with manganese sulphate .
NNC 05-2090 hydrochloride is a GABA uptake inhibitor and inhibitor of the β-GABA transporter (BGT-1) (IC50< /sub>: 10.6 μM). NNC 05-2090 hydrochloride also inhibits mGAT2 with a Ki value of 1.4 μM. NNC 05-2090 has anticonvulsant activity and can be used in the study of epilepsy and neurological diseases [3].
NNC 05-2090 is aGABA uptake inhibitor and inhibitor of the β-GABA transporter (BGT-1) (IC50sub>: 10.6 μM). NNC 05-2090 also inhibits mGAT2 with a Ki value of 1.4 μM. NNC 05-2090 has anticonvulsant activity and can be used in the study of epilepsy and neurological diseases [3].
Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL.
KHK-IN-1 (compound 8) is a selective and cell membrane permeable ketohexokinase (KHK) inhibitor (IC50=12 nM; F=34%). KHK-IN-1 inhibits the production of F1P in HepG2 cell lysates (IC>sub>50=400 nM). KHK-IN-1 has potential for the study of diabetes and obesity .
KHK-IN-1 hydrochloride (compound 8) is a selective and cell membrane permeable ketohexokinase (KHK) inhibitor (IC50=12 nM; F=34%). KHK-IN-1 hydrochloride inhibits the production of F1P in HepG2 cell lysates (IC>sub>50=400 nM). KHK-IN-1 hydrochloride has potential for the study of diabetes and obesity .
Sorafenib- 13C,d3 is the 13C- and deuterium labeled Sorafenib. Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator[1].
Regorafenib- 13C,d3 is the 13C- and deuterium labeled Regorafenib. Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.
Triclabendazole sulfoxide- 13C,d3 is the 13C- and deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP[1][2].
Apixaban- 13C,d3 is a deuterium and 13C labeled Apixaban. Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively[1].
(Rac)-Fosfomycin (benzylamine)- 13C3 is the 13C labeled Fosfomycin[1]. Fosfomycin (MK-0955) is a broad-spectrum antibiotic. Fosfomycin can cross blood-brain barrier penetrating, and irreversibly inhibits an early stage in cell wall synthesis. Fosfomycin shows anti-bacteria activity for a range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria[2][3].
L-Alanine- 13C3 is the 13C-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
Caffeic acid- 13C3 is an 13C labeled caffeic acid. Caffeic acid is a phytonutrient belonging to the flavonoids. Caffeic acid and its derivatives, are potential antimicrobial agents, chronic infection induced by microbes such as bacteria, fungi, and viruses[1].
Acetyl-L-carnitine-d3-1 (hydrochloride) is the deuterium labeled Acetyl-L-carnitine hydrochloride. Acetyl-L-carnitine hydrochloride is a blood-brain permeable acetyl ester of the amino acid L-carnitine found in the body. Acetyl-L-carnitine hydrochloride is often used as a dietary supplement, and exibits anti-stress-related psychiatric disorders[1].
Moxifloxacin- 13C,d3 hydrochloride (BAY 12-8039- 13C,d3) is 13C and deuterated labeled Moxifloxacin (HY-66011A). Moxifloxacin is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia.
O-Phospho-L-serine- 13C3, 15N is the 13C- and 15N-labeled O-Phospho-L-serine. O-Phospho-L-serine is the immediate precursor to L-serine in the serine synthesis pathway, and an agonist at the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8); O-Phospho-L-serine also acts as a weak antagonist for mGluR1 and a potent antagonist for mGluR2[1].
Pelargonidin chloride is an anthocyanidin and also is a scavenger of nitric oxide radical and has antioxidant activities. Pelargonidin inhibits cell viability and induces cell cycle arrest at sub-G1 phase. Pelargonidin chloride increases the mRNA and protein expression of HO-1, NQO1, Nrf2. Pelargonidin chloride improves Aβ-induced memory and learning impairment [3].
Cantharidic acid is a selective inhibitor for protein phosphatase 2 (PP2A) and protein phosphatase 1 (PP1). Cantharidic acid inhibits cell viability and arrest cell cycle at sub G1 phase, induces apoptosis in cells NPC-39 and HONE-1 through the upregulation of ERK1/2, p38, and JNK1/2 pathway .
Stewart-Grubbs catalyst is an effective catalyst for the cross-metathesis of olefins with a large number of allylic substituents. In addition, ChemBeads are chemically coated glass beads that improve flowability and chemical homogeneity, making them ideal for automated solid dispensing and high-throughput experiments. Notably, the manufacture of ChemBeads does not require additional chemicals or surfactants, allowing for precise dispensing of sub-milligram amounts of catalyst.
Ganitumab (AMG 479) is a recombinant human monoclonal antibody to the human type 1 insulin-like growth factor receptor (IGF1R). Ganitumab recognizes murine IGF1R with sub-nanomolar affinity (KD=0.22 nM) and inhibits the interaction of murine IGF1R with IGF1 and IGF2. Ganitumab can be used in research of cancer .
TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1 .
Dehydro Nifedipine-13C,d3 is a deuterated labeled Dehydro Nifedipine . Dehydro nifedipine (BAY-b 4759) is a metabolite of Nifedipine (HY-B0284). Nifedipine (BAY-a-1040) is a potent calcium channel blocker and an agent of choice for cardiac insufficiencies .
Levomefolic acid- 13C,d3 is the deuterium labeled Levomefolic acid (HY-14781) . Levomefolic acid (5-MTHF) is an orally active, brain-penetrant natural active form of folic acid and is one of the most widely used folic acid food supplements [3].
Epinastine- 13C,d3 (hydrobromide) is the 13C- and deuterium labeled Epinastine. Epinastine (WAL801) is an antihistamine and mast cell stabilizer. Epinastine is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine also inhibits IL-8 release and has an antiallergic action[1][2][3][4].
Tubulin polymerization-IN-65 is a tubulin polymerisation inhibitor with a broad spectrum cytotoxic. Tubulin polymerization-IN-65 induces G2 + M cell cycle arrest .
13C20, 15N10-Cyclic di-GMP ( 13C20, 15N10-c-di-GMP) is 13C and 15N labeled Cyclic-di-GMP (disodium). Cyclic-di-GMP disodium is a STING agonist and a bacterial second messenger that coordinates different aspects of bacterial growth and behavior, including motility, virulence, biofilm formation, and cell cycle progression. Cyclic-di-GMP disodium has anti-cancer cell proliferation activity and also induces elevated CD4 receptor expression and cell cycle arrest. Cyclic-di-GMP disodium can be used in cancer research [3] .
Duocarmycin A, which is one of well-known antitumor antibiotics, is a DNA alkylator and efficiently alkylates adenine N3 at the 3′ end of AT-rich sequences in the DNA. Duocarmycin A, as a chemotherapeutic agent, results HLC-2 cells typically apoptotic changes, including chromatin condensation, sub-G1 accumulation in DNA histogram pattern, and decrease in procaspase-3 and 9 levels .
L-Alanine- 13C3, 15N,d4 is the deuterium, 13C-, and 15-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
Paroxetine EP impurity D-d4 (hydrochloride) is deuterium labeled (3R,4S)-3-((benzo[d][1,3]dioxol-5-yloxy)methyl)-4-(4-fluorophenyl)piperidine?(Paroxetine Impurity).
Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50=650 nM). Thailanstatin A exerts effects via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome and shows low-nM to sub-nM IC50s against multiple cancer cell lines. Thailanstatin A, a payload for ADCs, is conjugated to the lysines on trastuzumab yielding “linker-less” ADC [3].
PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator. PZ-2891 act as an orthosteric inhibitor at high concentrations and an allosteric activator at lower sub-saturating concentrations. PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC50s of 40.2 nM, 0.7 nM and 1.3 nM, respectively .
Amentoflavone (Standard) is the analytical standard of Amentoflavone. This product is intended for research and analytical applications. Amentoflavone (Didemethyl-ginkgetin) is a potent and orally active GABA(A) negative modulator. Amentoflavone also shows anti-inflammatory, antioxidative, anti-viral, anti-tumor, anti-radiation, anti-fungal, antibacterial activity. Amentoflavone induces apoptosis and cell cycle arrest at sub-G1 phase [3] .
(3S,5R)-Fluvastatin-d6 (sodium) is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway[1].
Antitumor agent-159 (Compound 13b) targets the mitochondria and downregulates cardiolipin levels. Antitumor agent-159 inhibits the proliferation of cancer cell MDA-MB-231, arrests the cell cycle at sub-G1 phase, and induces apoptosis in MDA-MB-231. Antitumor agent-159 exhibits antitumor efficacy in MDA-MB-231 xenograft mouse models .
3,3'-Diiodo-L-thyronine- 13C6 is the 13C labeled 3,3'-Diiodo-L-thyronine[1]. 3,3'-Diiodo-L-thyronine (3,3'-T2) is an endogenous metabolite of thyroid hormone. 3,3'-Diiodo-L-thyronine significantly enhances COX activity[2][3].
Zidovudine O-β-D-glucuronide-d3 (sodium) (3'-Azido-3'-deoxythymidine β-D-glucuronide-d3 (sodium)) is a deuterium labeled Zidovudine O-β-D-glucuronide (sodium) (HY-137522). Zidovudine O-β-D-glucuronide (3'-Azido-3'-deoxythymidine β-D-glucuronide) sodium is the major metabolite of Zidovudine. Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection [3].
Felbamate-d5 is the deuterium labeled Felbamate[1]. Felbamate (W-554) is a potent nonsedative anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA)[2][3].
Oxypurinol- 13C, 15N2 is 15N and 13C labeled Oxypurinol (HY-19657). Oxipurinol (Oxipurinol), the major active metabolite of Allopurinol, is an inhibitor of xanthine oxidase. Oxipurinol can be used to regulate blood urate levels and treat gout .
Zidovudine-d4 is deuterated labeled Zidovudine (HY-17413). Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection.
MeOIstPyrd is an anti-skin cancer agent. MeOIstPyrd inhibits cell proliferation, migration, and spheroid formation by activating the mitochondrial intrinsic apoptotic pathway. MeOIstPyrd induces DNA damage. MeOIstPyrd activates p53, and increases the half-life of p53 and stabilizes p53 by phosphorylating it at ser15. MeOIstPyrd binds to MDM2 in the p53 sub-pocket and blocks p53-MDM2 interaction .
Pretomanid-d4 is the deuterium labeled Pretomanid. Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL[1][2].
Pretomanid (Standard) is the analytical standard of Pretomanid. This product is intended for research and analytical applications. Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL.
Tolterodine-d14 (hydrochloride) is the deuterium labeled Tolterodine hydrochloride[1]. Tolterodine hydrochloride is a potent muscarinic receptor antagonist[2][3].
Pentoxifylline-d5 is the deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation[1][2][3].
Pirenzepine-d8 (LS 519-d8; Pirenzepin-d8) dihydrochloride is a deuterium labeled Pirenzepine (dihydrochloride) (HY-17037). Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells [3].
N-Desmethylclozapine-d8 is the deuterium labeled N-Desmethylclozapine. N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist[1][2].
N-Desmethylclozapine-d8 (hydrochloride) is the deuterium labeled N-Desmethylclozapine hydrochloride. N-Desmethylclozapine hydrochloride is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine hydrochloride is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine hydrochloride is also a δ-opioid agonist[1][2][3].
Dulcite-d2 is the deuterium labeled Dulcite. Dulcite is a sugar alcohol with a slightly sweet taste which is a metabolic breakdown product of galact[1][2].
Pentoxifylline-d6 is the deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation[1][2][3].
Camptothecin-d5 is the deuterium labeled Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM[1]. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells[2][3].
Demethoxycurcumin-d4 is the deuterium labeled Demethoxycurcumin. Demethoxycurcumin (Curcumin II) is a major active curcuminoid; possess anti-inflammatory properties[1].
Tetradecyltrimethylammonium-d29 (bromide) is the deuterium labeled Tetradecyltrimethylammonium (bromide)[1]. Tetradecyltrimethylammonium bromide, an organic building block, is a cationic surfactant with asymmetrical structure[2][3].
Tetradecyltrimethylammonium-d38 (bromide) is the deuterium labeled Tetradecyltrimethylammonium (bromide)[1]. Tetradecyltrimethylammonium bromide, an organic building block, is a cationic surfactant with asymmetrical structure[2][3].
Moricizine-d8 (Hydrochloride) is the deuterium labeled Moricizine Hydrochloride (HY-B0615A). Moricizine Hydrochloride is an orally active Class I antiarrhythmic agent. Moricizine Hydrochloride decreases the maximum rate of phase 0 depolarization; increases rates of phase 2 and 3 repolarization, decreases action potential duration, and decreases effective refractory period[1][2].
Demethoxycurcumin-d7 is the deuterium labeled Demethoxycurcumin. Demethoxycurcumin(Curcumin II), a major active curcuminoid, possess anti-inflammatory properties; also exert cytotoxic effects in human cancer cells via induction of apoptosis.
Picropodophyllin-d6 (AXL1717-d6) is deuterium labeled Picropodophyllin. Picropodophyllin (AXL1717) is a selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 of 1 nM.
L-Lactic acid- 13C3 ((S)-2-hydroxypropanoic- 13C3) sodium (20% in water) is the 13C labeled L-Lactic acid. L-Lactic acid- 13C3 sodium (20% in water) can be used for lactate metabolism research .
ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis .
CTL-06 is an inhibitor of Fatty Acid Synthase (FASN) (IC50: 3 μM) and can induce apoptosis. CTL-12 blocks the cell cycle in the Sub-G1/S phase, upregulates the expression of caspase-9 and the apoptosis marker Bax, and downregulates the anti-apoptotic marker Bcl-xL. CTL-12 inhibits de novo lipogenesis, blocks the metabolic demands of tumor cells, and is commonly used in breast and colorectal cancer research .
hCAIX-IN-16 (Compound 12d) is hCA IX inhibitor, with Ki values of 190.0 and 187.9 nM for hCA IX and hCA XII, respectively. hCAIX-IN-16 can arrest the cell cycle of breast cancer MDA-MB-468 in G0-G1 and S phase and induce apoptosis. hCAIX-IN-16 shows good broad-spectrum anticancer activity and can be used for cancer research .
Tiagabine-d5 (hydrochloride) is deuterium labeled Tiagabine (hydrochloride). Tiagabine hydrochloride is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [ 3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively .
Acetaminophen-d7 is the deuterium labeled Acetaminophen. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.
Alpha-Estradiol-d2 is the deuterium labeled Alpha-Estradiol. Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia[1].
D-Glucose-d4 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molec
Isoniazid-d4 is the deuterium labeled Isoniazid. Isoniazid (INH) is a proagent and must be activated by a bacterial catalase-peroxidase enzyme KatG. Isoniazid is bactericidal to rapidly dividing mycobacteria and has anti-tuberculostatic activity[1][2][3][4].
D-Glucose-d22 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
Squalene-d6 is a deuterium labeled Squalene. Squalene (Super Squalene) is an intermediate product in the synthesis of cholesterol, and shows several pharmacological properties such as hypolipidemic, hepatoprotective, antiatherosclerotic, cardioprotective, antioxidant, and antitumour activity .
Irinotecan-d10 is a deuterium labeled Irinotecan ((+)-Irinotecan). Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex[1].
Tucidinostat-d4 is the deuterium labeled Tucidinostat. Tucidinostat is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, respectively[1].
D-Glucose-d77 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
Acetaminophen-d4 is the deuterium labeled Acetaminophen. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent[1][2][3]. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor[4].
D-Glucose-d is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molec
Indocyanine green-d7 (Foxgreen-d7) is the deuterium labeled Indocyanine green (HY-D0711). Indocyanine green is a low toxicic fluorescent agent that has been widely used in medical diagnostics, such as determining cardiac output, hepatic function, and liver blood flow, and for ophthalmic angiography .
Tauroursodeoxycholate-d4 (sodium) is the deuterium labeled Tauroursodeoxycholate sodium. Tauroursodeoxycholate (Tauroursodeoxycholic acid; TUDCA) sodium is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
Vitamin D2-d6 is the deuterium labeled Vitamin D2. Vitamin D2 (Ergocalciferol), drived from plant sources or dietary supplements, could be used as supplement of Vitamin D[1][2].
Enclomiphene-d4 (hydrochloride) is a deuterium labeled Enclomiphene. Enclomiphene-d4 (hydrochloride) is a potent and orally active oestrogen receptor antagonist, with antioestrogenic property[1].
Sudan IV-d6 is the deuterium labeled Sudan IV(HY-D0932).Sudan IV is a lysochrome (fat-soluble dye) diazo dye used for the staining of lipids, triglycerides and lipoproteins on frozen paraffin sections .
Irinotecan-d5 hydrochloride is deuterated labeled Irinotecan hydrochloride (HY-16562A). Irinotecan hydrochloride ((+)-Irinotecan hydrochloride) is a topoisomerase I inhibitor mainly used to treat colon cancer and rectal cancer .
Tucatinib-d6 (Irbinitinib-d6) is deuterium labeled Tucatinib. Tucatinib (Irbinitinib) is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM .
Tauroursodeoxycholate-d4 is deuterium labeled Tauroursodeoxycholate. Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
Tiagabine-d4 hydrochloride is deuterated labeled Tiagabine hydrochloride (HY-B0696A). Tiagabine hydrochloride is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [ 3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively .
Umbelliferone-d5 is the deuterium labeled Umbelliferone. Umbelliferone (7-Hydroxycoumarin), a natural product of the coumarin family, is a fluorescing compound which can be used as a sunscreen agent.
Zoledronic acid-d5 is deuterated labeled Zoledronic Acid (HY-13777). Zoledronic Acid (Zoledronate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic Acid inhibits the differentiation and apoptosis of osteoclasts. Zoledronic Acid also has anti-cancer effects .
Cyclosporin A- 13C2,d4 (Cyclosporine A- 13C2,d4; Ciclosporin A- 13C2,d4) is a 13C labeled Cyclosporin A (HY-B0579) . Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM . Cyclosporin A also inhibits CD11a/CD18 adhesion [3].
D-Glucose- 13C2,d2 is the deuterium and 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical si
1,2-Dihydropyridazine-3,6-dione-3,4,5,6- 13C4 (1,2-Dihydro-3,6-pyridazine- 13C4-dione) is 13C labeled Maleic hydrazide. Maleic hydrazide is extensively used as a systemic plant growth regulator and as a herbicide. Maleic hydrazide acts as an inhibitor of the synthesis of nucleic acids and proteins .
5-Aminosalicylic acid-d7 (5-ASA-d7; Mesalamie-d7; Mesalazie-d7) is deuterium labeled 5-Aminosalicylic Acid. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB. 5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN) .
Dimethoxycurcumin-d6 is the deuterium labeled Dimethoxycurcumin (HY-100977). Dimethoxycurcumin is a derivative of Curcumin that has anti-inflammatory and antioxidant activities .
N,N-Dimethylglycine-d6 (Dimethylglycine-d6) hydrochloride is the deuterium labeled N,N-Dimethylglycine hydrochloride (HY-W001158). N,N-Dimethylglycine (Dimethylglycine) is a natural N-methylated glycine, is a nutrient supplement and acts as an NMDAR glycine site partial agonist. N,N-Dimethylglycine is a methyl donor, could improve immunity, function as an antioxidant to prevent oxidative stress, and scavenge excess of free radicals. N,N-Dimethylglycine exhibits antidepressant-like and surfactant effects [3] .
Cortodoxone-d2 is the deuterium labeled Cortodoxone. Cortodoxone is a glucocorticoid steroid hormone that can be oxygenated to cortisol (Hydrocortisone)[1].
Cetrimonium-d9 (bromide) is the deuterium labeled Cetrimonium bromide[1]. Cetrimonium bromide (CTAB) is an amine based cationic quaternary surfactant, is one of the components of the topical antiseptic Cetrimide.
Erlotinib-d6 (CP-358774 D6) is a deuterium labeled Erlotinib (CP-358774). Erlotinib is a directly acting inhibitor EGFR tyrosine kinase inhibitor with an IC50 of 2 nM for human EGFR[1]. Erlotinib-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Urethane-d5 is the deuterium labeled Urethane. Urethane (Ethyl carbamate), the ethyl ester of carbamic acid, is a byproduct of fermentation found in various food products. Urethane has the ability to suppress bacterial, protozoal, sea urchin egg, and plant tissue growth in vitro[1].
Alectinib-d6 is deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
Elvitegravir-d8 is deuterium labeled Elvitegravir. Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
Cetrimonium-d33 (bromide) is the deuterium labeled Cetrimonium bromide[1]. Cetrimonium bromide (CTAB) is an amine based cationic quaternary surfactant, is one of the components of the topical antiseptic Cetrimide.
Phosphorylethanolamine-d4 (Monoaminoethyl phosphate-d4; NSC 254167-d4) is a deuterium labeled Phosphorylethanolamine (HY-N5034). Phosphorylethanolamine is an endogenous metabolite.
Elvitegravir-d6 (GS-9137-d6) is deuterium labeled Elvitegravir. Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively .
Vemurafenib-d7 is deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively[1][4]. Vemurafenib induces cell autophagy[5].
Telbivudine-d4 is deuterium labeled Telbivudine. Telbivudine (Epavudine), an orally active thymidine nucleoside analog, is a potent antiviral inhibitor of hepatitis B virus (HBV) replication[1].
Erlotinib-d6 (hydrochloride) a deuterium labeled Erlotinib Hydrochloride. Erlotinib Hydrochloride inhibits purified EGFR kinase with an IC50 of 2 nM[1]. Erlotinib-d6 (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Oleoylethanolamide-d2 is the deuterium labeled Oleoylethanolamide. Oleoylethanolamide is a high affinity endogenous PPAR-α agonist, which plays an important role in the treatment of obesity and arteriosclerosis.
Pirenzepine-d8 is the deuterium labeled Pirenzepine dihydrochloride. Pirenzepine dihydrochloride (LS519) is a selective M1 muscarinic receptor antagonist.
Cyclosporin A-d4 is the deuterium labeled Cyclosporin A. Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of calcineurin with an IC50 of 5 nM. Cyclosporin A also inhibits CD11a/CD18 ad
Bortezomib-d8 is the deuterium labeled Bortezomib. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity[1][2].
Miglustat-d9 is the deuterium labeled Miglustat. Miglustat (N-Butyldeoxynojirimycin) is an inhibitor of glucosylceramide synthase, primarily to treat Type I Gaucher disease (GD1) .
Oleoylethanolamide-d4 is the deuterium labeled Oleoylethanolamide. Oleoylethanolamide is a high affinity endogenous PPAR-α agonist, which plays an important role in the treatment of obesity and arteriosclerosis.
Venetoclax-d8 is deuterium labeled Venetoclax. Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy[1][2][3].
Delafloxacin-d5 is deuterium labeled Delafloxacin. Delafloxacin (RX-3341; WQ-3034; ABT492) is a broad-spectrum fluoroquinolone antibiotic. Delafloxacin has a broad spectrum of activity that includes drug-resistant Staphylococcus aureus, Streptococcus pneumoniae, and Klebsiella pneumonia[1].
Sonidegib-d4 is a isotope of Sonidegib. Sonidegib is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively .
Avatrombopag-d8 (hydrochloride) is deuterium labeled Avatrombopag (hydrochloride). Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A[1][2][3].
Curcumin-d6is a deuterium labeled Curcumin (Turmeric yellow). Curcumin (Turmeric yellow) is a natural phenolic compound with diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin is an inhibitor of p300 histone acetylatransferase (HATs) and also shows inhibitory effects on NF-κB and MAPKs.
Miglustat-d9 (hydrochloride) is the deuterium labeled Miglustat (hydrochloride). Miglustat hydrochloride is an inhibitor of glucosylceramide synthase, primarily to treat Type I Gaucher disease (GD1)[1][2].
Alectinib-d8 is the deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
Melanotan I is a potent non-selective melanocortin receptor (MCR) agonist. Melanotan I is a synthetic analogue of α-melanocyte stimulating hormone (α-MSH) that stimulates melanogenesis. Melanotan I can induce skin tanning by mimicking the actions of a-MSH on the melanocortin type 1 receptors (MC1R) of melanocytes. Melanotan I can be used for the research of sun-induced skin cancer, melanoma, inflammation and male erectile dysfunction [3] .
Cephalexin-d5 is deuterium labeled Cephalexin. Cephalexin (Cefalexin; Cephacillin) is a potent, orally active and the first-generation cephalosporin antibiotic. Cephalexin kills gram-positive and some gram-negative bacteria by disrupting the growth of the bacterial cell wall. Cephalexin monohydrate is used for the research of pneumonia, strep throat, and bacterial endocarditis, et al[1].
Ligustrazine-d12 (Chuanxiongzine-d12) is deuterium labeled Ligustrazine. Ligustrazine (Chuanxiongzine), an alkylpyrazine isolated from Ligusticum chuanxiong Hort. (Chuan Xiong) , is present in french fries, bread, cooked meats, tea, cocoa, coffee, beer, spirits, peanuts, filberts, dairy products and soy products as fragrance and flavouring ingredienexhibits. Ligustrazine also has potential nootropic and anti-inflammatory activities in rats [3] .
Hordenine-d6 (Ordenina-d6) is the deuterium labeled Hordenine. Hordenine, an alkaloid found in plants, inhibits melanogenesis by suppression of cyclic adenosine monophosphate (cAMP) production .
Diacerein-d6 is the deuterium labeled Diacerein[1]. Diacerein (Diacerhein), a interleukin-1 beta inhibitor, is a slow-acting medicine of the class anthraquinone used to treat joint diseases[2].
Acyclovir-d4 is the deuterium labeled Acyclovir. Acyclovir (Aciclovir) is a guanosine analogue and an orally active antiviral agent. Acyclovir inhibits HSV-1 (IC50 of 0.85 μM), HSV-2 (IC50 of 0.86 μM) and varicella-zoster virus. Acyclovir can be phosphorylated by viral thymidine kinase (TK), and Acyclovir triphosphate interferes with viral DNA polymerization through competitive inhibition with guanosine triphosphate and obligatory chain termination[1][2][3]. Acyclovir prevents bacterial infections during induction therapy for acute leukaemia[4].
Guanidine-d5 (hydrochloride) is the deuterium labeled Guanidine hydrochloride[1]. Guanidine hydrochloride (Guanidinium chloride) a strong chaotrope, is also a strong denaturant of proteins[2][3].
Procyclidine-d5 (Tricyclamol-d5) is deuterium labeled Procyclidine (hydrochloride). Procyclidine (Tricyclamol, (±)-Procyclidine) hydrochloride , an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine hydrochloride can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy [3].
Hydroxyzine-d4 (dihydrochloride) is the deuterium labeled Hydroxyzine dihydrochloride. Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder[1][2].
Sulfamethazine-d4 is a deuterium labeled Sulfamethazine (Sulfadimidine). Sulfamethazine is an antimicrobial that is widely used to treat and prevent various animal diseases (such as gastrointestinal and respiratory tract infections)[1][2].
4-Acetyl-N-methylaniline-13C,d3 (1-(4-(Methylamino)phenyl)ethanone-13C,d3) is a 13C and deuterated isotope of 4-Acetyl-N-methylaniline. Compounds labeled with stable or radioactive isotopes can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
4-Aminobenzoic acid-d4 is the deuterium labeled 4-Aminobenzoic acid. 4-Aminobenzoic acid is an intermediate in the synthesis of folate by bacteria, plants, and fungi.
Roflumilast-d4 is the deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells[1][2].
2-Phenylethanol-d9 is the deuterium labeled 2-Phenylethanol[1]. 2-Phenylethanol (Phenethyl alcohol), extracted from rose, carnation, hyacinth, Aleppo pine, orange blossom and other organisms, is a colourless liquid. It has a pleasant floral odor and also an autoantibiotic produced by the fungus Candida albicans[2]. It is used as an additive in cigarettes and also used as a preservative in soaps due to its stability in basic conditions.
Butylparaben-d4 is the deuterium labeled Butylparaben. Butylparaben is an organic compound, has proven to be a highly successful antimicrobial preservative in cosmetics, also used in medication suspensions, and as a flavoring additive in food.
2-Phenylethanol-d5 is the deuterium labeled 2-Phenylethanol[1]. 2-Phenylethanol (Phenethyl alcohol), extracted from rose, carnation, hyacinth, Aleppo pine, orange blossom and other organisms, is a colourless liquid. It has a pleasant floral odor and also an autoantibiotic produced by the fungus Candida albicans[2]. It is used as an additive in cigarettes and also used as a preservative in soaps due to its stability in basic conditions.
2-Phenylethanol-d4 is the deuterium labeled 2-Phenylethanol[1]. 2-Phenylethanol (Phenethyl alcohol), extracted from rose, carnation, hyacinth, Aleppo pine, orange blossom and other organisms, is a colourless liquid. It has a pleasant floral odor and also an autoantibiotic produced by the fungus Candida albicans[2]. It is used as an additive in cigarettes and also used as a preservative in soaps due to its stability in basic conditions.
Toremifene-d6 (Z-Toremifene-d6) hydrochloride is deuterium labeled Toremifene. Toremifene is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively .
Phenylbutyrate-d11 (sodium) is deuterium labeled Sodium 4-phenylbutyrate. Sodium 4-phenylbutyrate (4-PBA sodium) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research[1].
D-erythro-Sphingosine-13C2,d2 is a deuterated labeled D-erythro-Sphingosine . D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator [3] .
L-Tryptophan- 15N2,d8 is the deuterium and 15N-labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3[1].
Cisapride-d6 (R51619-d6) is deuterium labeled Cisapride. Cisapride (R 51619) is an orally active 5-HT4 receptor agonist with an EC50 value of 140 nM. Cisapride is a hERG blocker with an IC50 value of 9.4 nM. Cisapride is a gastroprokinetic agent that stimulates gastrointestinal motor activity [3] .
L-Tryptophan-d8 is the deuterium labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3[1].
Rifampicin-d8 (Rifampin-d8) is the deuterium labeled Rifampicin. Rifampicin is a potent and broad spectrum antibiotic against bacterial pathogens. Rifampicin has anti-influenza virus activities.
Oxaprozin-d5 is deuterium labeled Oxaprozin. Oxaprozin is an inhibitor of both COX-1 and COX-2 with IC50s of 2.2 μM and 36 μM for human platelet COX-1 and IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin also inhibits the activation of NF-κB.
Thymidine-d4 is the deuterium labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[1][2][3].
Miltefosine-d4 (HePC-d4) is deuterium labeled Miltefosine. Miltefosine is a broad spectrum antimicrobial, anti-leishmanial, phospholipid agent acting by inhibiting the PI3K/Akt activity [3] . Miltefosine is an inhibitor of CTP-phosphocholine cytidyltransferase (CCT) .
Levamlodipine-d4 is the deuterium labeled Levamlodipine. Levamlodipine ((S)-Amlodipine) is a powerful dihydropyridine calcium channel blocker, possessing vasodilation properties and used in the treatment of hypertension and angina[1].
Norverapamil-d7 is a deuterium labeled Norverapamil ((±)-Norverapamil). Norverapamil, an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor[1][2].
Pitolisant-d5 hydrochloride (Ciproxidine-d5 hydrochloride) is the deuterium labeled Pitolisant hydrochloride (HY-12199B). Pitolisant hydrochloride is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM) .
Loratadine-d4 is the deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
Dexamethasone-d5 is the deuterium labeled Dexamethasone. Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses[1][2].
Adefovir-d4 is the deuterium labeled Adefovir. Adefovir (GS-0393) is an adenosine monophosphate analog antiviral agent that after intracellular conversion to Adefovir diphosphate inhibits HBV DNA polymerase. Adefovir has an IC50 of 0.7 μM against HBV in the HepG2.2.15 cell line. Adefovir has good antiviral activity against several viruses, including HBV and herpesviruses[1][2][3].
Bisdemethoxycurcumin-d8 is the deuterium labeled Bisdemethoxycurcumin. Bisdemethoxycurcumin(Curcumin III; Didemethoxycurcumin) is a natural derivative of curcumin with anti-inflammatory and anti-cancer activities.
Estrone-d2 is the deuterium labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells[1][2].
N-Nitrosodiethylamine-d4 is the deuterium labeled N-Nitrosodiethylamine[1]. N-Nitrosodiethylamine (Diethylnitrosamine) is a potent hepatocarcinogenic dialkylnitrosoamine. N-Nitrosodiethylamine is mainly present in tobacco smoke, water, cheddar cheese, cured, fried meals and many alcoholic beverages. N-Nitrosodiethylamine is responsible for the changes in the nuclear enzymes associated with DNA repair/replication. N-Nitrosodiethylamine results in various tumors in all animal species. The main target organs are the nasal cavity, trachea, lung, esophagus and liver.
Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].
Piperin-d10 is deuterium labeled Piperine. Piperine is an alkaloid, can be isolated from pepper. Piperine can inhibit the activity of P-glycoprotein and CYP3A4. Piperine inhibits HeLa cells with an IC50 of 61.94±0.054 μg/mL [3] .
Omadacycline-d9 (PTK 0796-d9; Amadacycline-d9) is the deuterium labeled Omadacycline (HY-14865) that can be used as the internal standard for the analysis of Omadacycline .
Thymidine-d2 is the deuterium labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[1
N-Nitrosodiethylamine-d10 is the deuterium labeled N-Nitrosodiethylamine[1]. N-Nitrosodiethylamine (Diethylnitrosamine) is a potent hepatocarcinogenic dialkylnitrosoamine. N-Nitrosodiethylamine is mainly present in tobacco smoke, water, cheddar cheese, cured, fried meals and many alcoholic beverages. N-Nitrosodiethylamine is responsible for the changes in the nuclear enzymes associated with DNA repair/replication. N-Nitrosodiethylamine results in various tumors in all animal species. The main target organs are the nasal cavity, trachea, lung, esophagus and liver.
Altrenogest-d5 is the deuterium labeled Altrenogest. Altrenogest (Allyltrenbolone) is a progestogen structurally related to veterinary steroid trenbolone.
Bambuterol-d9 (hydrochloride) is the deuterium labeled Bambuterol. Bambuterol ((±)-Bambuterol) hydrochloride is a long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma; it also is a prodrug of terbutaline.
Dexamethasone-d4 is deuterium labeled Dexamethasone. Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
Leriglitazone-d4 (MIN-102-d4; Hydroxypioglitazone-d4) is deuterium labeled Leriglitazone. Leriglitazone is an orally active and a BBB-penatrable PPARγ agonist with an EC50 of 9 μM. Leriglitazone, as a regulator of mitochondrial function, has neuroprotective, anti-inflammatory and antioxidant effects. Leriglitazone can be used in the study of neuroinflammatory and neurodegenerative diseases .
Sucralose-d6 is deuterium labeled Sucralose. Sucralose (E955; Trichlorosucrose) is a non-nutritive artificial sweetener and sugar substitute. Sucralose can activate a conserved neural fasting response and thereby exerts an appetite-stimulating effect in rodents[1][2].
Spermine-d20 (NSC 268508-d20) is deuterium labeled Spermine. Spermine (NSC 268508) functions directly as a free radical scabenger to protect DNA from free radical attack. Spermine has antiviral effects .
Sulfameter-d4 (Sulfametoxydiazine-d4; 5-Methoxysulfadiazine-d4) is the deuterium labeled Sulfameter (HY-B0213) . Sulfameter (Sulfametoxydiazine; 5-Methoxysulfadiazine) is an effective long-acting sulfonamide antibiotic with antibacterial activities. Sulfameter can be used for the research of urinary tract infections and lepriasis .
Mitoxantrone-d8 dihydrochloride is deuterated labeled Mitoxantrone dihydrochloride (HY-13502A). Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity [3] . Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively .
Rifampicin-d4 is the deuterium labeled Rifampicin. Rifampicin is a potent and broad spectrum antibiotic against bacterial pathogens. Rifampicin has anti-influenza virus activities.
Rifabutin-d7 is the deuterium labeled Rifabutin. Rifabutin (Ansamycin) is a semisynthetic ansamycin antibiotic with potent antimycobacterial properties. Rifabutin inhibits DNA-dependent RNA polymerase.
Exemestane-d2 is the deuterium labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research[1][2].
Rebamipide-d4 is deuterium labeled Rebamipide. Rebamipide is a mucoprotective agent. Rebamipide induces COX-2 expression, increases PGE2 levels, and enhances gastric mucosal defense in a COX-2-dependent manner[1].
Salbutamol-d9 (acetate) is the deuterium labeled Salbutamol[1]. Salbutamol is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease (COPD).
(±)-Penbutolol-d9 (hydrochloride) is a deuterium labeled (±)-Penbutolol hydrochloride. (+)-Penbutolol hydrochloride is a β-adrenoceptor antagonist, with an IC50 of 0.74 μM[1].
L-Tryptophan-d5 is the deuterium labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3[1].
Rifampicin-d11 (Rifampin-d11; Rifamycin AMP-d11) is the deuterium labeled Rifampicin (HY-B0272) . Rifampicin is a potent and broad spectrum antibiotic against bacterial pathogens. Rifampicin has anti-influenza virus activities. Rifampicin shows anti-orthopoxvirus activity .
Mecillinam-d12 is deuterium labeled Mecillinam. Mecillinam (Amdinocillin), the β-lactam antibiotic, has a broad spectrum of activity against gram-negative organisms[1].
Salbutamol-d9 is the deuterium labeled Salbutamol. Salbutamol is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease (COPD).
Guanosine-d13 (DL-Guanosine-d13) is a deuterium of Guanosine (HY-N0097). Guanosine (DL-Guanosine) is a purine nucleoside comprising guanine attached to a ribose (ribofuranose) ring via a β-N9-glycosidic bond. Guanosine possesses anti-HSV activity .
Norverapamil-d6 ((±)-Norverapamil-d6) hydrochloride is deuterium labeled Norverapamil (hydrochloride). Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor [3].
Nateglinide-d5 is a deuterium labeled Nateglinide. Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K+ channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus[1][2].
DL-Mevalonolactone-d7 is the deuterium labeled DL-Mevalonolactone. DL-Mevalonolactone ((±)-Mevalonolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone (Mevalonolactone) decreases mitochondrial membrane potential (∆Ψm), NAD(P)H content and the capacity to retain Ca2+ in the brain, besides inducing mitochondrial swelling[1][2].
Sulfabrom-d4 (N 3517-d4) is is the deuterium labeled Sulfabrom (HY-U00131). Sulfabrom is a long-acting Sulfonamide that is used for the treatment of coccidiosis and various bacterial infections in the poultry, swine and cattle .
Aspirin-d4 is the deuterium labeled Aspirin. Aspirin is a non-selective and irreversible inhibitor of COX-1 and COX-2 with IC50s of 5 and 210 μg/mL[1][2].
Ritonavir-d8 is deuterated labeled Ritonavir (HY-90001). Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.61 μM.
Estrone-d4 is the deuterium labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells[1][2].
Thymidine-d14 (DThyd-d14; NSC 21548-d14) is deuterium labeled Thymidine (HY-N1150). Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication.
Mitoxantrone-d8 (mitozantrone-d8) is the deuterium labeled Mitoxantrone. Mitoxantrone is a topoisomerase II inhibitor and also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM[1][2].
Ritonavir-d6 is the deuterium labeled Ritonavir. Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.61 μM[1][2].
Loratadine-d5 is the deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
Imidaprilate-d5 is deuterium labeled Imidaprilate. Imidaprilate is an active metabolite of TA-6366, acts as a potent angiotensin converting enzyme (ACE) inhibitor, with an IC50 of 2.6 nM, and is used in the research of hypertensive disease.
Nicotinamide-d4 is the deuterium labeled Nicotinamide. Nicotinamide is a form of vitamin B3 that plays essential roles in cell physiology through facilitating NAD+ redox homeostasis and providing NAD+ as a substrate to a class of enzymes that catalyze non-redox reactions. Nicotinamide is an inhibitor of SIRT1.
D-Alanine-d7 is the deuterium labeled D-Alanine. D-Alanine is a weak GlyR (inhibitory glycine receptor) and PMBA agonist, with an EC50 of 9 mM for GlyR.
Citicoline-d9 (Cytidine diphosphate-choline-d9) sodium is the deuterium labeled Citicoline sodium (HY-B0739A). Citicoline sodium is an endogenous intermediate in the synthesis of phosphatidylcholine which is a component of cell membranes. Citicoline sodium inhibits reactive oxygen species (ROS) and apoptosis. Citicoline sodium can be used for neurological disease and hearing loss study [3] .
Propylthiouracil-d5 is the deuterium labeled Propylthiouracil. Propylthiouracil (6-Propyl-2-thiouracil) is a thyroperoxidase and 5'-deiodinase inhibitor.
D-Alanine-d4 is the deuterium labeled D-Alanine. D-Alanine is a weak GlyR (inhibitory glycine receptor) and PMBA agonist, with an EC50 of 9 mM for GlyR.
Cabazitaxel-d6 is the deuterium labeled Cabazitaxel. Cabazitaxel is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity[1][2].
Cabazitaxel-d9 is deuterium labeled Cabazitaxel. Cabazitaxel is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity.
(-)-(S)-Cibenzoline-d4 (Escibenzoline-d4) is deuterium labeled (-)-(S)-Cibenzoline. (-)-(S)-Cibenzoline (Escibenzoline), a S(+)-enantiomer of Cibenzoline, is an antiarrhythmic agent .
Obeticholic acid-d5 is the deuterium labeled Obeticholic acid. Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy[1][2][3].
Clomipramine-d6 (hydrochloride) is the deuterium labeled Clomipramine hydrochloride. Clomipramine (Chlorimipramine) hydrochloride is a potent 5-HT reuptake blocker with the IC50 value of 1.5 nM. Clomipramine hydrochloride is a tricyclic antidepressant that can be used for the research of depression and obsessive compulsive disorder (OCD)[1].
D-Alanine-d is the deuterium labeled D-Alanine. D-Alanine is a weak GlyR (inhibitory glycine receptor) and PMBA agonist, with an EC50 of 9 mM for GlyR[1].
Raloxifene-d10-1 is the deuterium labeled Raloxifene[1]. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research[2].
Benzoin-d10 (DL-Benzoin-d10) is the deuterium labeled Benzoin (HY-B1550). Benzoin (DL-Benzoin), a natural balsamic resin, is a PI3Kα inhibitor with anticancer effects. Benzoin inihits the growth of colon cancer cell line (HCT-116). Benzoin can be used as a food additive .
Daclatasvir- 13C2,d6 (BMS-790052- 13C2,d6) is 13C and deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 μM and 3.27 μM, respectively [3] .
HTR2A antagonist 1 (Compound 15f) is a HTR2A antagonist, with an IC50 of 42.79 nM. HTR2A antagonist 1 induces sub-G1 cell cycle arrest and apoptosis in colorectal cancer cells via the activation of p53/p21/caspase 3 signaling. HTR2A antagonist 1 has good liver microsomal stability. HTR2A antagonist 1 can be used for the research of colorectal cancer .
CTL-12 is an inhibitor of fatty acid synthase (FASN) (IC50: 2.5 μM) and can induce apoptosis. CTL-12 blocks the cell cycle in the Sub-G1/S phase, upregulates the expression of caspase-9 and the apoptosis marker Bax, and downregulates the anti-apoptotic marker Bcl-xL. CTL-12 inhibits de novo lipogenesis, blocks the metabolic demands of tumor cells, and is commonly used in breast and colorectal cancer research .
3-Hydroxykynurenine- 13C3, 15N (3-Hydroxy-DL-kynurenine- 13C3, 15N) is the 13C and 15N labeled 3-Hydroxykynurenine (HY-113294) . 3-Hydroxykynurenine, a metabolite of tryptophan, is a potential endogenous neurotoxin whose increased levels have been described in several neurodegenerative disorders. 3-Hydroxykynurenine induces neuronal apoptosis .
L-Alanine- 13C3, 15N is the 13C- and 15N-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
Estradiol-d2 is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway[1][2][3].
D-Glucose-d1-2 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
Retinoic acid-d6 is the deuterium labeled Retinoic acid[1]. Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha[2][3][4][5][6][7].
Estradiol-d5 is deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway[1][2][3].
Vincristine-d6 (sulfate) is the deuterium labeled Vincristine sulfate. Vincristine sulfate is an antitumor vinca alkaloid which inhibits microtubule formation in mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. It binds to microtubule with a Ki of 85 nM.
D-Glucose-d12-12 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
D-Glucose-d2-1 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling mol
Retinoic acid-d5 is the the deuterium labeled Retinoic acid (HY-14649). Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha [3] .
Doxifluridine-d2 is the deuterium labeled Doxifluridine[1]. Doxifluridine is a thymidine phosphorylase activator for PC9-DPE2 cells with IC50 of 0.62 μM.
Estradiol-d4 is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway[1][2][3].
D-Glucose-d-44 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
Tauroursodeoxycholate-d4-1 is the deuterium labeled Tauroursodeoxycholate. Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
D-Glucose-d2-2 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling mol
D-Glucose-d-11 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
Molnupiravir-d7 is the deuterium labeled Molnupiravir. Molnupiravir (EIDD-2801) is an orally bioavailable prodrug of the ribonucleoside analog EIDD-1931. Molnupiravir has broad spectrum antiviral activity against influenza virus and multiple coronaviruses, such as SARS-CoV-2, MERS-CoV, SARS-CoV. Molnupiravir has the potential for the research of COVID-19, and seasonal and pandemic influenza[1][2].
Adenosine-d13 (Adenine riboside-d13; D-Adenosine-d13) is deuterium labeled Adenosine (HY-B0228). Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation.
Dapivirine-d4 (TMC120-d4) is deuterium labeled Dapivirine. Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations [3].
Paquinimod-d5 is a deuterated analog of Paquinimod (HY-100442). Paquinimod (ABR 215757) is a specific and orally active inhibitor of S100A8/S100A9. Paquinimod rescues the pneumonia with substantial reduction of viral loads in SARS-CoV-2-infected mice [3].
Naftopidil-d5 is deuterium labeled Naftopidil. Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia[1][2].
(±)-Leucine-d10 is the deuterium labeled (±)-Leucine. (±)-Leucine (DL-Leucine), an isomer of Leucine, chemosterilant and dietary additive. (±)-Leucine inhibits growth of Escherichia coli HfrH by 92.08%[1].
Etoricoxib-d4 is a deuterium labeled Etoricoxib. Etoricoxib is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.
Vitamin K1-d4 is the deuterium labeled Vitamin K1. Vitamin K1 a naturally occurring vitamin required for blood coagulation and bone and vascular metabolism[1].
L-Carnitine-d9 (chloride)e is the deuterium labeled L-Carnitine chloride. L-Carnitine chloride, a highly polar, small zwitterion, is an essential co-factor for the mitochondrial β-oxidation pathway. L-Carnitine chloride functions to transport long chain fatty acyl-CoAs into the mitochondria for degradation by β-oxidation. L-Carnitine chloride is an antioxidant. L-Carnitine chloride can ameliorate metabolic imbalances in many inborn errors of metabolism[1][2][3].
Pantoprazole-d6 is deuterium labeled Pantoprazole. Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI)[1]. Pantoprazole, a substituted benzimidazole, is a potent H+/K+-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142)[3][4].
Amantadine-d15 is the deuterium labeled Amantadine. Amantadine (1-Adamantanamine) is an antiviral agent with activity against influenza A viruses. Amantadine blocks the proton flow through the M2 ion channel (M2 proton channel of influenza A) and thus prevents the release of viral RNA into the cytoplasm of the infected cells. Amantadine is an antiparkinsonian agent[1][2].
Dalbavancin-d6 is the deuterium labeled Dalbavancin[1]. Dalbavancin (MDL-63397) is a semisynthetic lipoglycopeptide antibiotic with potent bactericidal activity against Gram-positive bacteria. Dalbavancin inhibits Staphylococcus aureus and Bacillus anthracis with MIC90s of 0.06 μg/mL and 0.25 μg/mL, respectively[2][3].
Fosamprenavir-d4 is deuterium labeled Fosamprenavir. Fosamprenavir (Amprenavir phosphate;GW 433908) is a phosphate ester proagent of the antiretroviral protease inhibitor Amprenavir, with improved solubility[1]. Anti-HIV infection[1].
Lapatinib-d4 is the deuterium labeled Lapatinib (HY-50898). Lapatinib is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1][2].
Lapatinib-d5 is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1].
Lapatinib-d4 (GW572016-d4) tosylate is deuterium labeled Lapatinib (tosylate). Lapatinib (GW572016) tosylate is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
Tulathromycin A-d7 (Tulathromycin-d7) is deuterium labeled Tulathromycin A. Tulathromycin A (Tulathromycin), a macrolide antibiotic, inhibits protein synthesis (IC50=0.26 μM) by targeting bacterial ribosome. Tulathromycin A is used for the research of respiratory disease in cattle and swine. Immunomodulatory effects [3] .
Samidorphan-d4 is the deuterium labeled Samidorphan(HY-123689).Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo .
Etravirine-d4 is the deuterium labeled Etravirine. Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.
Molindone-d8 is the deuterium labeled Molindone. Molindone hydrochloride (EN-1733A) is a therapeutic antipsychotic, used in the treatment of schizophrenia, works by blocking the effects of dopamine in the brain, leading to diminished psychoses[1][2].
Dacomitinib-d10 is deuterium labeled Dacomitinib. Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively[1].
Atropine-d5 is the deuterium labeled Atropine (sulfate monohydrate). Atropine (Tropine tropate) sulfate monohydrate is a broad-spectrum and competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect[1].
Amantadine-d6 is the deuterium labeled Amantadine[1]. Amantadine (1-Adamantanamine) is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine also has anti-orthopoxvirus and anticancer activity. Amantadine can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research[2][3][4][5][6][7].
Daclatasvir-d6 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively[1][2][3].
(±)-Leucine-d7 is the deuterium labeled (±)-Leucine. (±)-Leucine (DL-Leucine), an isomer of Leucine, chemosterilant and dietary additive. (±)-Leucine inhibits growth of Escherichia coli HfrH by 92.08%[1].
Lifitegrast-d6 (SAR 1118-d6) is deuterium labeled Lifitegrast. Lifitegrast (SAR 1118) is a potent integrin antagonist. Lifitegrast blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. Lifitegrast can be used for researching dry eye disease .
Levodropropizine-d8 is deuterium labeled Levodropropizine. Levodropropizine (DF-526) is a histamine receptor inhibitor, Levodropropizine is an effective and very well tolerated peripheral antitussive agent.
Docosahexaenoic acid-d5 is the deuterium labeled Docosahexaenoic Acid. Docosahexaenoic Acid (DHA) is an omega-3 fatty acid abundantly present brain and retina. It can be obtained directly from fish oil and maternal milk.
Mavacamten-d6 (MYK461-d6; SAR439152-d6) is deuterium labeled Mavacamten (HY-109037). Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
Mifepristone-d6 is deuterated labeled Mifepristone (HY-13683). Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay .
D-Sorbitol-d4 is the deuterium labeled D-Sorbitol. D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and diet
Irbesartan-d7 is deuterated labeled Irbesartan (HY-B0202). Irbesartan (SR-47436) is an orally active Ang II type 1 (AT1) receptor blocker (ARB). Irbesartan can relax the blood vessels, low blood pressure and increase the supply of blood and oxygen to the heart. Irbesartan can be used for the research of high blood pressure, heart failure, and diabetic kidney disease .
Cobimetinib-d4 hydrochloride is deuterated labeled Cobimetinib (HY-13064). Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK1 inhibitor with an IC50 of 4.2 nM for MEK1.
Baloxavir-d4 (Baloxavir acid-d4; S-033447-d4) is the deuterium-labeled Baloxavir (HY-109025A). Baloxavir-d4 (Baloxavir-d4 acid), derived from the proagent Baloxavir-d4 marboxil, is a first-in-class, potent and selective cap-dependent endonuclease (CEN) inhibitor within the polymerase PA subunit of influenza A and B viruses. Baloxavir-d4 inhibits viral RNA transcription and replication and has potently antiviral activity .
Selexipag-d6 is deuterium labeled Selexipag. Selexipag (NS-304) is an orally available and potent agonist for the Prostacyclin (PGI2) receptor (IP receptor).
Navtemadlin-d7 is the deuterium labeled Navtemadlin. Navtemadlin (AMG 232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC50 of 0.6 nM. Navtemadlin binds to MDM2 with a Kd of 0.045 nM[1][2].
N-Benzylaniline-d2 (N-Phenylbenzylamine-d2) is the deuterium labeled N-Benzylaniline (HY-W016321). N-Benzylaniline is an N-alkyl-ated derivative of aniline .
Serotonin-d4 (5-Hydroxytryptamine-d4) hydrochloride is the deuterium labeled Serotonin (hydrochloride) (HY-B1473) . Serotonin (5-Hydroxytryptamine) hydrochloride is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin hydrochloride is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM .
Octacosane-d58 is the deuterium labeled Octacosane[1]. Octacosane is an endogenous metabolite with antibacterial activity. Octacosane shows high cytotoxicity against murine melanoma B16F10-Nex2 cells besides inducing protection against a grafted subcutaneous melanoma. Octacosane has the larvicidal activity against mosquito Culex quinquefasciatus with the LC50 concentration of 7.2 mg/l[2][3][4].
Fexofenadine-d10 (hydrochloride) is deuterium labeled Fexofenadine (hydrochloride). Fexofenadine hydrochloride (MDL-16455 hydrochloride), a H1R antagonist, is an anti-allergic agent used in seasonal allergic rhinitis and chronic idiopathic urticarial (person aged ≥16 years)[1].
D-Sorbitol-d2 is the deuterium labeled D-Sorbitol. D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and diet
Pergolide-d7 (mesylate) is the deuterium labeled Pergolide mesylate. Pergolide mesylate (Pergolide methanesulfonate), an Ergoline derivative, is a potent and orally active dopamine D1 and D2 receptors agonist. Pergolide mesylate can be used for Parkinson's disease and hyperprolactinaemia research[1][2].
Procainamide-d4 hydrochloride is deuterated labeled Procainamide. Procainamide hydrochloride is an antiarrhythmic agent used in the study of cardiac arrhythmias.
Secnidazole-d6 is the deuterium labeled Secnidazole. Secnidazole (RP-14539;PM-185184) is an orally active azole antibiotic with a longer half-life than metronidazole (HY-B0318). Secnidazole is against the vaginosis-associated bacteria and has the potential for bacterial vaginosis research[1].
Entinostat-d4 is the deuterium labeled Entinostat[1]. Entinostat is an oral and selective class I HDAC inhibitor, with IC50s of 243 nM, 453 nM, and 248 nM for HDAC1, HDAC2, and HDAC3, respectively[2].
Ondansetron-d6 (hydrochloride) is the deuterium labeled Ondansetron hydrochloride[1]. Ondansetron hydrochloride is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy[2][3][4][5][6][7].
Lornoxicam-d4 is the deuterium labeled Lornoxicam. Lornoxicam (Chlortenoxicam), a COX-1 and COX-2 inhibitor, is a new nonsteroidal anti-inflammatory agent (NSAID).
Chlorambucil-d8 is the deuterium labeled Chlorambucil. Chlorambucil (CB-1348), an orally active antineoplastic agent, is a bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease[1][2][3][4].
Olaparib-d5 (AZD2281-d5) is the deuterium labeled Olaparib (HY-10162). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator [3] .
Entecavir-d2 is the deuterium labeled Entecavir. Entecavir (SQ 34676; BMS 200475) is a potent and selective inhibitor of HBV, with an EC50 of 3.75 nM in HepG2 cell.
D-Sorbitol-d8 is the deuterium labeled D-Sorbitol. D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and dietary supplement[1].
Boceprevir-d9 is the deuterium labeled Boceprevir. Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a Ki of 14 nM in both enzyme assay and an EC90 of 350 nM in cell-based replicon assay[1][2][3][4][5]. Boceprevir inhibits SARS-CoV-2 3CLpro activity[6].
Dehydroaripiprazole-d8 is deuterium labeled Dehydroaripiprazole. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole[1][2][3].
Adenosine-d9 is the deuterium labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physio .
Penciclovir-d4 is the deuterium labeled Penciclovir. Penciclovir is reported to be potent against HSV types 1 and 2 with IC50 of 0.04-1.8 μg/mL and 0.06-4.4 μg/mL, respectively[1][2].
Tasimelteon-d5 is the deuterium labeled Tasimelteon. Tasimelteon (BMS-214778) is an orally active and selective dual melatonin receptor agonist (DMRA). Tasimelteon has 2.1-4.4 times greater affinity for the MT2 receptor than for the MT1 receptor. Tasimelteon is a circadian regulator and has the potential for Non-24-Hour Sleep-Wake Disorder (Non-24)[1][2].
Lifitegrast-d4 (SAR 1118-d4) is deuterium labeled Lifitegrast. Lifitegrast (SAR 1118) is a potent integrin antagonist. Lifitegrast blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. Lifitegrast can be used for researching dry eye disease .
Cysteamine-d4 (hydrochloride) is the deuterium labeled Cysteamine hydrochloride. Cysteamine hydrochloride (2-Aminoethanethiol hydrochloride) is an orally active agent for the treatment of nephropathic cystinosis and an antioxidant.
Cabozantinib-d6 is the deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively[1][2][3].
Samidorphan-d5 (ALKS-33-d5) is is a deuterated compound of Samidorphan. Samidorphan is an orally active opioid system modulator that binds with high affinity to μ-opioid, κ-opioid, and δ-opioid receptors. Samidorphan is a μ-opioid receptor antagonist and a partial agonist at k-opioid and δ-opioid receptors. Samidorphan acts primarily as an opioid receptor antagonist in vivo [3] .
Adenosine-d2 is the deuterium labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physio
Isavuconazole-d4 is a deuterium labeled Isavuconazole (BAL-4815). Isavuconazole is a triazole proagent with antifungal activity against yeasts, molds, and dimorphic fungi[1].
Fluralaner-d5 (A1443-d5) is deuterium labeled Fluralaner. Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels .
Glycochenodeoxycholic acid-d7 (sodium) is the deuterium labeled Glycochenodeoxycholic acid (sodium salt). Glycochenodeoxycholic acid sodium salt (Chenodeoxycholylglycine sodium salt) is a bile acid formed in the liver from chenodeoxycholate and glycine. It acts as a detergent to solubilize fats for absorption and is itself absorbed. Glycochenodeoxycholic acid sodium salt (Chenodeoxycholylglycine sodium salt) induces hepatocyte apoptosis[1][2].
Mirtazapine-d4 is deuterium labeled Mirtazapine. Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively[1][2].
Lapatinib-d7 (dihydrochloride) is the deuterium labeled Lapatinib dihydrochloride. Lapatinib (GW572016) dihydrochloride is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1].
Dacomitinib-d10 (dihydrochloride) is the deuterium labeled Dacomitinib dihydrochloride. Dacomitinib (PF-00299804) dihydrochloride is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively[1].
Cephalexin-d5 (monohydrate) is the deuterium labeled Cephalexin monohydrate. Cephalexin monohydrate is a potent, orally active and the first-generation cephalosporin antibiotic. Cephalexin monohydrate kills gram-positive and some gram-negative bacteria by disrupting the growth of the bacterial cell wall. Cephalexin monohydrate is used for the research of pneumonia, strep throat, and bacterial endocarditis, et al[1].
Tivozanib-d6 (AV-951-d6) is deuterium labeled Tivozanib. Tivozanib (AV-951; KRN951) is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib exhibits antitumor efficacy .
Defactinib-d6 is a deuterium labeled Defactinib (HY-12289). Defactinib is a novel FAK inhibitor with potential antiangiogenic and antineoplastic activities .
Midostaurin-d5 is a deuterium labeled Midostaurin. Midostaurin is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM[1].
Palmitoylethanolamide-d4 is the deuterium labeled Palmitoylethanolamide. Palmitoylethanolamide (Palmidrol) is an active endogenous compound which can used for preventing virus infection of the respiratory tract.
Actinine-d9 chloride is the deuterium labeled Actinine chloride. Actinine chloride is angiopathic substance produced as an intermediary metabolite by gut microbiota that feed on carnitine in dietary red meat[1][2].
6-Mercaptopurine-d2 is the deuterium labeled 6-Mercaptopurine. 6-Mercaptopurine is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive agent[1][2].
Cyclamic acid-d11 (Sodium cyclamate-d11) sodiumis deuterium labeled Cyclamic acid (sodium). Cyclamic acid sodium (Sodium cyclamate) is a commonly used sweetener. Cyclamic acid sodium is toxic to osteoblasts and can inhibit cell proliferation, induce apoptosis and reduce cell mineralization. Cyclamic acid sodium causes focal necrosis of bladder organs in rats in vitro, which can promote bladder cancer, but some studies have shown that low doses of Cyclamic acid sodium have no carcinogenic effect. In addition, Cyclamic acid sodium has no effect on insulin and glucagon secretion induced by arginine [3] .
Undecanoic acid-d2 is the deuterium labeled Undecanoic acid. Undecanoic acid (Undecanoate) is a monocarboxylic acid with antimycotic property, which inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum[1].
Mavacamten-d1 (MYK461-d1; SAR439152-d1) is deuterium labeled Mavacamten (HY-109037). Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
Ambrisentan-d10 (BSF 208075-d10; LU 208075-d10) is the deuterium labled Ambrisentan (HY-13209). Ambrisentan is a selective ET type A receptor (ETAR) antagonist.
Gestodene-d6is the deuterium labeled Gestodene. Gestodene(SHB 331) is a progestogen hormonal contraceptive[1][2]. Gestodene-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Lubiprostone-d7 (RU-0211-d7) is the deuterium labeled Lubiprostone. Lubiprostone (RU0211) is a gastrointestinal agent used for the treatment of idiopathic chronic constipation[1][2].
Tegoprazan (CJ-12420; RQ-00000004), a potassium-competitive acid blocker, is a reversible, oral active and highly selective inhibitor of gastric H+/K+-ATPase that could control gastric acid secretion and motility, with IC50 values ranging from 0.29-0.52 μM for porcine, canine, and human H +/K +-ATPases in vitro. Tegoprazan significantly improves colitis in mice and enhances the intestinal epithelial barrier function. Tegoprazan is promising for research of Inflammatory bowel, gastric acid-related, motilityimpaired diseases [3].
Duloxetine-d7 hydrochloride ((S)-Duloxetine-d7 hydrochloride) is the deuterium labeled Duloxetine hydrochloride (HY-B0161A). Duloxetine hydrochloride ((S)-Duloxetine hydrochloride) is a serotonin-norepinephrine reuptake inhibitor (SNRI) with a Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD) .
Glimepiride-d4-1 is deuterium labeled Glimepiride. Glimepiride (Glimperide) is a medium-to-long acting sulfonylurea anti-diabetic compound with an ED50 of 182 μg/kg.
Darolutamide-d4 (ODM-201-d4) is deuterium labeled Darolutamide. Darolutamide (ODM-201;BAY-1841788) is a potent androgen receptor (AR) antagonist with an IC50 of 26 nM in in vitro assay .
Resveratrol-d4 is the deuterium labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].
Resiquimod-d5 is deuterium labeled Resiquimod. Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α .
Caspofungin-d4 (acetate) is the deuterium labeled Caspofungin diacetate[1]. Caspofungin (MK-0991) diacetate is a potent antifungal agent. Caspofungin diacetate inhibits the synthesis of the fungal cell wall component β-(l,3)-D-glucan[2][3].
Citronellol-d6 is deuterated labeled Linalool (HY-N0368). Linalool is a natural monoterpene which is a competitive NMDA receptor antagonist. Linalool is orally active and crosses the blood-brain barrier. Linalool has anticancer, antibacterial, anti-inflammatory, neuroprotective, anxiolytic, antidepressant, anti-stress, cardioprotective, hepatoprotective, nephroprotective and pulmonary protective activities [3] .
Ondansetron-d5 is the deuterium labeled Ondansetron. Ondansetron (GR 38032; SN 307) is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy.
Fusidic acid-d6 is the deuterium labeled Fusidic acid. Fusidic acid (Fusidate) a bacteriostatic antibiotic produced from the Fusidium coccineum fungus, belongs to the class of steroids. Fusidic acid has no corticosteroid effects. Fusidic acid inhibits the growth of bacteria by preventing the release of translation elongation factor G (EF-G) from the ribosome[1][2].
L-Serine-d2 is the deuterium labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
Sparsentan-d5 is deuterium labeled Sparsentan. Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively[1].
Irbesartan-d7 hydrochloride is deuterated labeled Irbesartan hydrochloride (HY-B0202A). Irbesartan (SR-47436) hydrochloride is an orally active Ang II type 1 (AT1) receptor blocker (ARB). Irbesartan hydrochloride can relax the blood vessels, low blood pressure and increase the supply of blood and oxygen to the heart. Irbesartan hydrochloride can be used for the research of high blood pressure, heart failure, and diabetic kidney disease .
Pregnanediol-d5 is the deuterium labeled Pregnanediol. Pregnanediol is the major metabolite of progesterone and can be excreted via urine. Pregnanediol offers an indirect way to measure progesterone levels in vivo[1].
Crisaborole-d4 is deuterium labeled Crisaborole. Crisaborole (AN-2728) is a potent inhibitor of PDE4 and cytokine release; inhibit PDE4 with an IC50 of 0.49 μM.
(-)-Epigallocatechin Gallate-d4 (EGCG-d4) is the deuterium labeled (-)-Epigallocatechin Gallate (HY-13653). (-)-Epigallocatechin Gallate (EGCG) is a major polyphenol in green tea, which can inhibit cell proliferation and induce cell apoptosis. (-)-Epigallocatechin Gallate inhibits glutamate dehydrogenase 1/2 (GDH1/2, GLUD1/2) activity. (-)-Epigallocatechin Gallate has a potent anticancer, antioxidant and anti-inflammatory properties against various types of cancers such as colorectal cancer, myeloid leukemia, thyroid carcinoma [3] .
Sparfloxacin-d5 is deuterium labeled Sparfloxacin (HY-B0308). Sparfloxacin is a fluoroquinolone antibiotic, shows broad and potent antibacterial activity .
Everolimus-d4 is the deuterium labeled Everolimus. Everolimus (RAD001) is a Rapamycin derivative and a potent, selective and orally active mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities[1][2].
Olaparib-d8 (AZD2281-d8) is the deuterium labeled Olaparib (HY-10162). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator [3] .
Baricitinib-d5 is the deuterium labeled Baricitinib. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
Barnidipine-d5 (hydrochloride) is the deuterium labeled Barnidipine hydrochloride. Barnidipine hydrochloride (Mepirodipine hydrochloride) is an L-type calcium antagonist (CaA) with high affinity for [3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors[1].Barnidipine hydrochloride (Mepirodipine hydrochloride) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action[2].
Fedratinib-d9 (TG-101348-d9) is deuterium labeled Fedratinib. Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research [3].
Verapamil-d6 (CP-16533-1-d6) hydrochloride is the deuterium labled Verapamil (hydrochloride) (HY-A0064). Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research [3].
Phenylephrine-d6 (hydrochloride) is deuterium labeled Phenylephrine (hydrochloride). (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
Secnidazole-d4 is the deuterium labeled Secnidazole[1]. Secnidazole (RP-14539) is an orally active azole antibiotic and a imidazole mitigator of Serratia marcescens virulence. Secnidazole, as an analog of acylhomoserine lactones, effectively inhibits QS resulting in the attenuation of Pseudomonas aeruginosa pathogenesis. Secnidazole has antimicrobial activity against many anaerobic Gram-negative and Gram-positive bacterial species in vitro. Secnidazole can be used for the research of various diseases, such as amoebiasis and giardiasis, and bacterial vaginitis[1][2][3].
Lomitapide-d8 is deuterium labeled Lomitapide. Lomitapide (AEGR-733; BMS-201038) is a potent inhibitor of microsomal triglyceride-transfer protein (MTP) with an IC50 of 8 nM in vitro.
Pyridoxine-d5 (hydrochloride) is the deuterium labeled Pyridoxine hydrochloride[1]. Pyridoxine hydrochloride (Pyridoxol;Vitamin B6) is a pyridine derivative. Pyridoxine (Pyridoxol;Vitamin B6) exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway[2].
Verapamil-d7 is the deuterium labeled Verapamil (HY-14275). Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research [3].
Serotonin-d4 is deuterium labeled Serotonin. Serotonin is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM.
Albendazole sulfoxide-d7 is the deuterium labeled Albendazole sulfoxide. Albendazole sulfoxide (Ricobendazole), the main active metabolite of Albendazole, exhibits anti-parasite effect against Echinococcus multilocularis Metacestodes[1].
Ranolazine-d8 (dihydrochloride) is the deuterium labeled Ranolazine dihydrochloride. Ranolazine dihydrochloride (CVT 303 dihydrochloride) is an anti-angina agent that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine dihydrochloride is also a partial fatty acid oxidation inhibitor[3].
Undecanoic acid-d21 is the deuterium labeled Undecanoic acid. Undecanoic acid (Undecanoate) is a monocarboxylic acid with antimycotic property, which inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum[1].
Caspofungin-d4 (MK-0991-d4; L-743872-d4) is a deuterium labeled Caspofungin (HY-17006A). Caspofungin is a potent antifungal agent. Caspofungin inhibits the synthesis of the fungal cell wall component β-(l,3)-D-glucan [3].
L-Serine-d7 is the deuterium labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
Cabozantinib-d4 is deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
Dapivirine-d11 is the deuterium labeled Dapivirine. Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations[1][2].
L-Carnitine-d9 is the deuterium labeled L-Carnitine. L-Carnitine (Levocarnitine) is an endogenous molecule involved in fatty acid metabolism, biosynthesized within the human body using amino acids: L-lysine and L-methionine, as substrates. L-Carnitine functions to transport long chain fatty acyl-CoAs into the mitochondria for degradation by β-oxidation. L-carnitine can ameliorate metabolic imbalances in many inborn errors of metabolism[1][2].
Daclatasvir-d16 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively[1][2][3].
Mavacamten-d5 (MYK461-d5; SAR439152-d5) is deuterium labeled Mavacamten (HY-109037). Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
Verlukast-d6 is a deuterium labeled Verlukast. Verlukast is a potent, selective, and orally active antagonist of leukotriene receptor. Verlukast has the potential for the research of asthma[1].
Volinanserin-d4 (hydrochloride) is the deuterium labeled Volinanserin hydrochlorid. Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity[1][2].
Baloxavir-d5 is deuterium labeled Baloxavir. Baloxavir (Baloxavir acid), derived from the proagent Baloxavir marboxil, is a first-in-class, potent and selective cap-dependent endonuclease (CEN) inhibitor within the polymerase PA subunit of influenza A and B viruses. Baloxavir inhibits viral RNA transcription and replication and has potently antiviral activity[1][2].
Methionine-d4 is the deuterium labeled Methionine. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
Ribavirin- 15N, d2 is 15N and deuterated labeled Ribavirin (HY-B0434). Ribavirin (ICN-1229) is an antiviral agent against a broad spectrum of viruses including HCV, HIVl, and RSV. Ribavirin also has anti-orthopoxvirus and anti-variola activities.
Metaxalone-d6 is deuterium labeled Metaxalone. Metaxalone (AHR438; NSC170959) is an FDA-approved muscle relaxant. Metaxalone acts mainly on the central nervous system and achieves muscle relaxation by inhibiting polysynaptic reflex arcs. In addition, Metaxalone is an inhibitor of MAO-A, which has anti-inflammatory and antioxidant effects. Metaxalone inhibits IL-1β-induced inflammatory phenotype, modulates NF-κB and other related signaling pathways, and decreases MAO-A expression and activity in IL-1β-treated microglia [3].
Cyclosporin A acetate-d4 (Cyclosporine A acetate-d4; Ciclosporin A acetate-d4) is a deuterium labeled Cyclosporin A (HY-B0579) . Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM . Cyclosporin A also inhibits CD11a/CD18 adhesion [3].
Maribavir-d6 (1263W94-d6) is a deuterium labeled Maribavir (HY-16305). Maribavir is a potent inhibitor of histone phosphorylation catalyzed by wild-type pUL97 in vitro, with an IC50 of 3 nM .
D-erythro-Sphingosine-d7 is the deuterium labeled D-erythro-Sphingosine. D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator[1][2][3][4].
Ibudilast-d7-1 is the deuterium labeled Ibudilast[1]. Ibudilast (KC-404;AV-411;MN-166) is a cyclic AMP phosphodiesterase (PDE) inhibitor. Ibudilast has platelet anti-aggregatory effects. Ibudilast can be used for the research of asthma for its inhibitory effects on tracheal smooth muscle contractility. Ibudilast may be a useful neuroprotective and anti-dementia agent counteracting neurotoxicity in activated microglia[2].
Glutathione oxidized- 13C4, 15N2 is the 13C and 15N labeled Glutathione oxidized (HY-D0844). Glutathione oxidized is produced by the oxidation of glutathione. Detoxification of reactive oxygen species is accompanied by production of glutathione oxidized. Glutathione oxidized can be used for the research of sickle cells and erythrocytes .
Estradiol-d2-1 is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway[1][2][3][4].
Dabrafenib-d9 is the deuterium labeled Dabrafenib. Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively[4].
Ethynyl Estradiol-d4 is the deuterium labeled Ethynyl Estradiol. Ethynyl Estradiol (17α-Ethynylestradiol;Ethynylestradiol) is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills. Ethynyl Estradiol-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Propylparaben-d4 is the deuterium labeled Propylparaben[1]. Propylparaben (Propyl parahydroxybenzoate) is an antimicrobial preservative which can be produced naturally by plants and bacteria. Propylparaben is prevalently used in cosmetics, pharmaceuticals, and foods. Propylparaben disrupts antral follicle growth and steroidogenic function by altering the cell-cycle, apoptosis, and steroidogenesis pathways. Propylparaben also decreases sperm number and motile activity in rats[2][3][4].
Ethyl linoleate-d2 (Linoleic Acid ethyl ester-d2; Mandenol-d2) is the deuterium labeled Ethyl linoleate (HY-W013812). Ethyl linoleate (Linoleic Acid ethyl ester) inhibit the development of atherosclerotic lesions and the expression of inflammatory mediators .
Imatinib-d4 is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity[1][2].
Labetalol-d6 hydrochloride (AH5158-d6 hydrochloride; Sch-15719W-d6) is a deuterium labeled Labetalol (HY-121383). Labetalol is an orally active α1- and β-adrenergic receptors competitive antagonist, which exhibits anti-hypertensive property .
Flibanserin-d4 is a deuterium labeled Flibanserin (BIMT-17). Flibanserin is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM)[1].
Prostaglandin E1-d9 is deuterium labeled Prostaglandin E1.Prostaglandin E1 is a prostanoid receptor ligand, with Kis of 1.1 nM, 2.1 nM, 10 nM, 33 nM and 36 nM for mouse EP3, EP4, EP2, IP and EP1, respectively. Prostaglandin E1 induces vasodilation and inh
Licarbazepine-d4 is the deuterium labeled Licarbazepine (HY-108506). Licarbazepine is a voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects[1][2].
Tamsulosin-d4 (hydrochloride) is deuterium labeled Tamsulosin (hydrochloride). Tamsulosin hydrochloride ((R)-(-)-YM12617) is an inhibitor of α1-adrenergic receptor. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth in animal models[1].
Vildagliptin-d7 is deuterium labeled Vildagliptin. Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity[1].
Ethyl linoleate-d11 (Linoleic Acid ethyl ester-d11) is deuterium labeled Ethyl linoleate. Ethyl linoleate (Linoleic Acid ethyl ester) inhibit the development of atherosclerotic lesions and the expression of inflammatory mediators .
i-Inositol-d6 is the deuterium labeled i-Inositol. i-Inositol is a chemical compound, associated lipids are found in many foods, in particular fruit, especially cantaloupe and oranges.
Thiamine-d4 (hydrochloride) is deuterium labeled Thiamine (hydrochloride). Thiamine hydrochloride (Thiamine chloride hydrochloride) is an essential micronutrient needed as a cofactor for many central metabolic enzymes.
Fosaprepitant-d4 (dimeglumine) is deuterium labeled Fosaprepitant (dimeglumine). Fosaprepitant dimeglumine (MK-0517) is a proagent of Aprepitant (HY-10052). Fosaprepitant dimeglumine is a neurokinin-1 receptor antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV)[1].
Nefazodone-d6 (hydrochloride) is the deuterium labeled Nefazodone hydrochloride. Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity[1][2].
Prostaglandin E2-d9 is the deuterium labeled Prostaglandin E2. Prostaglandin E2 (PGE2) is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation[1][2].
Phenylacetylglutamine-d5 (NSC 203800-d5) is the deuterium labeled Phenylacetylglutamine (HY-W050026). Phenylacetylglutamine is a colonic microbial metabolite from amino acid fermentation .
Deoxycholic acid-d6 is the deuterium labeled Deoxycholic acid. Deoxycholic acid is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.
Panobinostat-d4 is the deuterium labeled Panobinostat. Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities[1][2]. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells[4]. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma[3].
Panobinostat-d4 (hydrochloride) is deuterium labeled Panobinostat. Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities[1][2]. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells[4]. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma[3].
Ethylparaben-d5 (Ethyl parahydroxybenzoate-d5) is deuterium labeled Ethylparaben. Ethylparaben is the ethyl ester of paraben and is used as an antifungal preservative and food additive .
Enrofloxacin-d5 is the deuterium labeled Enrofloxacin. Enrofloxacin (BAY Vp 2674) is an effective antibiotic with an MIC90 of 0.312 μg/mL for Mycoplasma bovis.
Dapsone-d4 is the deuterium labeled Dapsone. Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities[1]. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al[2][3].
Valproic acid-d15 is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches[1][2].
Nefazodone-d6 (dihydrochloride) is deuterium labeled Nefazodone (hydrochloride). Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity[1][2].
Ranolazine-d5 is the deuterium labeled Ranolazine. Ranolazine (CVT 303) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor[3]. Antianginal agent.
Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC50 values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice [3] .
Valproic acid-d4 is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches[1][2].
Tamsulosin-d5 (hydrochloride) is the deuterium labeled Tamsulosin hydrochloride. Tamsulosin hydrochloride ((R)-(-)-YM12617) is an inhibitor of α1-adrenergic receptor. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth in animal models[1].
N-Acetylglycine-d2 (Aceturic acid-d2) is the deuterated labeled N-Acetylglycine (HY-Y0069). N-Acetylglycine (Aceturic acid) is a minor constituent of numerous foods. N-Acetylglycine is a flavor enhancer which elicits Monosodium glutamate (MSG)-like sensory experiencesN-Acetylglycine .
Imatinib-d8 is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity[1][2].
Chloroxylenol-d6 is the deuterium labeled Chloroxylenol. Chloroxylenol is a broad spectrum antimicrobial chemical compound used to control bacteria, algae, fungi and virus.
Adenine-d is the deuterium labeled Adenine. Adenine (6-Aminopurine), a purine, is one of the four nucleobases in the nucleic acid of DNA. Adenine acts as a chemical component of DNA and RNA. Adenine also plays an important role in biochemistry involved in cellular respiration, the form of both ATP and the cofactors (NAD and FAD), and protein synthesis[1][2][3].
Taurocholic acid-d8 (sodium) is deuterium labeled Taurocholic acid (sodium). Taurocholic acid sodium (Sodium taurocholate) has marked bioactive effects such as an inhibitory potential against hepatic artery ligation induced biliary damage by upregulation of VEGF-A expression. Taurocholic acid sodium has immunoregulation effect .
Mycophenolate Mofetil-d4 hydrochloride is deuterated labeled Mycophenolate mofetil hydrochloride (HY-B0199A). Mycophenolate mofetil (RS 61443) hydrochloride is a immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPD) type I/II with IC50s of 39 nM and 27 nM, respectively.
Ebastine-d6 is deuterated labeled Ebastine (HY-B0674). Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research .
Valproic acid-d6 is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches[1][2].
Clopidogrel carboxylic acid-d4 is a deuterated derivative of Clopidogrel carboxylic acid, which is an inactive metabolite of the antiplatelet agent Clopidogrel (HY-15283) in plasma. Clopidogrel carboxylic acid-d4 can be used to further explore the metabolic characteristics of Clopidogrel .
N-Acetylglycine-d5 (Aceturic acid-d5) is the deuterium labeled N-Acetylglycine (HY-Y0069). N-Acetylglycine (Aceturic acid) is a minor constituent of numerous foods. N-Acetylglycine is a flavor enhancer which elicits Monosodium glutamate (MSG)-like sensory experiencesN-Acetylglycine .
Theophylline-d6 is the deuterium labeled Theophylline. Theophylline is a nonselective phosphodiesterase (PDE) inhibitor, adenosine receptor blocker, and histone deacetylase (HDAC) activator.
Enrofloxacin-d5 (hydrochloride) is deuterium labeled Enrofloxacin (monohydrochloride). Enrofloxacin monohydrochloride (BAY Vp 2674 monohydrochloride) is an effective antibiotic with an MIC90 of 0.312 μg/mL for Mycoplasma bovis.
Valproic acid-d4 (sodium) is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
Prostaglandin E2-d4 is the deuterium labeled Prostaglandin E2. Prostaglandin E2 (PGE2) is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation[1][2].
Paroxetine-d4 (hydrochloride) is deuterium labeled Paroxetine (hydrochloride). Paroxetine hydrochloride is a potent selective serotonin-reuptake inhibitor, commonly prescribed as an and has GRK2 inhibitory ability with IC50 of 14 μM. Paroxetine hydrochloride can be used for the research of depressive disorder[1][2][3].
Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice [3].
Dapsone-d8 is a deuterium labeled Dapsone. Dapsone is an orally active and blood-brain penetrant sulfonamide antibiotic with antibacterial, antigenic and anti-inflammatory activities[1]. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone can be used as an anticonvulsant and also in the research of skin and glioblastoma diseases[2][3][4][5].
N-Desmethylolanzapine-d8 hydrochloride (N-Demethylolanzapine-d8 hydrochloride) is the deuterium labeled N-Desmethylolanzapine (HY-W009247). N-Desmethylolanzapine is an antipsychotic drug. The formation of N-Desmethylolanzapine correlates with the level and activity of human liver flavin-containing monooxygenase (FMO3). N-Desmethylolanzapine can be used in the study of antipsychotic drugs .
Propylparaben-d7 (Propyl parahydroxybenzoate-d7) is the deuterium labeled Propylparaben (HY-N2026) . Propylparaben (Propyl parahydroxybenzoate) is an antimicrobial preservative which can be produced naturally by plants and bacteria. Propylparaben is prevalently used in cosmetics, pharmaceuticals, and foods. Propylparaben disrupts antral follicle growth and steroidogenic function by altering the cell-cycle, apoptosis, and steroidogenesis pathways. Propylparaben also decreases sperm number and motile activity in rats [3] .
Sofosbuvir-d6 is the deuterium labeled Sofosbuvir. Sofosbuvir (PSI-7977) is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.
N-Acetyl-S-(3-hydroxypropyl-1-methyl)-L-cysteine-d3 (MethylN-acetyl-S-(3-hydroxypropyl)-L-cysteinate-d3) is the deuterium labeled N-Acetyl-S-(3-hydroxypropyl-1-methyl)-L-cysteine.
Toremifene-d6 is deuterium labeled Toremifene. Toremifene (Z-Toremifene) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively[1][2].
NAD+-d4 is the deuterium-labeled NAD+ (HY-B0445). NAD+-d4 is a coenzyme composed of ribosylnicotinamide 5'-diphosphate coupled to adenosine 5'-phosphate by pyrophosphate linkage.
sn-Glycero-3-phosphocholine-d9 is the deuterium labeled sn-Glycero-3-phosphocholine. sn-Glycero-3-phosphocholine (Choline Alfoscerate) is a precursor in the biosynthesis of brain phospholipids and increases the bioavailability of choline in nervous tissue. sn-Glycero-3-phosphocholine (Choline Alfoscerate) has significant effects on cognitive function with a good safety profile and tolerability, and is effective in the treatment of Alzheimer's disease and dementia[1][2].
Pimelic acid-d4 is the deuterium labeled Pimelic acid[1]. Pimelic acid is the organic compound and its derivatives are involved in the biosynthesis of the amino acid called lysine.
MNI-caged kainate is a photoprotected neuroactive amino acid with the activity to generate large inward currents. MNI-caged kainate can be released at the resting membrane potential of Purkinje cells and generate significant inward currents. The release of MNI-caged kainate results in approximately 40% of the current being generated through AMPA receptor activation. MNI-caged kainate is used to study fast synaptic receptor mechanisms. The photorelease time of MNI-caged kainate is in the sub-microsecond range, making it suitable for investigating the mechanisms of fast synaptic transmission .
Thymidine- 13C10, 15N2 is the 13C and 15N labeled Thymidine[1]. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[2][3][4].
(±)-1,2-Propanediol-d2 is the deuterium labeled (±)-1,2-Propanediol. (±)-1,2-Propanediol (1,2-(RS)-Propanediol) is an aliphatic alcohol and frequently used as an excipient in many agent formulations to increase the solubility and stability of agents .
(±)-1,2-Propanediol-d8 is the deuterium labeled (±)-1,2-Propanediol. (±)-1,2-Propanediol (1,2-(RS)-Propanediol) is an aliphatic alcohol and frequently used as an excipient in many agent formulations to increase the solubility and stability of agents .
Menaquinone-7-d7 is the deuterium labeled Menaquinone-7. Menaquinone-7 (Vitamin K2-7), belongs to a class of K2-vitamin homologs, is originally discovered as the anti-hemorrhagic factors[1]. Menaquinone-7 (Vitamin K2-7) is identified as the most bioactive cofactor for the carboxylation reaction of Gla-proteins [2]. Supplementation with Menaquinone-7 (Vitamin K2-7) is a pharmacological option for activating matrix Gla protein and intervening in the progression of calcific aortic valve stenosis (CAVS)[3].
6-Aminocaproic acid-d6 is deuterium labeled 6-Aminocaproic acid. 6-Aminocaproic acid (EACA), a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders[1][2].
6-Aminocaproic acid-d10 is the deuterium labeled 6-Aminocaproic acid. 6-Aminocaproic acid (EACA), a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders[1][2].
(±)-1,2-Propanediol-d6 is the deuterium labeled (±)-1,2-Propanediol. (±)-1,2-Propanediol (1,2-(RS)-Propanediol) is an aliphatic alcohol and frequently used as an excipient in many agent formulations to increase the solubility and stability of agents .
Coenzyme Q10-d9 is the deuterium labeled Coenzyme Q10. Coenzyme Q10 is an essential cofactor of the electron transport chain and a potent antioxidant agent.
Higenamine-d4-1 (Norcoclaurine-d4-1) hydrochloride is deuterium labeled Higenamine (hydrochloride). Higenamine hydrochloride is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine (Norcoclaurine) can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine hydrochloride protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine hydrochloride can be used to study cancer, inflammation, cardiorenal syndrome and other diseases [3] .
4-Phenylbutyric acid-d2 is the deuterium labeled 4-Phenylbutyric acid[1]. 4-Phenylbutyric acid (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.
Diethyltoluamide-d7 is the deuterium labeled Diethyltoluamide[1]. Diethyltoluamide is the most common active ingredient in insect repellents. It is intended to provide protection against mosquitoes, ticks, fleas, chiggers, leeches, and many other biting insects[2].
Barnidipine-d5 is the deuterium-labeled Barnidipine (HY-107322A). Barnidipine-d5 (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors . Barnidipine-d5 (Mepirodipine) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action .
Estrone-d2-1 is the deuterium labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells[1][2].
L-Ascorbic acid-d2 is the deuterium labeled L-Ascorbic acid. L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a colla
Triacetin-d5 is the deuterium labeled Triacetin. Triacetin is an artificial chemical compound, is the triester of glycerol and acetic acid, and is the second simplest fat after triformin.
Dorzolamide-d5(hydrochloride) (L671152 hydrochloride-d5) is deuterium labeled Dorzolamide (hydrochloride). Dorzolamide (L671152) hydrochloride is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity .
L-5-Hydroxytryptophan-d4 (L-5-HTP-d4; Oxitriptan-d4) is a deuterium labeled L-5-Hydroxytryptophan (HY-B1716). L-5-Hydroxytryptophan (L-5-HTP), a naturally occurring amino acid and a dietary supplement for use as an antidepressant, appetite suppressant, and sleep aid, is the immediate precursor of the neurotransmitter serotonin and a reserpine antagonist . L-5-Hydroxytryptophan (L-5-HTP) is used to treat fibromyalgia, myoclonus, migraine, and cerebellar ataxia [3] .
N-Desmethyl Sildenafil-d8 is the deuterium labeled N-Desmethyl Sildenafil (HY-117605). N-Desmethyl Sildenafil is a major metabolite of Sildenafil. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor[1][2][3].
Levocarnitine propionate-d5 (hydrochloride) is the deuterium labeled Levocarnitine propionate hydrochloride. Levocarnitine propionate hydrochloride (L-Propionylcarnitine chloride; ST-261) is used to treat the deterioration of renal function, congestive heart failure, intermittent claudication, and other diseases.
Retinyl acetate-d4 is the deuterium labeled Retinyl acetate[1]. Retinyl acetate is a synthetic acetate ester form derived from retinol and has potential antineoplastic and chemo preventive activities[2].
Levulinic acid-d5 is the deuterium labeled Levulinic acid[1]. Levulinic acid is a precursor for the synthesis of biofuels, such as ethyl levulinate[2].
rel-Ritonavir-d6 (rel-ABT 538-d6; rel-RTV-d6) is the deuterium labeled Ritonavir (HY-90001). Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.61 μM .
Loratadine-d4-1 (Loratidine-d4-1) is deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators .
Glyceryl Triacetate-d9 is the deuterium labeled Triacetin[1]. Triacetin is an artificial chemical compound, is the triester of glycerol and acetic acid, and is the second simplest fat after triformin.
Folic acid-d4 is the deuterium labeled Folic acid. Folic acid (Vitamin M; Vitamin B9) is a B vitamin; is necessary for the production and maintenance of new cells, for DNA synthesis and RNA synthesis.
2-Methoxyestradiol-d5 is the deuterium labeled 2-Hydroxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa[1][2][3][4][5][6][7].
4-Phenylbutyric acid-d11 is the deuterium labeled 4-Phenylbutyric acid. 4-Phenylbutyric acid (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.
4-Phenylbutyric acid-d5 is the deuterium labeled 4-Phenylbutyric acid[1]. 4-Phenylbutyric acid (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research[2][3][4].
17α-Hydroxyprogesterone-d8 is the deuterium labeled 17α-Hydroxyprogesterone. 17α-Hydroxyprogesterone (17-Hydroxyprogesterone) is an endogenous progestogen as well as chemical intermediate in the biosynthesis of other steroid hormones, including the corticosteroids and the androgens and the estrogens.
Folic acid-d2 (Vitamin B9-d2) is the deuterium labeled Folic acid. Folic acid (Vitamin M; Vitamin B9) is a B vitamin; is necessary for the production and maintenance of new cells, for DNA synthesis and RNA synthesis.
N,N'-Dinitrosopiperazine-d8 is the deuterium labeled N,N'-Dinitrosopiperazine[1]. N,N'-Dinitrosopiperazine (1,4-Dinitrosopiperazine;DNP) is a carcinogen with specificity for nasopharyngeal epithelium and facilitates NPC metastasis. N,N'-Dinitrosopiperazine regulates multiple signaling pathways through protein phosphorylation, including LYRIC at serine 568[2].
Pitavastatin-d4 (hemicalcium) is deuterium labeled Pitavastatin (Calcium). Pitavastatin Calcium (NK-104 hemicalcium) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin Calcium (NK-104 hemicalcium) inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin Calcium is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Anti-cancer activity[1][2][3].
Tetrabenazine-d7 (TBZ-d7-d7) is deuterium labeled Tetrabenazine. Tetrabenazine (Ro 1-9569) is a reversible inhibitor of the vesicular monoamine transporter VMAT2 with the Kd value of 1.34 nM. Tetrabenazine can be used for research on diseases related to hyperactive movement disorders such as Huntington's disease [3] .
Diethyltoluamide-d10 is the deuterium labeled Diethyltoluamide[1]. Diethyltoluamide is the most common active ingredient in insect repellents. It is intended to provide protection against mosquitoes, ticks, fleas, chiggers, leeches, and many other biting insects[2].
Mitotane-d8 is the deuterium labeled Mitotane[1]. Mitotane (2,4′-DDD), an isomer of DDD and derivative of dichlorodiphenyltrichloroethane (DDT), is an antineoplastic agent, can be used to research adrenocortical carcinoma. Mitotane exert its adrenocorticolytic effect at least in part through lipotoxicity induced by intracellular free cholesterol (FC) accumulation. Mitotane can have direct pituitary effects on corticotroph cells. Mitotane can induce CYP3A4 gene expression via steroid and xenobiotic receptor (SXR) activation, and has agent-agent interactions[2][3][4][5].
Coenzyme Q10-d6 is deuterium labeled Coenzyme Q10. Coenzyme Q10 is an essential cofactor of the electron transport chain and a potent antioxidant agent.
Pyridoxine-d2 (hydrochloride) is the deuterium labeled Pyridoxine hydrochloride. Pyridoxine hydrochloride is a pyridine derivative. Pyridoxine (Pyridoxol; Vitamin B6) exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
Ganciclovir-d5 is the deuterium labeled Ganciclovir. Ganciclovir (BW 759), a nucleoside analogue, is an orally active antiviral agent with activity against CMV. Ganciclovir also has activity in vitro against members of the herpes group and some other DNA viruses. Ganciclovir inhibits the in vitro replication of human herpes viruses (HSV 1 and 2, CMV) and adenovirus serotypes 1, 2, 4, 6, 8, 10, 19, 22 and 28. Ganciclovir has an IC50 of 5.2 μM for feline herpesvirus type-1 (FHV-1)[1][2][3].
(R)-Hydroxytolterodine-d14 is deuterated labeled Desfesoterodine (HY-76569). Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) [3]. Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
Dexamethasone-d5-1 is deuterium labeled Dexamethasone. Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
L-Tryptophan- 13C11, 15N2 is the 13C- and 15N-labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3[1].
5'-Guanylic acid- 15N5,d12 (5'-GMP- 15N5,d12 dilithium; 5'-guanosine monophosphate- 15N5,d12) dilithium is deuterium and 15N labeled 5'-Guanylic acid (HY-N5134). 5'-Guanylic acid (5'-GMP) is involved in several metabolic disorders, including the AICA-ribosiduria pathway, adenosine deaminase deficiency, adenine phosphoribosyltransferase deficiency (aprt), and the 2-hydroxyglutric aciduria pathway.
Guanosine- 13C10, 15N5 is the 13C and 15N labeled Guanosine (HY-N0097). Guanosine (DL-Guanosine) is a purine nucleoside comprising guanine attached to a ribose (ribofuranose) ring via a β-N9-glycosidic bond. Guanosine possesses anti-HSV activity .
α-Lipoic Acid-d5 is the deuterium labeled α-Lipoic Acid. α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation[1][2][3]. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells[4].
Secnidazole- 13C2, 15N2 is the 13C2, 15N2 labeled Secnidazole. Secnidazole (RP-14539;PM-185184) is an orally active azole antibiotic with a longer half-life than metronidazole (HY-B0318). Secnidazole is against the vaginosis-associated bacteria and has the potential for bacterial vaginosis research.
p-Anisic acid-d4 is the deuterium labeled p-Anisic acid[1]. p-Anisic acid (4-Methoxybenzoic acid) is one of the isomers of anisic acid, with anti-bacterial and antiseptic properties[2].
Acetyl-L-carnitine-d9 (O-Acetyl-L-carnitine-d9) is deuterium labeled Acetyl-L-carnitine. Acetyl-L-carnitine (O-Acetyl-L-carnitine) is a compound involved in human metabolic research. It has relevant applications in predicting metabolite biomarker changes using the Recon 2 metabolic reconstruction model and integrating and analyzing multiple data types, but its specific activity mechanism is not described in detail based on the existing information [3].
Lapatinib-d4-1 is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1].
D-Sorbitol-d-2 is the deuterium labeled D-Sorbitol. D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and di
Dinoprost-d4 is the deuterium labeled Dinoprost. Dinoprost (Prostaglandin F2α) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost plays a key role in the onset and progression of labour[1][2].
Dinoprost-d9 is the deuterium labeled Dinoprost. Dinoprost (Prostaglandin F2α) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost plays a key role in the onset and progression of labour[1][2].
N-(3-Indolylacetyl)-L-alanine-d4 (Indoleacetylalanine-d4) is the deuterium labeled N-(3-Indolylacetyl)-L-alanine (HY-W141858). N-(3-Indolylacetyl)-L-alanine is an indoleacetylamino acid. N-(3-Indolylacetyl)-L-alanine appears to increase callus growth and reduces the ability of growths to differentiate into shoots of Phalaenopsis orchids .
Levomilnacipran-d10 ((1S,2R)-Milnacipran-d10) hydrochloride is deuterium labeled Levomilnacipran. Levomilnacipran (F2696; (1R,2S)-milnacipran), an enantiomer of milnacipran, is a selective serotonin and norepinephrine (5-HT/NE) reuptake inhibitor. Levomilnacipran also is a human alpha-adrenergic receptor antagonist, with an IC50 of 3.4 μM. (patent WO2013014263A1) .
Atomoxetine-d5 (hydrochloride) is the deuterium labeled Atomoxetine hydrochloride. Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5, 77 and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively)[1][2].
Paquinimod-d5-1 is a deuterated analog of Paquinimod (HY-100442). Paquinimod (ABR 215757) is a specific and orally active inhibitor of S100A8/S100A9. Paquinimod rescues the pneumonia with substantial reduction of viral loads in SARS-CoV-2-infected mice [3].
Norgestimate metabolite norelgestromin-d6 is the deuterium labeled Norgestimate metabolite norelgestromin. Norelgestromin is a metabolite of Norgestimate, which is a progestin or synthetic progestogen. Norgestimate metabolite norelgestromin-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
D-Sorbitol-d2-2 is the deuterium labeled D-Sorbitol. D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and di
D-(+)-Trehalose-d2 is the deuterium labeled D-(+)-Trehalose. D-(+)-Trehalose, isolated from Saccharomyces cerevisiae, can be used as a food ingredient and pharmaceutical excipi[1][2].
D-Sorbitol-d2-1 is the deuterium labeled D-Sorbitol. D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and di
(S)-Timolol-d9 (maleate) is deuterium labeled (S)-Timolol (Maleate). (S)-Timolol Maleate (L-714,465 Maleate) is a non-cardioselective hydrophilic β-adrenoceptor blocker. (S)-Timolol Maleate is widely used as standard medication for intraocular pressure (glaucoma) by preventing the production of aqueous humor. (S)-Timolol Maleate can be used for hypertension, angina pectoris and myocardial infarction[1][2][3].
L-Norleucine-d9 is the deuterium labeled L-Norleucine. L-Norleucine ((S)-2-Aminohexanoic acid) is an isomer of leucine, specifically affects protein synthesis in skeletal muscle, and has antivirus activity.
Meta-Fexofenadine-d6 is the deuterium labeled meta-Fexofenadine. meta-Fexofenadine (meta-MDL-16455) is an impurity of Fexofenadine[1]. Fexofenadine, a H1R antagonist, is an anti-allergic agent used in seasonal allergic rhinitis and chronic idiopathic urticarial[2].
Olaparib-d4-1 (AZD2281-d4-1) is the deuterium labeled Olaparib (HY-10162). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator [3] .
β-Nicotinamide mononucleotide-d4 is the deuterium labeled β-Nicotinamide mononucleotide. β-nicotinamide mononucleotide (β-NM) is a product of the nicotinamide phosphoribosyltransferase (NAMPT) reaction and a key NAD+ intermediate. The pharmacological activities of β-nicotinamide mononucleotide include its role in cellular biochemical functions, cardioprotection, diabetes, Alzheimer's disease, and complications associated with obesity[1].
Safinamide-d4-1 is deuterium labeled Safinamide. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM)[1]. Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al[2][3].
Alfacalcidol-d7 is the deuterium labeled Alfacalcidol. Alfacalcidol (1-hydroxycholecalciferol) is a vitamin D active metabolites, acts as a non-selective VDR activator medication, and widely be used in the management of osteoporosis[1][2][3][4].
D-(+)-Trehalose-d14 is the deuterium labeled D-(+)-Trehalose. D-(+)-Trehalose, isolated from Saccharomyces cerevisiae, can be used as a food ingredient and pharmaceutical excipi[1][2].
Escitalopram-d4 (oxalate) is deuterium labeled Escitalopram (oxalate). Escitalopram ((S)-Citalopram) oxalate, the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram oxalate has ∼30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram oxalate is an antidepressant for the research of major depression[1][2].
Cortisone-d2 is the deuterium labeled Cortisone. Cortisone (17-Hydroxy-11-dehydrocorticosterone), an oxidized metabolite of Cortisol (a Glucocorticoid). Cortisone acts as an immunosuppressant and anti-inflammatory agent. Cortisone can partially intervene in binding of Glucocorticoid to Glucocorticoid-receptor at high concentrations[1][3][4][5].
Palmitoylethanolamide-d5 (Palmidol-d5, PEA-15,15,16,16,16-d5) is deuterium labeled Palmitoylethanolamide. Palmitoylethanolamide (Palmidrol) is an active endogenous compound which can used for preventing virus infection of the respiratory tract .
Chlorambucil-d8-1 is the deuterium labeled Chlorambucil. Chlorambucil (CB-1348), an orally active antineoplastic agent, is a bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease[1][2][3][4].
13-Methyltetradecanoic acid-d6 is a deuterated labeled 13-Methyltetradecanoic acid . 13-Methyltetradecanoic acid (13-MTD), a saturated branched-chain fatty acid with potent anticancer effects. 13-Methyltetradecanoic acid induces apoptosis in many types of human cancer cells [3].
C6 Ceramide-d11 is deuterated labeled C6 Ceramide (HY-19542). C6-ceramide, a ceramide pathway activator, shows activity against a variety of cancer cell lines. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects .
Chlophedianol- 13C6 is the 13C labeled Chlophedianol (HY-A0161). Chlophedianol is an orally active and potent antitussive agent. Chlophedianol can be used for the research of acute cough due to upper respiratory tract infections (URIs)[1][2][3].
2-Deoxy-D-glucose-d is the deuterium labeled 2-Deoxy-D-glucose. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase[1][2].
Clascoterone-d5 (Cortexolone 17 alpha-propionate-d5) is the deuterated analog of Clascoterone. Clascoterone is a topical and peripheral androgen antagonist [3].
Clascoterone-d6 (Cortexolone 17 alpha-propionate-d6) is deuterium labeled Clascoterone. Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist .
Maribavir-d6 TFA (1263W94-d6 TFA; BW1263W94-d6 TFA; GW257406X-d6 TFA) is a deuterium labeled Maribavir (HY-16305). Maribavir is an orally active antiviral agent for cytomegalovirus (CMV) through inhibition of protein kinase UL97 and the following CMV DNA replication .
L-Asparagine- 15N2 (monohydrate) is the 15N-labeled L-Asparagine. L-Asparagine ((-)-Asparagine) is a non-essential amino acid that is involved in the metabolic control of cell functions in nerve and brain tissue.
L-Asparagine- 13C4 (monohydrate) is the 13C-labeled L-Asparagine. L-Asparagine ((-)-Asparagine) is a non-essential amino acid that is involved in the metabolic control of cell functions in nerve and brain tissue.
Adenine- 13C5,15C5 (6-Aminopurine- 13C5,15C5; Vitamin B4- 13C5,15C5) is 13C-labeled Adenine (HY-B0152). Adenine (6-Aminopurine), a purine, is one of the four nucleobases in the nucleic acid of DNA. Adenine acts as a chemical component of DNA and RNA. Adenine also plays an important role in biochemistry involved in cellular respiration, the form of both ATP and the cofactors (NAD and FAD), and protein synthesis.
Riboflavin- 13C4, 15N2is the 13C-labeled and 15N-labeled Riboflavin. Riboflavin is an easily absorbed micronutrient with a key role in maintaining health in humans and other animals.
L-Arginine- 13C6, 15N4,d7 (hydrochloride) is the deuterium, 13C-, and 15-labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
D-Glucose- 13C2 is the 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
5-Azacytidine- 15N4 is 13C and 15N labeled 5-Azacytidine. 5-Azacytidine (Azacitidine; 5-AzaC; Ladakamycin) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation. 5-Azacytidine is incorporated into DNA to covalently trap DNA methyltransferases and contributes to reverse epigenetic changes. 5-Azacytidine induces cell autophagy[3] .
Epeleuton-d5 (15(S)-HEPE-d5ethyl ester) is deuterium labeled Epeleuton. Epeleuton is a second-generation synthetic N-3 fatty acid derivative with activity in patients with non-alcoholic fatty liver disease, although it did not reach the primary endpoints of alanine aminotransferase and liver stiffness, but it can significantly reduce triglycerides, glycated hemoglobin, plasma glucose and inflammatory markers .
Acetaminophen-13C6 (Paracetamol-13C6) is the 13C-labeled Acetaminophen. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent [3]. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor .
Aliskiren-d6 (hemifumarate) is a deuterium labeled Aliskiren hemifumarate. Aliskiren hemifumarate is a direct and orally active renin inhibitor with an IC50 of 1.5 nM[1][2].
Efavirenz- 13C6 is the 13C-labeled Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture[1].
α-Hydroxyglutaric acid-d4 (disodium) is the deuterium labeled α-Hydroxyglutaric acid disodium[1]. α-Hydroxyglutaric acid (2-Hydroxyglutarate) disodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid disodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases[2].
D-Glucose- 13C6 is a stable isotope-labeled counterpart of D-glucose (HY-B0389). D-Glucose- 13C6 can be used as a metabolic tracer to trace glucose-related synthetic catabolism or as synthesis ingredient, minimal media reagent, and internal standard [3].
DCVC- 13C3, 15N is 15N and 13C labeled DCVC. DCVC (S-[(1E)-1,2-Dichloroethenyl]-L-cysteine) is a bioactive metabolite of trichloroethylene (TCE). DCVC inhibits pathogen-stimulated pro-inflammatory cytokines IL-1β, IL-8, and TNF-α release from tissue cultures .
Tazarotene-13C2,d2 (AGN 190168-13C2,d2) is the 13C and deuterium labeled isotope of Tazarotene (HY-15388). Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris. Tazarotene is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups .
Acotiamide-d6 is a deuterium labeled Acotiamide. Acotiamide is an orally active and first-in-class gastroprokinetic agent for the treatment of functional dyspepsia[1][2].
Nitroxoline-d4 is the deuterium labeled Nitroxoline. Nitroxoline is an antibiotic that has proven to be very effective at combating biofilm infections. Nitroxoline functions by chelating Fe2+ and Zn2+ ions from the biofilm matrix[1][2].
p,p'-DDE-d8 is the deuterium labeled p,p'-DDE[1]. p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent androgen receptor antagonist, with an IC50 of 5 μM and a Ki of 3.5 μM[2].
Valproic acid-d4-1 is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches[1][2].
Rufinamide-d2 (CGP 33101-d2) is the deuterium labeled Rufinamide. Rufinamide (E 2080) is a new antiepileptic agent that differs structurally from other antiepileptic drugs and is approved as adjunctive therapy for Lennox-Gastaut syndrome (LGS).
(Rac)-5-Hydroxymethyl Tolterodine-d14 is the deuterium labeled (Rac)-5-Hydroxymethyl Tolterodine. (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research[1].
Lipoic acid-d4 ((R)-(+)-α-Lipoic acid-d4) is deuterium labeled Lipoic acid. Lipoic acid ((R)-(+)-α-Lipoic acid) is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. (R)-(+)-α-Lipoic acid is more effective than racemic Lipoic acid .
Enrofloxacin-d5 (hydriodide) is the deuterium labeled Enrofloxacin (monohydrochloride). Enrofloxacin monohydrochloride (BAY Vp 2674 monohydrochloride) is an effective antibiotic with an MIC90 of 0.312 μg/mL for Mycoplasma bovis.
Flibanserin-d4-1 is deuterium labeled Flibanserin. Flibanserin (BIMT-17) is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM). Flibanserin binds to dopamine D4 receptors (4-24 nM), and has negligible affinity for a variety of other neurotransmitter receptors and ion channels. Flibanserin is efficacious in treating hypoactive sexual desire disorder (HSDD)[1][2].
Uridine triphosphate-d13 (UTP-d13 dilithium; Uridine 5'-triphosphate-d13) dilithium is deuterium labeled Uridine triphosphate (HY-107372). Uridine triphosphate (UTP;Uridine 5'-triphosphate) is a nucleotide that regulates the functions of the pancreas in endocrine and exocrine secretion, proliferation, channels, transporters, and intracellular signaling under normal and disease states.
Treprostinil- 13C2,d is the 13C- and deuterium labeled Treprostinil. Treprostinil (UT-15) is a potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively.
rel-Paroxetine-d4 (hydrochloride) is an isotope-labeled Paroxetine hydrochloride (HY-B0492). Paroxetine hydrochloride is an orally active and selective serotonin-reuptake inhibitor, commonly prescribed as an GRK2 inhibitor with IC50 of 14 μM. Paroxetine hydrochloride can be used for the research of depressive disorder[1][2][3][4].
N-Decyl-N,N-dimethyldecan-1-aminium-d6 (chloride) is a deuterated labeled N-Decyl-N,N-dimethyldecan-1-aminium (chloride) . N-Decyl-N,N-dimethyldecan-1-aminium chloride (Didecyldimethylammonium chloride) is a dialkyl-quaternary ammonium compound that is used in numerous products for its bactericidal, virucidal and fungicidal properties .
N-Desmethyl imatinib-d4 is the deuterium-labeled N-Desmethyl imatinib (HY-G0017). N-Desmethyl imatinib-d4 (Norimatinib) is a metabolite of Imatinib (HY-15463). Imatinib is a multi-target inhibitor of v-Abl, c-Kit and PDGFR .
Indinavir-d6 is the deuterium labeled Indinavir. Indinavir (MK-639; L735524) is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability.
Bzo-poxizid-d9 (5C-MDA-19-d9, Petyl MDA-19-d9) is deuterium labeled Bzo-poxizid. Bzo-poxizid is a synthetic cannabinoid that is a psychoactive substance .
O-Desmethyl Midostaurin-d5 is a deuterium labeled O-Desmethyl PKC412. O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) is the active metabolite of Midostaurin (HY-10230) via cytochrome P450 liver enzyme metabolism[1].
Cinnamic acid-d6 is the deuterium labeled Cinnamic acid. Cinnamic acid has potential use in cancer intervention, with IC50s of 1-4.5 mM in glioblastoma, melanoma, prostate and lung carcinoma cells.
Tamoxifen-d5 is a deuterium labeled Tamoxifen. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM). Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity .
rac Timolol-d5 (maleate) is a labelled racemic (S)-Timolol maleate. (S)-Timolol Maleate (L-714,465 Maleate) is a non-cardioselective hydrophilic β-adrenoceptor blocker. (S)-Timolol Maleate is widely used as standard medication for intraocular pressure (glaucoma) by preventing the production of aqueous humor. (S)-Timolol Maleate can be used for hypertension, angina pectoris and myocardial infarction[1][2][3].
Licarbazepine-d4-1 is deuterium labeled Licarbazepine. Licarbazepine (BIA 2-005; GP 47779) is a voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects[1].
Estradiol- 13C6 is the 13C-labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway[1][2][3].
Estradiol- 13C2 is the 13C-labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway[1][2][3].
5-Aminosalicylic acid- 13C6 is the 13C labeled 5-Aminosalicylic Acid[1]. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB[2][3][4].
Adenosine monophosphate- 13C10, 15N5,d12 (AMP- 13C10, 15N5,d12) dilithium is 13C and 15N-labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction [3].
Erlotinib- 13C6 (hydrochloride) is the 13C labeled Erlotinib Hydrochloride[1]. Erlotinib Hydrochloride (CP-358774 Hydrochloride) inhibits purified EGFR kinase with an IC50 of 2 nM[2]. Erlotinib-13C6 (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
5-Aminosalicylic acid-13C6 hydrochloride?(Mesalamine-13C6 hydrochloride; 5-ASA-13C6 hydrochloride; Mesalazine-13C6 hydrochloride) is the 13C labeled 5-Aminosalicylic Acidhydrochloride. 5-Aminosalicylic acid-13C6 hydrochloride?acts as a PPARγ agonist, and also inhibits p21-activated kinase 1 (PAK1) and NF-κB [3].
Hydrocortisone-d7 is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex[1].
Dyclonine-d9 (hydrochloride) is deuterium labeled Dyclonine (hydrochloride). Dyclonine hydrochloride (Dyclocaine hydrochloride) is an effective component of Runhou tablets. Dyclonine hydrochloride has significant bactericidal and fungicidal activity[1][2].
Amodiaquine-d10 hydrochloride is deuterated labeled Amodiaquine (HY-B1322A). Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect [3] .
Sulfanilamide-d4 is the deuterium labeled Sulfanilamide. Sulfanilamide is a competitive inhibitor for bacterial enzyme dihydropteroate synthetase with IC50 of 320 μM.
Phenformin-d5 (hydrochloride) is the deuterium labeled Phenformin hydrochloride. Phenformin hydrochloride is an anti-diabetic agent from the biguanide class, can activate AMPK activity[1][2].
Ramiprilat-d4 hydrochloride is deuterated labeled Ramiprilat (HY-A0115). Ramiprilat (HOE 498 diacid), an active metabolite of Ramipril, is a potent and orally active angiotensin converting enzyme (ACE) inhibitor with a Ki value of 7 pM. Ramiprilat can be used for high blood pressure and heart failure research .
Sulfacetamide-d4 (Sulphacetamide-d4) is the deuterium labeled Sulfacetamide (HY-N7123). Sulfacetamide (Sulphacetamide) is a sulfonamide antibiotic that can be used for the study of ocular infections. Sulfacetamide has antifungal and antibacterial activities .
Fenoverine-d8 is the deuterium labeled Fenoverine[1]. Fenoverine (Spasmopriv) is an antispasmodic agent and inhibits calcium channel currents[2]. Fenoverine induces rhabdomyolysis[3].
Dipivefrin-d6 (hydrochloride) is deuterium labeled Dipivefrin (hydrochloride). Dipivefrin hydrochloride (Dipivefrine hydrochloride) is an antiglaucoma proagent that is hydrolyzed to the active compound, epinephrine, by esterases in the cornea[1][2].
Diphenylmethane-d2 (Benzylphenyl-d2) is the deuterium labeled Diphenylmethane (HY-W008814). Diphenylmethane (Benzylphenyl) is a kind of biological materials or organic compounds that are widely used in life science research .
Ethambutol-d4 dihydrochloride is deuterated labeled Ethambutol dihydrochloride (HY-B0535A). Ethambutol dihydrochloride is an antimycobacterial compound that prevents cell wall formation by inhibiting arabinosyltransferase activity.
Levofloxacin-d8 is the deuterium labeled Levofloxacin. Levofloxacin, a synthetic fluoroquinolone, is an antibacterial agent that inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication.
Deltamethrin-d5 is the deuterium labeled Deltamethrin. Deltamethrin (Decamethrin), a neurotoxic pyrethroid insecticide, produces a reversible sequence of motor symptoms in rats involving hind limb rigidity and choreoathetosis[1][2].
Sulfadimethoxine-d4 is a deuterium labeled Sulfadimethoxine (Sulphadimethoxine). Sulfadimethoxine is a sulfonamide antibiotic used to treat many infections including treatment of respiratory, urinary tract, enteric, and soft tissue infections[1].
Temephos-d12 is the deuterium labeled Temephos[1]. Temefos is an organophosphate larvicide, used to treat water infested with disease-carrying insects including mosquitoes, midges, and black fly larvae. Temefos affects the central nervous system through inhibition of cholinesterase, results in death before reaching the adult stage[2][3].
Pyridoxine-d5 (Pyridoxol-d5) is a deuterium labeled Pyridoxine (HY-B1328). Pyridoxine (Pyridoxol) is a pyridine derivative. Pyridoxine exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
Lidocaine-d6 (hydrochloride) is deuterium labeled Lidocaine (hydrochloride). Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative and a agent to treat ventricular arrhythmia and an effective tumor-inhibitor[2].
Salcaprozate-d4 (sodium) is a deuterated labeled Salcaprozate (sodium) . Salcaprozate sodium (SNAC), an oral absorption promoter, and has the potential as a delivery agent for oral forms of heparin and insulin. Salcaprozate sodium could increase passive transcellular permeation across small intestinal epithelia based on increased lipophilicity arising from non-covalent macromolecule complexation [3].
Salvigenin-d9 is the deuterium labeled Salvigenin. Salvigenin is a natural polyphenolic compound, with neuroprotective effect. Salvigenin has antitumor cytotoxic and immunomodulatory properties[1][2].
Isoprenaline-d7 (hydrochloride) is a deuterated labeled Isoprenaline (hydrochloride) . Isoprenaline (Isoproterenol) hydrochloride is a non-selective, orally active β-adrenergic receptor agonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma [3] .
Hexadecanal-d5 (Palmitaldehyde-d5) is deuterium labeled Hexadecanal. Hexadecanal (Palmitaldehyde) , a volatile long-chain aliphatic aldehyde, is emitted from human feces, skin, and breath. The receptor for hexadecanal(OR37B) is highly conserved across mammals. Hexadecanal may exert its effects by modulating functional connectivity between the brain substrates of social appraisal and the brain substrates of aggressive execution. Also, Hexadecanal is confirmed to be highly deterrent to the ant Lasius niger. Hexadecanal is promising for the research of startle responses and aggression [3]
Indomethacin-d4 is a deuterium labeled Indomethacin. Indomethacin is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells[1]. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes[2].
Meclizine-d8 is a deuterium labeled Meclizine. Meclizine is a histamine H1 receptor antagonist and has the potential to treat nausea and motion sickness. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR[1][2][3].
Imperatorin-d6 (Ammidin-d6) is the deuterium labeled Imperatorin. Imperatorin is a BChE inhibitor and HIV-1 replication inhibitor. Imperatorin shows mild activity against Gram-negative bacteria .
Dicyclomine-d4 is the deuterium labeled Dicyclomine[1]. Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively[2]. Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo[3].
Drospirenone-d4 is the deuterium labeled Drospirenone. Drospirenone (Dihydrospirorenone) is a synthetic progestin that is an analog to spironolactone[1][2].
Ethambutol-d10 is the deuterium labeled Ethambutol. Ethambutol is a bacteriostatic antimycobacterial agent, which obstructs the formation of cell wall by inhibiting arabinosyl transferases.
Hydrocortisone-d2 is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex[1][2].
Lumefantrine-d9 is the deuterium labeled Lumefantrine. Lumefantrine is an antimalarial drug, used in combination with Artemether. The artemether-lumefantrine (AL) as the first- and second-line anti-malarial drugs.
Anandamide-d11 is deuterium labeled Anandamide. Anandamide is an immune modulator in the central nervous system acts via not only cannabinoid receptors (CB1 and CB2) but also other targets (e.g., GPR18/GPR55)[1][2].
Sulfachloropyridazine-d4 is the deuterium labeled Sulfachloropyridazine. Sulfachloropyridazine is a broad spectrum sulfonamide used against both Gram-positive and Gram-negative aerobic bacteria[1].
Sulfisomidin-d4 (Sulfaisodimidine-d4) is deuterium labeled Sulfisomidin. Sulfisomidin (Sulfaisodimidine) is an orally active short-acting sulfonamide antibacterial. Sulfisomidin can be used for the research of lower urinary tract infections .
Cletoquine-d4 is deuterium labeled Cletoquine. Cletoquine (Desethylhydroxychloroquine) is a major active metabolite of Hydroxychloroquine. Cletoquine is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune diseases treatment[1][2].
Nefopam-d4 (hydrochloride) is deuterium labeled Nefopam (hydrochloride). Nefopam hydrochloride (Fenazoxine hydrochloride) is a centrally-acting but non-opioid analgesic drug, for the relief of moderate to severe pain. Nefopam hydrochloride targets β-catenin protein level in mesenchymal cells in-vitro and in-vivo[1][2].
Acetylcholine-d9 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs)[1][2]. Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro[5].
Ethambutol-d4 is the deuterium labeled Ethambutol. Ethambutol is a bacteriostatic antimycobacterial agent, which obstructs the formation of cell wall by inhibiting arabinosyl transferases.
Dibenzylamine-d4 (Bisbenzylamine-d4) is the deuterium labeled Dibenzylamine (HY-Y1067). Dibenzylamine is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Alimemazine-d6 hydrochloride (Trimeprazine-d6 hydrochloride) is the deuterium labeled Alimemazine (HY-12752). Alimemazine is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist.Alimemazine (Trimeprazine) is also acts as a partial agonist against the histamine H1 receptor (H1R) and other GPCRs. Alimemazine displays antiserotonin, antispasmodic, and antiemetic properties .
Prednisone-d7 (Dehydrocortisone-d7) is deuterium labeled Prednisone. Prednisone (Adasone) is a corticosteroid agent with anti-inflammatory and immunosuppressive effects that can be used to study diseases related to systemic lupus erythematosus .
Pramocaine-d9 (hydrochloride) is deuterium labeled Pramocaine (hydrochloride). Pramocaine hydrochloride decreases the permeability of neuronal membranes to sodium ions, blocking both initiation and conduction of nerve impulses.
Hydrochlorothiazid-d2 is the deuterium labeled Hydrochlorothiazide. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect[1][2][3].
Ethotoin-d5 is the deuterium labeled Ethotoin[1]. Ethotoin (Peganone) is an orally active anticonvulsant agent used in epilepsy research, Ethotoin is a hydantoin, similar to phenytoin[2].
Acenaphthylene-d8 is the deuterium labeled Acenaphthylene[1]. Acenaphthylene is a polycyclic aromatic hydrocarbon (PAH). PAHs are derived naturally from coal and tar deposits, and produced by incomplete combustion of organic matter[2].
Hydrocortisone-d4 is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex[1].
Racecadotril-d5 is the deuterium labeled Racecadotril. Racecadotril (Acetorphan) is a neutral endopeptidase (NEP) inhibitor. Racecadotril and its active metabolite Thiorphan inhibits purified NEP activity from mouse brain with Kis of 4500 and 6.1 nM, , respectively. Antidiarrheal agent[1].
Torsemide-d7 is the deuterium labeled Torsemide. Torsemide (Torasemide) is an orally active loop diuretic. Torsemide has anti-aldosterone and vasodilatory effects. Torsemide also can be used for the research of heart failure, renal disease and hepatic cirrhosis[1][1][3].
Piperacillin-d5 is deuterium labeled Piperacillin. Piperacillin is kind of semisynthetic penicillins. Piperacillin has a broad spectrum of activity against Gram-positive and Gram-negative aerobic and anaerobic bacteria. Piperacillin has shown greater activity against β-lactamase-producing organisms than the other penicillins[1].
Sulfadoxine-d4 is the deuterium labeled Sulfadoxine. Sulfadoxine(Sulphadoxine) is a long acting sulfonamide that is used, usually in combination with other agents, for respiratory, urinary tract and malarial infections. Sulfadoxine inhibits HIV replication in peripheral blood mononuclear cells.
Bestatin-d7 (hydrochloride) is deuterium labeled Bestatin (hydrochloride). Bestatin hydrochloride is an inhibitor of CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase, used for cancer research.
Psychosine-d7 is deuterium labeled Psychosine. Psychosine, a substrate of the galactocerebrosidase (GALC) enzyme, is a potential biomarker for Krabbe disease. Psychosine is a highly cytotoxic lipid, capable of inducing cell death in a wide variety of cell
Atovaquone-d5 is the deuterium labeled Atovaquone. Atovaquone (Atavaquone) is a potent, selective and orally active inhibitor of the parasite’s mitochondrial cytochrome bc1 complex. Atovaquone is against human and P. falciparum cytochrome bc1 activity with IC50 values of 460 nM and 2.0 nM, respectively. Atovaquone is an antimalarial agent and has the potential for the investigation of neumocystis pneumonia, toxoplasmosis, malaria, and babesia[1][2].
Dibucaine-d9 is the deuterium labeled Dibucaine(HY-B0552).Dibucaine (Cinchocaine) is a sodium channel inhibitor. Dibucaine is a potent SChE inhibitor .
Pitolisant-d10 (Tiprolisant-d10) is deuterium labeled Pitolisant. Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM) .
Prednisone-d8 is the deuterium labeled Prednisone. Prednisone (Adasone) is a synthetic corticosteroid agent that is particularly effective as an immunosuppressant compound.
THIP-d4 (Gaboxadol-d4) is the deuterium labeled THIP (HY-10232). THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 μM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders [3].
Phenacetin-d5 is the deuterium labeled Phenacetin. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats[1][2][3].
Ditiocarb-d10 sodium (Sodium diethyldithiocarbamate-d10) is the deuterium labeled Ditiocarb sodium. Ditiocarb sodium is a copper reagent. The reaction with Cu 2+ solution resulted in the formation of a complex, which increased the copper displacement precipitation rate. Ditiocarb sodium can reduce HIV infection and can be used in adjuvant immune research of high-risk breast cancer [3].
Anandamide-d8 is a deuterated labeled Anandamide . Anandamide is an endocannabinoid. Anandamide modulates both neuronal and immune functions through two protein-coupled cannabinoid receptors (CB1 and CB2). Anandamide can activate numerous other receptors like PPARS, TRPV1, and GPR18/GPR55. Anandamide also has potential anti-fungal and anti-inflammatory activities. Anandamide can be used for the research of Alzheimer’s disease (AD) and ulcerative colitis [3] .
Psychosine-d5 is deuterium labeled Psychosine. Psychosine, a substrate of the galactocerebrosidase (GALC) enzyme, is a potential biomarker for Krabbe disease. Psychosine is a highly cytotoxic lipid, capable of inducing cell death in a wide variety of cell.
Desmethylcitalopram-d4 hydrochloride is deuterated labeled Desmethylcitalopram hydrochloride (HY-113739). Desmethylcitalopram (DCIT) hydrochloride is the active metabolite of Citalopram (HY-121203). Desmethylcitalopram has antidepressant effects. Desmethylcitalopram also inhibits cytochrome P450-2D6, -2C19 with IC50s of 39.5 and 53.5 μM .
Bisphenol AF-d4 is the isotope labelled analog of Bisphenol AF (HY-W013782). Bisphenol AF is a full agonist for the estrogen receptor. Bisphenol AF acts as an endocrine-disrupting chemical (EDC), activating estrogen through the estrogen receptor Era. Bisphenol AF-d4 can be used for the research of endocrinology and cancer .
Colfosceril miristate-d63 (DMPC-d63) is deuterium labeled Colfosceril miristate. Colfosceril miristate a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
Deoxycytidine triphosphate-d14 (dCTP-d14 dilithium; 2′-Deoxycytidine-5′-triphosphate-d14) dilithium is deuterium labeled Deoxycytidine triphosphate (HY-101400). Deoxycytidine triphosphate (dCTP) is a nucleoside triphosphate that can be used for DNA synthesis. Deoxycytidine triphosphate has many applications, such as real-time PCR, cDNA synthesis, and DNA sequencing.
Ezetimibe phenoxy glucuronide-d4 is the deuterium labeled Ezetimibe phenoxy glucuronide. Ezetimibe phenoxy glucuronide is the active metabolite of Ezetimibe. Antihyperlipoproteinemic activity[1]. Ezetimibe is a potent cholesterol absorption inhibitor[2].
VcMMAE-d8 is an isotope of VcMMAE (HY-15575). VcMMAE-d8 is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc) .
p,p'-DDD-d8 is the deuterium labeled p,p'-DDD[1]. p,p'-DDD (4,4’-DDD) is an organochlorine insecticide, a major metabolite of p,p'-DDT. p,p'-DDD is an agonist at estrogen receptor α(ERα) and ERβ. p,p'-DDD increases DNA damage, apoptosis and necrosis in peripheral blood. p,p'-DDD stimulates cell proliferation in SKBR3 cells. p,p'-DDD activates the AP-1 transcription factor. p,p'-DDD decreases sleep times of barbiturates and steroids in rats [3] .
D-Fructose- 13C6,d7 is the deuterium and 13C labeled D-Fructose. D-Fructose (D(-)-Fructose) is a naturally occurring monosaccharide found in many plants[1].
Menaquinone-4-d7 (Vitamin K2(MK-4)-d7) is the deuterium labeled Menaquinone-4. Menaquinone-4 is a vitamin K, used as a hemostatic agent, and also a adjunctive therapy for the pain of osteoporosis.
5,6-Epoxyeicosatrienoic acid-d11 (5,6-EET-d11) is deuterium labeled 5,6-Epoxyeicosatrienoic acid. 5,6-Epoxyeicosatrienoic acid (5,6-EET; (±)5,6-EpETrE) is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5,6-Epoxyeicosatrienoic acid degrades into 5,6-DiHET and 5,6-δ-lactone, which can be converted to 5,6-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5,6-Epoxyeicosatrienoic acid has been implicated in the mobilization of calcium and hormone secretion. 5,6-Epoxyeicosatrienoic acid is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50=0.54 μM), and Cav3. and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2, as measured by oxygen consumption and product formation assays when used at a concentration of 50 μM. (±)5,6-Epoxyeicosatrienoic acid is provided as a mixture of the free acid and lactone .
Oleic acid-d9 is deuterium labeled Oleic acid (HY-N1446). Oleic acid is an abundant monounsaturated fatty acid. Oleic acid is a Na+/K+ ATPase activato .
α-Vitamin E-d11 ((+)-α-Tocopherol-d11) is the deuterium labeled α-Vitamin E (HY-N0683). α-Vitamin E ((+)-α-Tocopherol), a naturally occurring vitamin E form, is a potent antioxidant .
Colfosceril miristate-d9 (DMPC-d9) is deuterium labeled Colfosceril miristate. Colfosceril miristate a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
Mono-(2-ethylhexyl) phthalate-d4 is a deuterium labeled Mono-(2-ethylhexyl) phthalate (HY-W018392). Mono-(2-ethylhexyl) phthalate (MEHP) is a major bioactive metabolite of diethylhexyl phthalate (DEHP). Mono-(2-ethylhexyl) phthalate can promote fatty acid synthesis in hepatocytes by regulating the expression of relevant genes and proteins, contributing to non-alcoholic fatty liver disease (NAFLD) .
Leukotriene B4-d4 is the deuterium labeled Leukotriene B4. Leukotriene B4 (LTB4) is known as one of the most potent chemoattractants and activators of leukocytes and is involved in inflammatory diseases. Leukotriene B4 is also an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1][2][3].
1,2-Dimyristoyl-sn-glycero-3-phosphocholine-d67 is deuterium labeled 1,2-Dimyristoyl-sn-glycero-3-phosphocholine. 1,2-Dimyristoyl-sn-glycero-3-phosphocholine (DMPC) is a synthetic phospholipid used in liposomes. 1,2-Dimyristoyl-sn-glycero-3-phosphocholine
Colfosceril miristate-d13 (DMPC-d13) is deuterium labeled Colfosceril miristate. Colfosceril miristate a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
Colfosceril miristate-d58 (DMPC-d58) is deuterium labeled Colfosceril miristate. Colfosceril miristate a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
Tazarotenic acid-13C2,d2 (AGN 190299-13C2,d2) is the 13C and deuterium labeled isotope of Tazarotenic acid (HY-101108). Tazarotenic acid is the metabolite of Tazarotene. Tazarotenic acid binding to retinoic acid receptors (RARs) is the probable molecular target of retinoid action. Tazarotenic acid has the potential for the research of warty dyskeratoma [3].
Colfosceril miristate-d4 (DMPC-d4) is deuterium labeled Colfosceril miristate. Colfosceril miristate is a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
Docosahexaenoic acid-d5methyl ester is the deuterium labeled Docosahexaenoic Acid methyl ester. Docosahexaenoic Acid methyl ester is a methylated docosahexaenoic acid analog which can be intercalated into membrane phospholipids without being oxidized or hydrolyzed[1][2].
Oleic acid-d2) is the deuterium labeled Oleic acid (HY-N1446). Oleic acid (9-cis-Octadecenoic acid) is an abundant monounsaturated fatty acid ]. Oleic acid is a Na+/K+ ATPase activator .
Carvedilol metabolite 4-Hydroxyphenyl Carvedilol-d4 is deuterated labeled Carvedilol metabolite 4-Hydroxyphenyl Carvedilol (HY-12767). 4-Hydroxyphenyl Carvedilol is a metabolite of Carvedilol.
L-Arginine- 15N4,d7 (hydrochloride) is the deuterium and 15N-labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
Urea- 15N2 is the 15N-labeled Urea. Urea is a powerful protein denaturant via both direct and indirect mechanisms[1]. A potent emollient and keratolytic agent[2]. Used as a diuretic agent. Blood urea nitrogen (BUN) has been utilized to evaluate renal function[3]. Widely used in fertilizers as a source of nitrogen and is an important raw material for the chemical industry.
Thymidine- 15N2 is the 15N labeled Thymidine[1]. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[2][3][4].
Oleic acid-d17 is the deuterium labeled Oleic acid (HY-N1446). Oleic acid (9-cis-Octadecenoic acid) is an abundant monounsaturated fatty acid . Oleic acid is a Na+/K+ ATPase activator .
Tamsulosin-d4 ((R)-(-)-YM12617 (free base)-d4) is deuterium labeled Tamsulosin. Tamsulosin ((R)-(-)-YM12617 free base) is an inhibitor of α1-adrenergic receptor. Tamsulosin is used for the research of prostatic hyperplasia. Tamsulosin attenuates abdominal aortic aneurysm growth in animal models .
Cytidine-5'-triphosphate-d14 (Cytidine triphosphate-d14 dilithium; 5'-CTP-d14) dilithium is deuterium labeled Cytidine-5'-triphosphate (HY-125818). Cytidine 5′-triphosphate (Cytidine triphosphate; 5'-CTP) is a nucleoside triphosphate and serves as a building block for nucleotides and nucleic acids, lipid biosynthesis. Cytidine triphosphate synthase can catalyze the formation of cytidine 5′-triphosphate from uridine 5′-triphosphate (UTP). Cytidine 5′-triphosphate is an essential biomolecule?in the de novo?pyrimidine biosynthetic pathway in?T. gondii.
L-Glutamine- 13C5, 15N2,d5 is the deuterium, 13C-, and 15-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells .
Fosfructose- 13C6 (tetrasodium hydrate) is the 13C labeled Fosfructose (HY-106950). Fosfructose is a cytoprotective natural sugar phosphate for the potential treatment of cardiovascular ischemia, sickle cell anemia and asthma[1].
Butylparaben- 13C6 is the 13C labeled Butylparaben[1]. Butylparaben is an organic compound, has proven to be a highly successful antimicrobial preservative in cosmetics, also used in medication suspensions, and as a flavoring additive in food.
Riboflavin-5-Phosphate- 13C4, 15N2-1 is the 13C-labeled and 15N-labeled Riboflavin. Riboflavin is an easily absorbed micronutrient with a key role in maintaining health in humans and other animals.
5'-Guanylic acid- 13C10, 15N5 (5'-GMP- 13C10, 15N5 dilithium; 5'-guanosine monophosphate- 13C10, 15N5) dilithium is 13C and 15N-labeled 5'-Guanylic acid (HY-N5134). 5'-Guanylic acid (5'-GMP) is involved in several metabolic disorders, including the AICA-ribosiduria pathway, adenosine deaminase deficiency, adenine phosphoribosyltransferase deficiency (aprt), and the 2-hydroxyglutric aciduria pathway.
Chlorogenic acid- 13C3 (Heriguard- 13C3; NSC-407296- 13C3) is 13C- and 15N-labeled Chlorogenic acid (HY-N0055). Chlorogenic acid is a major phenolic compound in Lonicera japonica Thunb.. It plays several important and therapeutic roles such as antioxidant activity, antibacterial, hepatoprotective, cardioprotective, anti-inflammatory, antipyretic, neuroprotective, anti-obesity, antiviral, anti-microbial, anti-hypertension .
Clascoterone-d5-1 (Cortexolone 17 alpha-propionate-d5-1) is deuterium labeled Clascoterone. Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist .
HSP90-IN-11 (Compound 12c) is a potent inhibitor of HSP90. HSP90-IN-11 displays potent HSP90α inhibition comparable to AUY-922 (Luminespib). HSP90-IN-11 shows significant antiproliferative activity in CRC and NSCLC cells in a double digit nM range. HSP90-IN-11 leads to rapid degradation of client proteins EGFR and Akt in NSCLC cells. HSP90-IN-11 induces significant accumulation of a sub-G1 phase population .
ERK1/2 inhibitor 9 (Probe 1) is a covalent ERK1/2 inhibitor. ERK1/2 inhibitor 9 shows sub-micromolar activity in cells (A375 GI50=0.47 μM). ERK1/2 inhibitor 9 causes the downregulation of phospho-ERK1/2. ERK1/2 inhibitor 9 tagged trans-cyclo-octene (TCO) and Tz-Thalidomide (tetrazine tagged Thalidomide) can form the corresponding ERK-CLIPTAC to elicit degradation of ERK1/2 .
WWL0245 is a potent and seletive BRD4 PROTAC. WWL0245 selectively degrades BRD4 with sub-nanomolar DC50 (<1 nM) than BRD2/3 and PLK1 ( DC50>1 μM). WWL0245 shows excellent selective cytotoxicity in the BETi sensitive cancer cell lines, including AR-positive prostate cancer cell lines. WWL0245 is a promising drug candidate for AR-positive prostate cancer research and a valuable tool compound to study the biological function of BRD4 .
Cytidine-d13 (Cytosine β-D-riboside-d13; Cytosine-1-β-D-ribofuranoside-d13) is deuterium labeled Cytidine (HY-B0158). Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catecholamine synthesis, and mitochondrial function [3].
Thymidine- 13C10 (DThyd- 13C10; NSC 21548- 13C10) is 13C-labeled Thymidine (HY-N1150). Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication.
Cytidine 5′-monophosphate-d12 (5'-Cytidylic acid-d12 dilithium; 5'-CMP-d12) dilithium is deuterium labeled Cytidine 5'-monophosphate (HY-W009162). Cytidine 5'-monophosphate (5'-Cytidylic acid) is a nucleotide which is used as a monomer in RNA. Cytidine 5'-monophosphate consists of the nucleobase cytosine, the pentose sugar ribose, and the phosphate group.
5'-Guanylic acid-d12 (5'-GMP-d12 dilithium; 5'-guanosine monophosphate-d12) dilithium is deuterium labeled 5'-Guanylic acid (HY-N5134). 5'-Guanylic acid (5'-GMP) is involved in several metabolic disorders, including the AICA-ribosiduria pathway, adenosine deaminase deficiency, adenine phosphoribosyltransferase deficiency (aprt), and the 2-hydroxyglutric aciduria pathway.
L-Glutathione reduced-d2 (GSH-d2; γ-L-Glutamyl-L-cysteinyl-glycine-d2) is deuterated-labeled L-Glutathione reduced (HY-D0187). L-Glutathione reduced is an endogenous antioxidant and oxygen free radical scavenger.
Guanosine- 15N5 is the 15N labeled Guanosine[1]. Guanosine (DL-Guanosine) is a purine nucleoside comprising guanine attached to a ribose (ribofuranose) ring via a β-N9-glycosidic bond. Guanosine possesses anti-HSV activity[2].
Nicotinamide- 13C6 is the 13C-labeled Nicotinamide. Nicotinamide is a form of vitamin B3 that plays essential roles in cell physiology through facilitating NAD+ redox homeostasis and providing NAD+ as a substrate to a class of enzymes that catalyze non-redox reactions. Nicotinamide is an inhibitor of SIRT1.
Guanosine triphosphate- 15N5,d14 (GTP- 15N5,d14) dilithium is deuterium and 15N labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19.
L-Tryptophan- 13C11 is the 13C-labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3[1].
Sulfameter- 13C6 is the 13C6 labeled Sulfameter. Sulfameter (Sulfametoxydiazine; 5-Methoxysulfadiazine) is an effective long-acting sulfonamide antibiotic with antibacterial activities. Sulfameter can be used for the research of urinary tract infections and lepriasis.
Cytidine-d2 is the deuterium labeled Cytidine. Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catecholamine synthesis, and mitochondrial function[1][2][3].
(Rac)-Atomoxetine-d7 (hydrochloride) is a deuterium labeled (Rac)-Atomoxetine hydrochloride. (Rac)-Atomoxetine hydrochloride is a racemic form of Atomoxetine hydrochloride. Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5 nM, 77 nM and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively)[1].
Estrone- 13C2 is the 13C-labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells[1][2].
L-Tryptophan- 15N2 is the 15N-labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3 .
(E,E)-Farnesol-d6 is deuterium labeled Farnesol. Farnesol is a sesquiterpene alcohol that modulates cell-to-cell communication in Candida albicans, and has the activity in inhibiting bacteria.
(R,R)-Secoisolariciresinol diglucoside-d6 is deuterated labeled (R,R)-Secoisolariciresinol diglucoside (HY-N6937). (R,R)-Secoisolariciresinol diglucoside ((R,R)-SDG) is the minor isomer of Secoisolariciresinol diglucoside in flaxseed. (R,R)-Secoisolariciresinol diglucoside ((R,R)-SDG) possesses antioxidant and free radical scavenging activities and DNA-radioprotective properties. (R,R)-Secoisolariciresinol diglucoside ((R,R)-SDG) inhibits myeloperoxidase (MPO) activity by suppressing both the peroxidase and chlorination cyclesin inflammatory cells [3].
Guanosine- 13C10 is the 13C labeled Guanosine (HY-N0097). Guanosine is a purine nucleoside comprising guanine attached to a ribose (ribofuranose) ring via a β-N9-glycosidic bond. Guanosine possesses anti-HSV activity .
Adenosine monophosphate- 15N5,d12 (AMP- 15N5,d12) dilithium is deuterium and 15N labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction [3].
Cytidine-d is the deuterium labeled Cytidine. Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catechol
D-Glucose- 13C,d is the deuterium and 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical sig
D-Glucose- 13C,d2 is the deuterium and 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical sig
D-Glucose- 13C2-4 is the 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
Tacrolimus- 13C,d2 is a 13C-labeled and deuterium labeled Tacrolimus. Tacrolimus (FK506), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties[1].
((2R,3S,4R,5R)-5-(4-Amino-2-oxopyrimidin-1(2H)-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl phosphate- 13C9, 15N3 (sodium) is the 13C and 15N labeled Sodium ((2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1(2H)-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl phosphate[1].
Pentamidine-d4 (dihydrochloride) is the deuterium labeled Pentamidine dihydrochloride. Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dihydrochloride inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dihydrochloride is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dihydrochloride has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities[1][2][3][4].
Guaiacol-d7 is the deuterium labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
Pitavastatin-d5 (sodium) is the deuterium labeled Pitavastatin sodium. Pitavastatin (NK-104) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Anti-cancer activity.
Mirogabalin-d4 (DS5565-d4) is a deuterated compound of Mirogabalin (HY-12650), a ligand that selectively targets the voltage-sensitive calcium channel complex α2δ-1 .
Benzyl alcohol-d7 is the deuterium labeled Benzyl alcohol. Benzyl alcohol is an aromatic alcohol; a colorless liquid with a mild pleasant aromatic odor.
Gemfibrozil-d6 is the deuterium labeled Gemfibrozil. Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.
Agomelatine-d4 is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively[1]. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively[2].
Ambroxol-d5 (hydrochloride) is the deuterium labeled Ambroxol hydrochloride. Ambroxol hydrochloride (NA-872 hydrochloride), an active metabolite of the proagent Bromhexine, has potent expectorant effects. Ambroxol hydrochloride is a glucocerebrosidase (GCase) chaperone and increases glucocerebrosidase activity. Ambroxol hydrochloride induces lung autophagy and has the potential for Parkinson disease and neuronopathic Gaucher disease research[1][2].
Mequinol-d4 is the deuterium labeled Mequinol[1]. Mequinol (4-Methoxyphenol) is one of bioactive components in Mercurialis. Mequinol is used for skin depigmentation[2].
Efinaconazole-d4 is the deuterium labeled Efinaconazole. Efinaconazole (KP-103) is a triazole antifungal agent and againsts T. mentagrophytes SM-110 and C. albicans ATCC 10231 with MICs of 0.0039 μg/mL and 0.00098 μg/mL, respectively[1]. Efinaconazole has a potent in vitro activity against fungal pathogens including dermatophytes, Candida and Malassezia species[1].
Netupitant-d6 is the deuterium labeled Netupitant (CID-6451149), which is a highly potent and selective, orally active neurokinin-1 (NK1) receptor antagonist[1].
Phytosphingosine-d7 (4-Hydroxysphinganine-d7) is deuterium labeled Phytosphingosine. Phytosphingosine is a phospholipid with anti-inflammatory, antibacterial, and anti-cancer activities, which can induce apoptosis. Phytosphingosine is an immune regulator and can be used in the study of inflammatory skin diseases. Phytosphingosine is also an activator of GPR120 with an IC50 value of 33.4 μM and can be used in the study of type II diabetes [3] .
Norfloxacin-d8 is the deuterium labeled Norfloxacin. Norfloxacin (MK-0366) is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria, which functions by inhibiting DNA gyrase.
Ceftazidime-d5 is the deuterium labeled Ceftazidime. Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Ponesimod-d7 (ACT-128800-d7) is the deuterium-labeled Ponesimod (HY-10569). Ponesimod-d7 (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod-d7 activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod-d7 can protect against lymphocyte-mediated tissue inflammation [3].
Eliglustat-d15 (Genz 99067-d15) is deuterium labeled Eliglustat. Eliglustat is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC50 of 24 nM .
Rabeprazole-d4 (sodium) is the deuterium labeled Rabeprazole sodium. Rabeprazole sodium (LY307640 sodium) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H+/K+-ATPase. Rabeprazole sodium induces apoptosis. Rabeprazole sodium acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole sodium can be used for the research of gastric ulcerations and gastroesophageal reflux[1][2][3].
DL-dithiothreitol-d6 is the deuterated form of DL-dithiothreitol. DL-dithiothreitol (DTT) is a strong reductant with anti-disulfidptosis activity. DL-dithiothreitol is oxidized to form a stable six-membered ring with an internal disulfide bond .
Mozavaptan-d6 (OPC-31260-d6) is the deuterium labeled Mozavaptan. Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment .
Sucrose-d14 is the deuterium labeled Sucrose. Sucrose (D-(+)-Saccharose) is a disaccharide which is composed of two monosaccharides, glucose and fructose. Sucrose can be applied in some animal models, including metabolic disease, obesity, diet on preferen
Chlortetracycline-d6 (hydrochloride) is the deuterium labeled Chlortetracycline hydrochloride. Chlortetracycline hydrochloride (7-Chlorotetracycline hydrochloride) is a specific and potent calcium ionophore antibiotic, inhibits binding of aminoacyl-tRNA to ribosomes.
Bexarotene-d4 is a deuterium labeled Bexarotene (LGD1069). Bexarotene (LGD1069) is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma[1][2][3][4][5].
Lenvatinib-d4 is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities[1][2].
2-Hydroxyestrone-d4 is the deuterium labeled 2-Hydroxyestrone. 2-Hydroxyestrone (Catecholestrone) is a specific receptor-mediated antiestrogenic agent. 2-Hydroxyestrone is anticarcinogenic[1][2].
Imiquimod-d6 is the deuterium labeled Imiquimod. Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19[1][2].
Homosalate-d4 is the deuterium labeled Homosalate. Homosalate is an organic compound used in some sunscreens, it is used as a chemical UV filter, protecting the skin from sun damage.
Pomalidomide-d4 is the deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors<
Dienogest-d6 is deuterium labeled Dienogest (HY-B0084). Dienogest is an orally active progesterone receptor agonist that can be used in the study of endometriosis [3].
Oseltamivir-d5 (phosphate) is the deuterium labeled Oseltamivir phosphate. Oseltamivir phosphate (GS 4104) is a neuraminidase inhibitor recommended for the treatment and prophylaxis of influenza A and B[1][2].
Evocalcet-d4 (KHK7580-d4) is deuterium labeled Evocalcet. Evocalcet (KHK7580) is an orally active calcium sensing receptor (CaSR) agonist. Evocalcet inhibits the secretion of parathyroid hormone (PTH) from parathyroid gland cells. Evocalcet can be used for the research of hyperparathyroidism .
Ledipasvir-d6 hydrochloride is deuterated labeled Ledipasvir acetone (HY-15602A). Ledipasvir acetone (GS-5885 acetone) is the active ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
Upadacitinib-d5 is the deuterium labeled Upadacitinib. Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Pravastatin-d9 sodium is deuterated labeled Pravastatin (HY-B0165). Pravastatin (CS-514) is a competitive HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM .
Cariprazine-d6 is a deuterium labeled Cariprazine. Cariprazine Cariprazine is an antipsychotic agent that exhibits high affinity for the D3 (Ki of 0.085 nM) and D2 (Ki of 0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki of 2.6 nM)[1].
Ertugliflozin-d9 is deuterated labeled Ertugliflozin (HY-15461). Ertugliflozin (PF-04971729) is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), with an IC50 of 0.877 nM for h-SGLT2 . Has the potential for the treatment of type 2 diabetes mellitus .
Carboplatin-d4 is the deuterium labeled Carboplatin. Carboplatin (NSC 241240) is a DNA synthesis inhibitor which binds to DNA, inhibits replication and transcription and induces cell death. Carboplatin (NSC 241240) is a derivative of CDDP and a potent anti-cancer agent.
Oxcarbazepine-d4 (GP 47680-D4) is the deuterium labeled Oxcarbazepine. Oxcarbazepine is a sodium channel blocker[1]. Oxcarbazepine significantly inhibits glioblastoma cell growth and induces apoptosis or G2/M arrest in glioblastoma cell lines[2]. Anti-cancer and anticonvulsant effects[2][3].
Penicillin G-d5 (potassium) is the deuterium labeled Penicillin G potassium. Penicillin G potassium is a fast-acting antibiotic; used to treat bacterial infections that affect the blood, heart, lungs, joints, and genital areas[1][2].
Trandolapril-d5 is a deuterium labeled Trandolapril (RU44570). Trandolapril is an orally active angiotensin converting enzyme (ACE) inhibitor for hypertension and congestive heart failure (CHF)[1].
Levobupivacaine-d9 ((S)-(–)-Bupivacaie-d9) hydrochloride is deuterium labeled Levobupivacaine (hydrochloride). Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine hydrochloride exerts agent that can suppress or relieve pain. and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer [3] .
Posaconazole-d5 is a deuterium-labeled form of Posaconazole. Posaconazole is a broad-spectrum, second generation, triazole compound with antifungal activity[1].
Ergothioneine-d9 is the deuterium labeled Ergothioneine. Ergothioneine, an imidazole-2-thione derivative of histidine betaine, is synthesized by certain bacteria and fungi. Ergothioneine is generally considered an antioxidant[1].
Cuminaldehyde-d8 is deuterated labeled Cuminaldehyde (HY-Y0790). Cuminaldehyde is the major component of Cuminum cyminum, a natural aldehyde with inhibitory effect on alpha-synuclein fibrillation and cytotoxicity. Cuminaldehyde shows anticancer activity .
Odevixibat-d5 is deuterated labeled Odevixibat (HY-109120). Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis .
Amoxapine-d8 is the deuterium labeled Amoxapine. Amoxapine (CL-67772) is a norepinephrine reuptake blocker and a 5-HT2/5-HT3 antagonist. Amoxapine can be used for the research of depression. Amoxapine has antibacterial activity. Amoxapine can enhance the killing effect of macrophages on mycobacterium by inducing autophagy, while protecting the cells from death [3] .
Terconazole-d4 is the deuterium labeled Terconazole. Terconazole is a broad-spectrum antifungal medication for the treatment of vaginal yeast infection.
Lenvatinib-d5 is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities[1][2].
Resorufin-d6 is the deuterium labeled Resorufin. Resorufin (NSC 12097) is a highly fluorescent pink dye for the detection of ROS/RNS and a second analyte[1].
4-Hydroxytolbutamide-d9 is the deuterium labeled 4-Hydroxytolbutamide. 4-Hydroxytolbutamide (Hydroxytolbutamide) is a metabolite of Tolbutamide. 4-Hydroxytolbutamide is metabolized by CYP2C8 and CYP2C9. Tolbutamide is a first generation potassium channel blocker and a sulfonylurea oral antidiabetic[1][2].
Cilostazol-d4 is deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM[1][2].
Palbociclib-d8 is a deuterium labeled Palbociclib. Palbociclib is a selective and orally active CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research[1].
Arachidonic acid-d11 is the deuterium labeled Arachidonic acid. Arachidonic acid is an essential fatty acid and a major constituent of biomembranes[1][2].
Itraconazole-d5 is the deuterium labeled Itraconazole. Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects[1][2][3].
Sotalol-d6 (hydrochloride) is a deuterium labeled Sotalol hydrochloride. Sotalol hydrochloride is an orally active, non-selective competitive β-adrenergic receptor blocker. Sotalol hydrochloride is a potent antiarrhythmic agent that can be used for the research of pediatric arrhythmias. Sotalol hydrochloride blocks β-receptors, and potassium KCNH2 channels[1][2].
Bezafibrate-d4 is deuterium labeled Bezafibrate. Bezafibrate is an agonist of PPAR, with EC50s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent.
Darifenacin-d4 is the deuterium labeled Darifenacin[1]. Darifenacin(UK88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9. IC50 value: 8.9 (pKi)[2].
Fingolimod-d4 (hydrochloride) is the deuterium labeled Fingolimod hydrochloride. Fingolimod hydrochloride (FTY720) is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod hydrochloride (FTY720) also is a pak1 activator, a immunosuppressant[1].
Troglitazone-d4 is deuterium labeled Troglitazone. Troglitazone is a PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively.
Abiraterone-d4 is the deuterium labeled Abiraterone. Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.
Treprostinil-d7 (UT-15-d7) is a deuterated version of Treprostinil (HY-100441). Treprostinil is a highly potent DP1 and EP2 agonist with EC50s of 0.6 nM and 6.2 nM, respectively [3] .
Anastrozole-d12 is the deuterium labeled Anastrozole. Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC50 of 15 nM[1][2].
Montelukast-d6 (sodium) is the deuterium labeled Montelukast (sodium). Montelukast sodium is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (Cysltr1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage[1].
Diaveridine-d6 (EGIS-5645-d6) is deuterium labeled Diaveridine. Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent .
Siponimod-d11 is deuterium labeled Siponimod (HY-12355). Siponimod is an orally active and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod is selective for S1P1 and S1P5 over S1P2, S1P3, and S1P4, with EC50s of 0.4, 0.98, >10000, >1000, and 750 nM, respectively. Siponimod can be used for multiple sclerosis (MS) research [3] .
Equilin-d4 is the deuterium labeled Equilin. Equilin (7-Dehydroestrone) is an important member of the large group of oestrogenic substances and is chemically related to menformon (oestrone). Equilin increases the growth of cortical neurons via an NMDA receptor-dependent mechanism[1][2].
Lauryl benzalkonium-d7 (Dimethylaurylbenzylammonium-d7) chloride is the deuterium labeled Lauryl benzalkonium chloride. Lauryl benzalkonium chloride is a cationic surfactant .
Dolasetron-d5 is deuterated labeled Dolasetron (HY-B0750). Dolasetron (MDL-73147) is a 5-HT3 receptor antagonist with potential for treatment of chemotherapy-induced nausea and vomiting.
Topiroxostat-d4 is deuterium labeled Topiroxostat. Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 value of 5.3 nM and a Ki value of 5.7 nM. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment[1][2].
Cimaterol-d7 is the deuterium labeled Cimaterol. Cimaterol is a potent agonist of β-adrenergic receptors (pEC50s=8.13, 8.78, and 6.62 for human β1, β2, and β3, respectively). Cimaterol has been used in farmed animals to increase carcass mass and to alter muscle and fat deposition.
Benzyl alcohol-d5 is the deuterium labeled Benzyl alcohol. Benzyl alcohol is an aromatic alcohol; a colorless liquid with a mild pleasant aromatic odor.
Azaperone-d4 is the deuterium labeled Azaperone. Azaperone (R-1929) acts as a dopamine antagonist but also has some antihistaminic and anticholinergic properties. Azaperone is a pyridinylpiperazine and butyrophenone neuroleptic agent with antiemetic effects, which is used mainly as a tranquilizer in veterinary medicine.
Levonorgestrel-d8 is the deuterium labeled Levonorgestrel. Levonorgestrel is a synthetic progestogen used as an active ingredient in some hormonal contraceptives[1][2]. Levonorgestrel-d8 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Ropinirole-d14 hydrochloride is deuterated labeled Ropinirole hydrochloride (HY-B0623A). Ropinirole (SKF 101468) hydrochloride is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease .
Valproic acid-d7 (sodium) is the deuterium labeled Valproic acid (sodium salt). Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium salt activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches[1][2].
Canagliflozin-d6 is the deuterium labeled Canagliflozin[1]. Canagliflozin (JNJ 28431754) is a selective SGLT2 inhibitor with IC50s of 2 nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and hSGLT2 in CHOK cells, respectively[2].
Losartan-d2 is the deuterium labeled Losartan[1]. Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.
Telmisartan-d4 is the deuterium labeled Telmisartan. Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM[1][2].
Apalutamide-d4 is a deuterium labeled Apalutamide. Apalutamide is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM[1].
Pemetrexed-d5 is the deuterium labeled Pemetrexed[1]. Pemetrexed (LY231514) is an antifolate, the Ki values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively[2].
Apremilast-d8 (CC-10004-d8) is deuterium labeled Apremilast. Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM .
Acetylcholine-d4 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs)[1][2]. Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro[5].
Clomifene-d5 (hydrochloride) is a deuterium labeled Clomifene. Clomifene is an orally active compound used for infertility. Clomifene is a simple, relatively safe, easily administered and well-tolerated efficacious compound to induce ovulation[1].
Acalabrutinib-d4 is a deuterium labeled Acalabrutinib. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor[1]. Acalabrutinib-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Carvedilol-d4 is the deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker[1]. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure[2]. Carvedilol is an autophagy inducer that inhibits the NLRP3inflammasome[3].
Crizotinib-d9 hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition [3].
Methylprednisolone-d2 is the deuterium labeled Methylprednisolone. Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels[3][4].
Posaconazole-d4 is a deuterium-labeled form of Posaconazole. Posaconazole is a broad-spectrum, second generation, triazole compound with antifungal activity[1].
Icotinib-d4 is the deuterium-labeled Icotinib (HY-15164A). Icotinib-d4 (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib-d4 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Debutyldronedarone-d7 hydrochloride is deuterated labeled Debutyldronedarone hydrochloride (HY-12753A). Debutyldronedarone (SR35021) hydrochloride, the main metabolite of Dronedarone, is a selective thyroid hormone receptor α1 (TRα1) inhibitor. Debutyldronedarone hydrochloride inhibits T3 binding to TRα1 and TRβ1 by 77% and 25%, respectively. Debutyldronedarone hydrochloride can be used for the research of arrhythmic .
Tigecycline-d9 is deuterium labeled Tigecycline. Tigecycline (GAR-936) is a broad-spectrum glycylcycline antibiotic. The mean inhibitory concentration (MIC) of Tigecycline for E. coli (MG1655 strain) is approximately 125 ng/mL[1]. MIC50 and MIC90 are 1 and 2 mg/L for Acinetobacter baumannii (A. baumannii), respectively[2].
Risedronic acid-d4 (Risedronate-d4) is the deuterium labeled Risedronic acid (HY-B0148).Risedronic acid (Risedronate) sodium, a bisphosphonate, is a potent anti-resorption agent that inhibits osteoclast-mediated bone resorption and changes the bone metabolism. Risedronic acid sodium suppresses osteoblast differentiation and induced caspase- and isoprenoid depletion-dependent apoptosis. Risedronic acid sodium inhibits blood stages of Plasmodium falciparum (IC50 of 20.3 μM). Risedronic acid sodium inhibits the transfer of the farnesyl pyrophosphate group to parasite proteins [3] .
Donepezil-d5 (hydrochloride) is deuterium labeled Donepezil (Hydrochloride). Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE[1]. Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity[2].
Permethrin-d9 is the deuterium labeled Permethrin. Permethrin (NRDC-143) is an insecticide, acaricide, and insect repellent; functions as a neurotoxin, affecting neuron membranes by prolonging sodium channel activation.
Losartan-d9 is the deuterium labeled Losartan[1]. Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.
Azilsartan-d4 is the deuterium labeled Azilsartan[1]. Azilsartan is an orally active, potent, selective and specific angiotensin II type 1 receptor (AT1) antagonist. Azilsartan induces ROS formation and apoptosis in HepG2 cells. Azilsartan shows neuroprotective and anticancer activity. Azilsartan can be used for hypertension and stroke research[2][3][4][5][6].
Desloratadine-d4 is the deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities[1][2].
Desloratadine-d5 is deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities[1][2].
Alfuzosin-d7 is the deuterium labeled Alfuzosin[1]. Alfuzosin (SL 77499-10) is an orally active, selective and competitive α1-adrenoceptor antagonist. Alfuzosin relaxes the muscles of the prostate and bladder neck, aiding in urination. Alfuzosin can be used in study of benign prostatic hyperplasia (BPH)[2][3].
Enzalutamide-d6 (MDV3100-d6) is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells .
1-Octanol-d5 is deuterated labeled Carvacrol (HY-N0711). Carvacrol is an orally active monoterpenic phenol that can be extract from an abundant number of aromatic plants, including thyme and oregano, possessing antioxidant, antibacterial, antifungal, anticancer, anti-inflammatory, hepatoprotective, spasmolytic, and vasorelaxant properties. Carvacrol also causes cell cycle arrest in G0/G1, downregulates Notch-1, and Jagged-1, and induces apoptosis. Carvacrol is used in low concentrations as a food flavoring ingredient and preservative, as well as a fragrance ingredient in cosmetic formulations .
Leniolisib-d5 is a deuterated labeled Leniolisib . Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor. Leniolisib has the potential for immunodeficiency disorders treatment.
Treprostinil-d9 (UT-15-d9) is the deuterium-labeled Treprostinil (HY-100441) . Treprostinil (UT-15) is a potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively.
1-Octanol-d17 is the deuterium labeled 1-Octanol[1]. 1-Octanol (Octanol), a saturated fatty alcohol, is a T-type calcium channels (T-channels) inhibitor with an IC50 of 4 μM for native T-currents[2]. 1-Octanol is a highly attractive biofuel with diesel-like properties[3].
Diphenyl Phosphate-d10 (DPhP-d10) is the deuterium labled Diphenyl Phosphate (HY-W008151). Diphenyl Phosphate inhibits growth and energy metabolism of zebrafish in a sex-specific manner.
Cefiderocol-d6 (S-649266-d6) is a deuterated labeled Cefiderocol (HY-17628). Cefiderocol is a siderophore cephalosporin which has a potent activity against a broad range of aerobic Gram-negative bacterial species with MIC50s of 2 μg/mL or less .
Paroxetine-d4 (BRL29060-d4) is deuterium labeled Paroxetine. Paroxetine is an oral inhibitor that falls under the category of selective serotonin reuptake inhibitors (SSRIs). Paroxetine is also a very weak norepinephrine (NE) reuptake inhibitor, capable of inducing cell apoptosis and having anti-tumor activity. Paroxetine has antidepressant, anti-anxiety, and pain-relieving effects, and it can help improve conditions like obsessive-compulsive disorder, panic disorder, post-traumatic stress disorder, premenstrual anxiety, and chronic headaches [3] .
Tetrahydrozoline-d4 (hydrochloride) is the deuterium labeled Tetrahydrozoline hydrochloride. Tetrahydrozoline hydrochloride (Tetryzoline hydrochloride), a derivative of imidazoline, is an α-adrenergic agonist that causes vasoconstriction. Tetrahydrozoline hydrochloride is widely used for the research of nasal congestion and conjunctival congestion[1][2].
Creatinine-d5 is the deuterium labeled Creatinine. Creatinine (NSC13123) is a break-down product of creatine phosphate in muscle, and is usually produced at a fairly constant rate by the body [3].
Tandospirone-d8 (SM-3997-d8) is deuterium labeled Tandospirone. Tandospirone (SM-3997) is a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM. Tandospirone has anxiolytic and antidepressant activities. Tandospirone can be used for the research of the central nervous system disorders and the underlying mechanisms [3] .
Dimethylamine-d6 hydrochloride is a deuterium labeled Dimethylamine hydrochloride. Dimethylamine hydrochloride is the immediate precursor of dimethylnitrosamine, a known potent carcinogen in a wide variety of animal species .
Bendamustine-d8 (hydrochloride) is deuterium labeled Bendamustine (hydrochloride). Bendamustine hydrochloride (SDX-105), a purine analogue, is a DNA cross-linking agent. Bendamustine hydrochloride activats DNA-damage stress response and apoptosis. Bendamustine hydrochloride has potent alkylating, anticancer and antimetabolite properties[1].
Laquinimod-d5 (ABR-215062-d5) is deuterium labeled Laquinimod. Laquinimod (ABR-215062), an orally available carboxamide derivative, is a potent immunomodulator that prevents neurodegeneration and inflammation in the central nervous system. Laquinimod reduces astrocytic NF-κB activation to protect from Cuprizone-induced demyelination. Laquinimod has the potential for relapsing-remitting (RR) and chronic progressive (CP) forms of multiple sclerosis (MS; RRMS or CPMS) as well as neurodegenerative diseases research .
Penicillin V-d5 (potassium) is the deuterium labeled Penicillin V Potassium[1]. Penicillin V Potassium (Phenoxymethylpenicillin potassium salt) is an orally active antibiotic. Penicillin V Potassium inhibits the growth of Streptococci, C. difficile and S. aureus. Penicillin V Potassium can be used for the research of otitis, sinusitis, pharyngitis and tonsillitis[2][3][4][5].
Cariprazine-d8 is a deuterium labeled Cariprazine. Cariprazine is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
Sotorasib-d7 (AMG-510-d7) is a deuterium-labeled Sotorasib (HY-114277). Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) [3].
Carvedilol-d5 is deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker[1]. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure[2]. Carvedilol is an autophagy inducer that inhibits the NLRP3inflammasome[3].
Lopinavir-d7 is deuterated labeled Lopinavir (HY-14588). Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM [3].
Octopamine-d4 (hydrochloride) is the deuterium labeled Octopamine hydrochloride. Octopamine ((±)-p-Octopamine) hydrochloride, a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates. Octopamine hydrochloride can stimulate alpha2-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha2-ARs. Octopamine hydrochloride increased glycogenolysis, glycolysis, oxygen uptake, gluconeogenesis and the portal perfusion pressure[1][2][3].
Elacestrant-d10 is the deuterium labeled of Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also inhibits growth of ER + breast cancer cell lines in vitro and in vivo .
Chenodeoxycholic Acid-d4 is the deuterium labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
Rimonabant-d10 is deuterium labeled Rimonabant. Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
Trifloxystrobin-d6 is the deuterium labeled Trifloxystrobin. Trifloxystrobin (CGA 279202) is a fungicide, with EC50s of 23.0 μg/L and 1.7 μg/L for Daphnia magna neonate and embryos, respectively, after treatment for 48 h[1].
Loperamide-d6 (hydrochloride) is a deuterium labeled Loperamide hydrochloride. Loperamide hydrochloride is an opioid receptor agonist for the treatment of diarrhea[1].
Celecoxib-d7 is the deuterium labeled Celecoxib. Celecoxib,a selective non-steroidal anti-inflammatory drug (NSAID), is a selective COX-2 inhibitor with an IC50 of 40 nM[1][2].
Edaravone-d5 is a deuterium labeled Edaravone. Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator[1][2][3][4].
Vandetanib-d6 is the deuterium labeled Vandetanib. Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM)[1].
Pimozide-d4 is a deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5[1][2][3].
Abemaciclib-d8 is the deuterium labeled Abemaciclib. Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.
Dimethyl phthalate-d6 is the deuterium labeled Dimethyl phthalate. Dimethyl phthalate, a known endocrine disruptor and one of the phthalate esters (PAEs), is a ubiquitous pollutant. Dimethyl phthalate is commonly used as a plasticizer to impart flexibility to rigid polyvinylchloride (PVC) resins[1].
Cinacalcet-d4 (AMG-073-d4) hydrochlorideis deuterium labeled Cinacalcet (hydrochloride). Cinacalcet hydrochloride (AMG-073 hydrochloride) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment .
Remdesivir-d5 is a deuterium labeled Remdesivir. Remdesivir (GS-5734) is a nucleoside analogue, with effective antiviral activity, with EC50s of 74 nM for SARS-CoV and MERS-CoV in HAE cells, and 30 nM for murine hepatitis virus in delayed brain tumor cells. Remdesivir is highly effective in the control of 2019-nCoV (COVID-19) infection in vitro[1][2].
Lenalidomide-d5 is deuterium labeled Lenalidomide. Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells[1][2].
Capsaicin-d7 is deuterated labeled Capsaicin (HY-10448). Capsaicin ((E)-Capsaicin), an active component of chili peppers, is a TRPV1 agonist. Capsaicin has pain relief, antioxidant, anti-inflammatory, neuroprotection and anti-cancer effects .
Valproic acid-d14 (sodium) is deuterium labeled Valproic acid (sodium). Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium salt activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
N-Ethylmaleimide-d5 is the deuterium labeled N-Ethylmaleimide. N-Ethylmaleimide (NEM), a reagent that alkylates free sulfhydryl groups, is a cysteine protease inhibitor[1]. N-ethylmaleimide specific inhibits phosphate transport in mitochondria[2]. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor[3].
Atazanavir-d6 is deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration[1]. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)[2]. Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM[3].
Ubrogepant-d5 (MK-1602-d5) is deuterium labeled Ubrogepant. Ubrogepant (MK-1602) is an orally active and selective antagonist of calcitonin gene-related peptide receptor (CGRP). Ubrogepant has high affinity for CGRP receptors in human and rhesus monkeys, and can effectively block the cAMP response stimulated by α-CGRP. Ubrogepant can be used in the study of acute migraine [3].
Acipimox-d4 is the deuterium labeled Acipimox. Acipimox (K-9321), a nicotinic acid analogue, is an antilipolytic compound. Acipimox acutely inhibits lipolysis and suppresses systemic levels of free fatty acids (FFAs) and improves insulin sensitivity .
Lurasidone-d8 is deuterium labeled Lurasidone. Lurasidone (SM-13496) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (SM-13496) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.
Afatinib-d4 is the deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.
Buformin-d9 (hydrochloride) is the deuterium labeled Buformin. Buformin (1-Butylbiguanide), a potent AMPK activator, acts as an orally active biguanide antidiabetic agent. Buformin decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al)[1].
Hydroxymetronidazole-d4 is the deuterium labeled Hydroxymetronidazole. Hydroxymetronidazole (Metronidazole-OH) is a metabolite of Metronidazole belonging to the class of nitroimidazoles. Hydroxymetronidazole can be used for the research of certain bacterial and protozoal diseases in poultry, swine dysentery and genital trichomoniasis in cattle[1].
(R)-Lansoprazole-d4 is deuterium labeled (R)-Lansoprazole. (R)-Lansoprazole is the R enantiomer of Lansoprazole, Lansoprazole (AG 1749) is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[1][2].
Olmesartan-d6 (RNH-6270-d6) is the deuterium labeled Olmesartan. Olmesartan (RNH-6270) is an angiotensin II receptor (AT1R) antagonist used to treat high blood pressure[1][2].
Ramelteon-d5 is deuterium labeled Ramelteon. Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation[1][2].
Vapendavir-d5 is the deuterium labeled Vapendavir. Vapendavir (BTA798) is a potent enteroviral capsid binder (CB). Vapendavir (BTA798) possesses potent antiviral activity for enterovirus 71 (EV71) replication, with EC50 values of 0.5-1.4 μM in different EV71 strains .
Flurbiprofen-d5 is the deuterium labeled Flurbiprofen. Flurbiprofen (dl-Flurbiprofen) is a potent, orally active nonsteroidal anti-inflammatory agent (NSAIA/NSAID), with antipyretic and analgesic activities. Flurbiprofen is commonly used for the research of inflammatory diseases, including osteoarthritis and rheumatoid arthritis. Flurbiprofen is a non-selective cyclooxygenase (COX) inhibitor that can be used for the research of colorectal cancer[1][2][3].
Levamisole-d5 (hydrochloride) is the deuterium labeled Levamisole hydrochloride. Levamisole ((-)-Tetramisole) hydrochloride is an anthelmintic and immunomodulator belonging to a class of synthetic imidazothiazole derivatives. Levamisole hydrochloride has antiviral effects against HSV[1][2].
Rabeprazole-d4 potassium is deuterated labeled Rabeprazole sodium (HY-B0656A). Rabeprazole sodium (LY307640 sodium) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H +/K +-ATPase. Rabeprazole sodium induces apoptosis. Rabeprazole sodium acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole sodium can be used for the research of gastric ulcerations and gastroesophageal reflux [3].
Permethrin-d5 (NRDC-143-d5) is the deuterium labeled Permethrin. Permethrin (NRDC-143) is an insecticide, acaricide, and insect repellent; functions as a neurotoxin, affecting neuron membranes by prolonging sodium channel activation[1][2].
Gefitinib-d6 is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity[1][2].
Ketoprofen-d4 is the deuterium labeled Ketoprofen. Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC50s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively[1].
Macitentan-d4 is a deuterium labeled Sulfamethoxazole. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin) receptor antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH)[1].
Nintedanib-d8 is deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
Sarpogrelate-d4 (MCI-9042-d4) hydrochloride is deuterium labeled Sarpogrelate (hydrochloride). Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis [3] .
Rupintrivir-d7 is a deuterated labeled Rupintrivir . Rupintrivirvr (AG7088), an antiviral agent, is a potent, selective and irreversible inhibitor of human rhinovirus (HRV) 3C protease. Rupintrivirvr inhibits replication of a panel of 48 different HRV serotypes in H1-HeLA and MRC-5 cell protection assays, with a mean EC50 of 0.023 μM. Rupintrivirvr shows immune-modulatory effect [3].
Famotidine-d4 (MK-208-d4) is deuterium labeled Famotidine. Famotidine (MK-208) is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion .
Desloratadine-d9 is the deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities[1][2].
Simvastatin-d6 (MK 733-d6) is the deuterium labeled Simvastatin. Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.
Ertugliflozin-d5 is the deuterium labeled Ertugliflozin[1]. Ertugliflozin (PF-04971729) is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), with an IC50 of 0.877 nM for h-SGLT2[2]. Has the potential for the treatment of type 2 diabetes mellitus[3].
Famciclovir-d4 is the deuterium labeled Famciclovir. Famciclovir (BRL 42810) is a guanine analogue antiviral agent used for the treatment of various herpesvirus infections[1][2].
Methoprene-d7 is the deuterium labeled Methoprene[1]. Methoprene, an insect juvenile growth hormone mimic, is a growth-regulating insecticide that manifests its toxicity to target organisms by acting as a juvenile hormone agonist[2][3].
Levocetirizine-d4 (dihydrochloride) is the deuterium labeled Levocetirizine. Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria[1].
Olanzapine-d8 is a deuterated labeled Olanzapine . Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic [3].
Spironolactone-d7 is the deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC50 of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes[1][2][3].
Latanoprost-d4 is the deuterium labeled Latanoprost. Latanoprost (PHXA41) is a prostaglandin F2α analogue and an agonist for the FP prostanoid receptor, and lowers intraocular-pressure (IOP).
Terbuthylazine-desethyl-d9 is the deuterium labeled Terbuthylazine-desethyl[1]. Terbuthylazine-desethyl (Desethylterbuthylazine) is a chloro dealkylated metabolite of Terbuthylazine (a triazine herbicide)[2][3].
Probucol-d6 is deuterium labeled Probucol. Probucol (DH-581) is an anti-hyperlipidemic agent by lowering the level of cholesterol in the bloodstream by increasing the rate of LDL catabolism.
Meropenem-d6 is the deuterium labeled Meropenem. Meropenem (SM 7338) is a carbapenem antibiotic with broad-spectrum antibacterial activity. Meropenem has activity against susceptible and resistant N. gonorrhoeae (MIC value of 0.02-0.06 mg/mL), H. influenzae (MIC value of 0.03-0.12 mg/mL), and H. ducreyi (MIC value of 0.015-0.12 mg/mL)[1][2].
Brinzolamide-d5 (hydrochloride) is the deuterium labeled Brinzolamide hydrochloride[1]. Brinzolamide (AL-4862) hydrochloride is a selective carbonic anhydrase II inhibitor with an IC50 value of 3.2 nM. Brinzolamide hydrochloride reduces intraocular pressure (IOP) by inhibiting ciliary CA-II and decreasing atrial fluid secretion. Brinzolamide hydrochloride can be used in glaucoma disease research[2][3].
Ethylenediaminetetraacetic acid-d16 is the deuterium labeled Ethylenediaminetetraacetic acid[1]. Ethylenediaminetetraacetic acid (EDTA) is a metal chelators (binds to metal divalent and trivalent cations including calcium), which shows activities of anticoagulant and anti-hypercalcemic. Ethylenediaminetetraacetic acid decreases the metal ion-catalyzed oxidative damage to proteins, and allows maintenance of reducing environment during protein purification. Ethylenediaminetetraacetic acid can also decrease the formation of disulfide bonds[2][3][4].
Sitagliptin-d4 (MK-0431-d4) is deuterium labeled Sitagliptin. Sitagliptin (MK-0431) is a potent and orally active inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts .
Palbociclib-d4 (hydrochloride) is the deuterium labeled Palbociclib hydrochloride. Palbociclib (PD 0332991) is a selective CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research[1].
Sacubitril-d4 is the deuterium labeled Sacubitril. Sacubitril (AHU-377) is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril (AHU-377) is a component of the heart failure medicine LCZ696.
Azimilide-d8 (dihydrochloride) is the deuterium labeled Azimilide dihydrochloride. Azimilide Dihydrochloride (NE-10064 Dihydrochloride) is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.
Pioglitazone-d4 is a deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively[1].
Rosiglitazone-d4 is deuterated labeled Rosiglitazone (HY-17386). Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone is an TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer .
Ivacaftor-d9 is a potent CFTR modulator and exhibits an EC50 value of 255 nM for CFTR potentiation in G551D/F508del HBE Cells. Ivacaftor-D9 acts as an orally active and improved deuterated Ivacaftor analog for cystic fibrosis research[1].
Losartan-d6 hydrochloride is deuterated labeled Losartan potassium (HY-17512A). Losartan potassium (DuP-753 potassium) is an angiotensin II receptor type 1 (AT1) antagonist, competing with the binding of angiotensin II to AT1 with an IC50 of 20 nM.
Moxonidine-d7 is deuterated labeled Moxonidine (HY-B0374). Moxonidine (BDF5895) is an imidazoline type 1 receptor (I1-R) selective agonist and antihypertensive agent.
Telaprevir-d4 is the deuterium labeled Telaprevir. Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide[1][2][3]. Telaprevir inhibits SARS-CoV-2 3CLpro activity[4].
Dabigatran-d4 (hydrochloride) is deuterium labeled Dabigatran, which is a reversible and selective, direct thrombin inhibitor (DTI) with a Ki value of 4.5 nM.
Remdesivir-d4 is deuterium labeled Remdesivir. Remdesivir (GS-5734), a nucleoside analogue with effective antiviral activity, has EC50s of 74 nM for SARS-CoV and MERS-CoV in HAE cells, and 30 nM for murine hepatitis virus in delayed brain tumor cells. Remdesivir is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro[1][2].
Finasteride-d9 is deuterium labeled Finasteride. Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia[1][2][3].
Odanacatib-d4 is the deuterium labeled Odanacatib (HY-10042). Odanacatib is a potent and selective inhibitor of cathepsin K, with an IC50 of 0.2 nM for human cathepsin K .
Ledipasvir-d6 is the deuterium labeled Ledipasvir. Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.62 μM[3].
Amitraz-d6 (BTS-27419-d6) is the deuterium labeled Amitraz. Amitraz is a non-systemic acaricide and insecticide, with alpha-adrenergic agonist activity, interaction with octopamine receptors of the central nervous system and inhibition of monoamine oxidases and prostaglandin synthesis.
DL-dithiothreitol-d10 is the deuterated form of DL-dithiothreitol. DL-dithiothreitol (DTT) is a strong reductant with anti-disulfidptosis activity. When DL-dithiothreitol is oxidized, it forms a stable six-membered ring with an internal disulfide bond .
Sitagliptin-d4 (hydrochloride) is the deuterium labeled Sitagliptin[1]. Sitagliptin (MK-0431) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts[2].
Losartan-d4 is the deuterium labeled Losartan. Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.
Nicardipine-d4 hydrochloride is deuterated labeled Nicardipine hydrochloride (HY-12515A). Nicardipine hydrochloride (YC-93) is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine hydrochloride acts as an agent for chronic stable angina and for controlling blood pressure .
1-Octanol-d2 is the deuterium labeled 1-Octanol[1]. 1-Octanol (Octanol), a saturated fatty alcohol, is a T-type calcium channels (T-channels) inhibitor with an IC50 of 4 μM for native T-currents[2]. 1-Octanol is a highly attractive biofuel with diesel-like properties[3].
Enasidenib-d6 (AG-221-d6) is the deuterium labeled Enasidenib (HY-18690) . Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2 R140Q and IDH2 R172K, respectively .
Miconazole-d2 is the deuterium labeled Miconazole[1]. Miconazole (R18134) is an imidazole antifungal agent. Miconazole also has antibacterial effects[2][3].
Ribociclib-d6 is a deuterium labeled Ribociclib. Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex[1].
Hydroxymetronidazole-d2 is the deuterium labeled Hydroxymetronidazole(HY-136440).Hydroxymetronidazole (Metronidazole-OH) is a metabolite of Metronidazole belonging to the class of nitroimidazoles. Hydroxymetronidazole can be used for the research of certain bacterial and protozoal diseases in poultry, swine dysentery and genital trichomoniasis in cattle .
Debutyldronedarone-d7 is deuterium labeled Debutyldronedarone. Debutyldronedarone is a major circulating active metabolite of dronedarone (HY-A0016) in humans.Debutyldronedarone exhibits a potency that is 1/10 to 1/3 of that of the parent agent[1][2].
Dapoxetine-d6 (LY-210448-d6) hydrochloride is the deuterium labeled Dapoxetine hydrochloride. Dapoxetine hydrochloride is a short-acting selective serotonin reuptake inhibitor (SSRI)
Brexpiprazole-d8 (OPC-34712-d8) is the deuterium labeled Brexpiprazole (HY-15780). Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM) [3].
Arachidonic acid-d8 is the deuterium labeled Arachidonic acid. Arachidonic acid is an essential fatty acid and a major constituent of biomembranes[1][2].
Ivacaftor-d9 is a potent CFTR modulator and exhibits an EC50 value of 255 nM for CFTR potentiation in G551D/F508del HBE Cells. Ivacaftor-D9 acts as an orally active and improved deuterated Ivacaftor analog for cystic fibrosis research .
Atazanavir-d9 is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration[1]. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)[2]. Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM[3].
Crizotinib-d5 is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition [3].
Ivacaftor-d18 is the deuterium labeled Ivacaftor[1]. Ivacaftor (VX-770) is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively[2].
Alfuzosin-d6 (SL 77499-d6) is deuterium labeled Alfuzosin. Alfuzosin (SL 77499-10) is an orally active, selective and competitive α1-adrenoceptor antagonist. Alfuzosin relaxes the muscles of the prostate and bladder neck, aiding in urination. Alfuzosin can be used in study of benign prostatic hyperplasia (BPH) [3].
2-Iodoacetamide-d4 is the deuterium labeled 2-Iodoacetamide[1]. 2-Iodoacetamide (Iodoacetamide), an alkylating agent, is a commonly used agent for alkylation of cysteine during sample preparation for proteomics[2][3].
Rabeprazole-d4 is a deuterium labeled Rabeprazole. Rabeprazole is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H+/K+-ATPase. Rabeprazole induces apoptosis. Rabeprazole acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole can be used for the research of gastric ulcerations and gastroesophageal reflux[1][2][3].
Clozapine-d4 is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors[1][2][3][4][5].
Chenodeoxycholic acid-d5 is the deuterium labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
Ticlopidine-d4 is the deuterium labeled Ticlopidine. Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively[1]. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively[2][3].
Quetiapine-d4 (hydrochloride) (ICI204636-d4 (hydrochloride)) is deuterium labeled Quetiapine. Quetiapine (ICI204636) is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
Pirfenidone-d5 is a deuterium labeled Pirfenidone. Pirfenidone is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone has growth-inhibitory effect and reduces TGF-β2 protein levels in human glioma cell lines. Pirfenidone also has anti-inflammatory activities[1][2][3].
Ponesimod-d4 (ACT-128800-d4) is the deuterium labeled Ponesimod (HY-10569) . Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation [3] .
Sotalol-d6 is the deuterium labeled Sotalol. Sotalol is an orally active, non-selective β-adrenergic receptor blocker. Sotalol is a potent antiarrhythmic agent that can be used for the research of pediatric arrhythmias. Sotalol blocks β-receptors, and potassium KCNH2 channels. Antiepileptic Agent[1][2][3][4].
Flecainide-d4 (acetate) is the deuterium labeled Flecainide acetate. Flecainide acetate (R-818) is a class 1C antiarrhythmic agent especially used for the management of supraventricular arrhythmia; works by blocking the Nav1.5 sodium channel in the heart, causing prolongation of the cardiac action potential[1][2].
Glycochenodeoxycholic acid-d4 is the deuterium labeled Glycochenodeoxycholic acid. Glycochenodeoxycholic acid (Chenodeoxycholylglycine) is a bile acid formed in the liver from chenodeoxycholate and glycine. It acts as a detergent to solubilize fats for absorption and is itself absorbed. Glycochenodeoxycholic acid (Chenodeoxycholylglycine) induces hepatocyte apoptosis[1][2].
Prasugrel-d4 is the deuterium labeled Prasugrel[1]. Prasugrel (PCR 4099), a thienopyridine and proagent, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation[2].
Apalutamide-d7 is deuterated labeled Apalutamide (HY-16060). Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM .
Delamanid-d4 is the deuterium labeled Delamanid. Delamanid, a newer mycobacterial cell wall synthesis inhibitor, inhibits the synthesisi of mucolic acids[1].
Tylvalosin-d9 (Acetylisovaleryltylo?sin-d9) is the deuterium labeled Tylvalosin (HY-128423A) . Tylvalosin is a third-generation macrolide, with anti-inflammatory property. Tylvalosin decreases the levels of IL-8, IL-6, IL-1β, PGE2, TNF-α and NO, and reduces the inflammatory cells recruitment and activation in mouse acute lung injury model .
Ciprofloxacin-d8 (hydrochloride) is the deuterium labeled Ciprofloxacin. Ciprofloxacin (Bay-09867) hydrochloride is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
Ropinirole-d7 (hydrochloride) is the deuterium labeled Ropinirole hydrochloride[1]. Ropinirole (SKF 101468) hydrochloride is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease[2][3].
Glasdegib-d4 (PF-04449913-d4) is deuterium labeled Glasdegib. Glasdegib (PF-04449913) is a potent and orally bioavailable smoothened inhibitor. Glasdegib (PF-04449913) binds to human SMO (amino acids 181-787) with an IC50 of 4 nM .
(R)-Oxybutynin-d10 (Aroxybutynin-d10) is deuterium labeled (R)-Oxybutynin. (R)-Oxybutynin (Aroxybutynin) is the racemic isomer of Oxybutynin and an orally active muscarinic receptor antagonist. (R)-Oxybutynin has antispasmodic, antimuscarinic, and anticholinergic activities and competitively antagonizes carbachol-induced contractions. (R)-Oxybutynin can be used to study urinary incontinence caused by neurogenic bladder dysfunction [3] .
Dapoxetine-d7 (hydrochloride) is the deuterium labeled Dapoxetine hydrochloride. Dapoxetine hydrochloride is a short-acting selective serotonin reuptake inhibitor (SSRI)[1].
Bazedoxifene-d4 is deuterium labeled Bazedoxifene. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[1][2].
Lusutrombopag-d13 is deuterium labeled Lusutrombopag. Lusutrombopag is an orally bioavailable thrombopoietin (TPO) receptor agonist, used for treatment of chronic liver disease.
Biperiden-d5 (KL 373-d5) is deuterium labeled Biperiden. Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders .
Tecovirimat-d4 (ST-246-d4) is a deuterium-labelled Tecovirimat (HY-14805). Tecovirimat is an orally bioavailable and selective compound against orthopoxviruses [including vaccinia, monkeypox, camelpox, cowpox, ectromelia (mousepox), smallpox and variola viruses]. Tecovirimat is evaluated against vaccinia, cowpox virus, ectromelia virus with EC50 values of 0.01 μM, 0.48 μM and 0.05 μM, respectively. Tecovirimat targets the orthopoxvirus protein VP37 which is necessary for membrane envelopment of intracellular mature virus particles to form enveloped virus. Tecovirimat exerts antiviral activity on the target of the cowpox virus V061 gene, which is homologous to vaccinia virus F13L, encoding a major envelope protein (p37) required for production of extracellular virus. Tecovirimat could be used in the study for orthopoxvirus-induced diseases [3] .
Teneligliptin-d8 is a deuterium labeled Teneligliptin (MP-513). Teneligliptin is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor[1].
Prasugrel-d5 is deuterium labeled Prasugrel. Prasugrel (PCR 4099), a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation[1].
Eliglustat-d4 is the deuterium labeled Eliglustat. Eliglustat is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC50 of 24 nM[1][2].
Linagliptin-d4 is deuterium labeled Linagliptin. Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM. Linagliptin-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Levocetirizine-d4 ((R)-Cetirizine-d4) is the deuterium-labeled Levocetirizine (HY-B0814) . Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptorthan (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria .
Erdosteine-d4 is a deuterium labeled Erdosteine (HY-B0289). Erdosteine has muco-modulatory, anti-bacterial, anti-inflammatory and anti-oxidant effects[1].
Diclazuril-d4 is deuterium labeled Diclazuril. Diclazuril (R-64433), a benzeneacetonitrile derivative, is a potent and orally active anticoccidial agent. Diclazuril can be used for the research of certain infectious and parasitic diseases, including coccidiosis, acute toxoplasmosis, equine protozoal pyoencephalitis (EPM) et.al[1][2].
Piracetam-d6 is deuterium labeled Piracetam. Piracetam (UCB-6215) is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders.
Meclofenamic acid-d4 is the deuterium labeled Meclofenamic acid. Meclofenamic Acid (Meclofenamate), a non-steroidal, anti-inflammatory agent, is a highly selective fat mass and obesity-associated (FTO) enzyme inhibitor. Meclofenamic Acid competes with FTO binding for the m(6)A-containing nucleic acid. Meclofenamic acid is a non-selective gap-junction blocker[1][2][3].
Ruxolitinib-d9 (INCB18424-d9) is deuterium labeled Ruxolitinib. Ruxolitinib (INCB18424) is an orally active and selective JAK1/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3 . Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy[3].
Glycocyamine-d2 is the deuterium labeled Glycocyamine. Glycocyamine (Guanidinoacetic acid), a precursor of creatine, is a replacement of dietary arginine and could support overall energy homeostasis of the bird.
Butenafine-d4 (KP363-d4) is the deuterium labeled Butenafine (HY-114518). Butenafine (KP363) is a potent and broad spectrum benzylamine antifungal agent . Butenafine inhibits fungal ergosterol biosynthesis at the point of squalene epoxidation, leading to a deficiency of the fungal cell membranes. Butenafine is effective against dermatophytes infections, such as ?tinea pedis, ?tinea cruris, tinea versicolor .
Varenicline-d4 is deuterium labeled Varenicline. Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively[1]. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment[2].
Ziprasidone-d88 is deuterium labeled Ziprasidone, which is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.
Albendazole-d7 is the deuterium labeled Albendazole. Albendazole is a broad-spectrum parasiticide with high effectiveness and low host toxicity. Albendazole is used for the research gastrointestinal parasites in humans and animals[1][2].
Elacestrant-d6 (RAD1901-d6) is a deuterated labeled Elacestrant (HY-19822). Elacestrant is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER + breast cancer cell lines both in vitro and in vivo.
Dexpanthenol-d6 is deuterium labeled D-Panthenol. D-Panthenol is the biologically-active alcohol of pantothenic acid, which leads to an elevation in the amount of coenzyme A in the cell.
Emodin-d4 is the deuterium labeled Emodin. Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction[1]. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects[2]. Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice[3].
Valsartan-d9 is deuterium labeled valsartan. Valsartan is an angiotensin II receptor antagonist and has the potential for high blood pressure and heart failure research[1].
Elacestrant-d4 (RAD1901-d4) is a deuterated labeled Elacestrant (HY-19822). Elacestrant (RAD1901) is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER + breast cancer cell lines both in vitro and in vivo.
Biperiden-d5 (hydrochloride) is the deuterium labeled Biperiden hydrochloride. Biperiden (KL 373) hydrochloride is an antiparkinsonian agent, which is the selective central M1 cholinoreceptors blocker.
Methylprednisolone-d4 is deuterium labeled Methylprednisolone. Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels[3].
Tulobuterol-d9 (hydrochloride) is the deuterium labeled Tulobuterol. Tulobuterol (C-78 free base) is a long-acting β2-adrenoceptor agonist, which reduces the frequency of exacerbations of chronic obstructive pulmonary disease and bronchial asthma. Tulobuterol is also a sympathomimetic agent used as a transdermal patch, and increases normal diaphragm muscle strength[1].
Dasatinib-d4 (BMS-354825-d4) is deuterium labeled Dasatinib. Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib also induces apoptosis and autophagy.
Methazolamide-d6 is the deuterium labeled Methazolamide. Methazolamide (L584601) is a sulfonamide derivative used as a carbonic anhydrase inhibitor with a Ki of 14 nM for human carbonic anhydrase II. Methazolamide, an intraocular pressure-lowering agent, reduces intraocular pressure elevations associated with glaucoma and other ocular disorders[1][2].
Promethazine-d6 (hydrochloride) is the deuterium labeled Promethazine hydrochloride. Promethazine hydrochloride is an orally active histamine receptor antagonist[1][2].
Licofelone-d6 is the deuterium labeled Licofelone[1]. Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC50=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins[2][3][4].
Ribociclib-d6 (hydrochloride) is a deuterium labeled Ribociclib. Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex[1].
Sildenafil-d8 is the deuterium labeled Sildenafil. Sildenafil (UK-92480) is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM[1][2].
Guaiacol-d4 is the deuterium labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
(±)-Darifenacin-d4 is deuterium labeled (±)-Darifenacin. (±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist[1].
Pemigatinib-d6 (INCB054828-d6) is deuterium labeled Pemigatinib. Pemigatinib (INCB054828) is an orally active, selective FGFR inhibitor with IC50s of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma [3].
Teneligliptin-d4 is deuterium labeled Teneligliptin. Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM[1].
Pomalidomide-d5 is deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.
Palbociclib-d4 is deuterium labeled Palbociclib. Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma [3] .
Donepezil-d4 (hydrochloride) is the deuterium labeled Donepezil hydrochloride. Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE[1]. Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity[2].
Aprocitentan-d4 is a deuterium labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is an orally active dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively. Aprocitentan is an antihypertensive agent .
Apremilast-d5 is a deuterium labeled Apremilast. Apremilast is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM[1].
Ribociclib-d8 is the deuterium labeled Ribociclib[1]. Ribociclib (LEE01) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex[2].
Itraconazole-d9 is the deuterium labeled Itraconazole[1]. Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor[2][3][4][5].
Cilnidipine-d7 is deuterium labeled Cilnidipine. Cilnidipine is a long-acting, second-generation dihydropyridine Ca2+-channel blocker on L and N-type Ca2+ channel[1][2][3][4]. Antihypertensive effects[5].
Ciprofloxacin-d8 (hydrochloride monohydrate) is the deuterium labeled Ciprofloxacin (hydrochloride monohydrate). Ciprofloxacin hydrochloride is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
Cabergoline-d6 is deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).
Ciprofloxacin-d8 is the deuterium labeled Ciprofloxacin. Ciprofloxacin (Bay-09867) is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
Fluconazole-d4 is the deuterium labeled Fluconazole. Fluconazole (UK-49858) is a triazole antifungal agent with excellent activities against a broad range of fungi, especially against Candida albicans. Fluconazole inhibits C. albicans and Candida kefyr with IC99s range from 0.20 μg/mL to 0.39 μg/mL[1].
Nemonoxacin-d4 is the deuterium labeled Nemonoxacin. Nemonoxacin (TG-873870) is an orally active and potent broad-spectrum antibiotic. Nemonoxacin shows good inhibitory activity against different species of staphylococci, streptococci, and enterococci, Neisseria gonorrhoeae, and Haemophilus influenza. Nemonoxacin can be used in the study of bacterial infections and community-acquired pneumonia[1][2][3].
Piroxicam-d4 is the deuterium labeled Piroxicam. Piroxicam (CP-16171) is a non-steroidal anti-inflammatory drugs, acts as a COX inhibitor, with IC50s of 47, 25 μM for human monocyte COX-1 and COX-2, respectively.
Debutyldronedarone-d6 (hydrochloride) is deuterium labeled Debutyldronedarone. Debutyldronedarone is a major circulating active metabolite of dronedarone (HY-A0016) in humans. Debutyldronedarone exhibits a potency that is 1/10 to 1/3 of that of the parent agent[1][2].
Didesethyl chloroquine-d4 is the deuterium labeled Didesethyl chloroquine. Didesethyl chloroquine (Bisdesethylchloroquine) is a major metabolite of the antimalarial agent Chloroquine. Didesethyl chloroquine is a potent myocardial depressant[1][2].
Valsartan-d8 is the deuterium labeled Valsartan. Valsartan (CGP 48933) is an angiotensin II receptor antagonist and has the potential for high blood pressure and heart failure research[1].
Methylprednisolone-d7 is deuterium labeled Methylprednisolone. Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels[3].
Relugolix-d6 is deuterium labeled Relugolix. Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209)[1]. Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al[2].
Bazedoxifene-d4 (acetate) is the deuterium labeled Bazedoxifene[1]. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[2][3].
Gilteritinib-d8 is deuterium labeled Gilteritinib. Gilteritinib (ASP2215) is a potent and ATP-competitive FLT3/AXL inhibitor with IC50s of 0.29 nM/0.73 nM, respectively.
Sarafloxacin-d8 (A-56620-d8) hydrochloride is the deuterium labeled Sarafloxacin hydrochloride. Sarafloxacin hydrochloride (A-56620 hydrochloride) is a quinolone antibiotic drug.
Moclobemide-d4 is deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A[1].Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
Terbinafine-d7 is the deuterium labeled Terbinafine. Terbinafine (TDT 067) is an antifungal medication used to treat fungal infections. It is a potent non-competitive inhibitor of squalene epoxidase from Candida with a Ki of 30 nM[1][2]. Terbinafine also antibacterial activity against certain Gram-positive and Gram-negative bacteria[3].
Clozapine-d8 is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors[1][2][3][4].
Moclobemide-d8 (Ro111163-d8) is the deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A .Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
Oxprenolol-d7 (hydrochloride) is the deuterium labeled Oxprenolol hydrochloride. Oxprenolol hydrochloride (Ba 39089) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle[1].
Carteolol-d9 (hydrochloride) is the deuterium labeled Carteolol hydrochloride. Carteolol hydrochloride (OPC-1085 hydrochloride) is a non-selective beta blocker used to treat glaucoma[1][2].
Mavatrep-d6 (JNJ-39439335-d6) is a deuterated labeled Mavatrep (HY-16935). Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with high affinity for hTRPV1 channels (Ki=6.5 nM). Mavatrep antagonizes capsaicin-induced Ca 2+ influx with an IC50 value of 4.6 nM. Mavatrep can be used in some studies of neuropathic pain .
Lisinopril-d5 is the deuterium labeled Lisinopril. Lisinopril (MK-521) is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks.
Pazopanib-d6 is the deuterium labeled Pazopanib. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
Atenolol-d7 is the deuterium labeled Atenolol. Atenolol ((RS)-Atenolol) is a cardioselective β1-adrenergic receptor blocker, with a Ki of 697 nM atβ1-adrenoceptor in guine pig left ventricle membrane. Atenolol can be used for the research of hypertension and angina pectoris[1][2].
Tazarotene-d8 is the deuterium labeled Tazarotene. Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris[1][2].
Filgotinib-d4 is the deuterium labeled Filgotinib. Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.
Empagliflozin-d4 is deuterium labeled Empagliflozin. Empagliflozin (BI 107730 is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor with an IC50 of 3.1 nM for human SGLT-2[1].
Tranylcypromine-d5 (hydrochloride) is a deuterium labeled (rel)-Tranylcypromine hydrochloride. Tranylcypromine hydrochloride is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. Tranylcypromine hydrochloride is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis[1][2].
Edoxaban-d6 is deuterium labeled Edoxaban. Edoxaban (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and can be used for stroke prevention. Edoxaban is also a weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10000-fold selectivity for FXa. Edoxaban has antithrombotic properties and has potential for thromboembolic diseases treatment [3].
Donepezil-d7 (hydrochloride) is the deuterium labeled Donepezil. Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively[1].
Venlafaxine-d6 (hydrochloride) is the deuterium labeled Venlafaxine hydrochloride. Venlafaxine hydrochloride (Wy 45030 hydrochloride) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant[1].
Bimatoprost-d4 is the deuterium labeled Bimatoprost. Bimatoprost is a prostaglandin analog used topically (as eye drops) to control the progression of glaucoma and in the management of ocular hypertension.
Docetaxel-d9 is the deuterium labeled Docetaxel. Docetaxel (RP-56976) is a microtubule depolymerization inhibitor, with an IC50 of 0.2 μM. Docetaxel attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel arrests the cell cycle at G2/M and leads to cell apoptosis. Docetaxel has anti-cancer activity[1][3].
Adinazolam-d5 is a deuterium labeled Adinazolam (HY-A0198). Adinazolam, a triazolobenzodiazepine, has dual anxiolytic and antidepressant activities[1].
Tezacaftor-d4 (VX-661-d4) is the deuterium-labeled Tezacaftor (HY-15448), a F508del CFTR corrector. Tezacaftor helps CFTR protein reach the cell surface .
Betaxolol-d7 (hydrochloride) is the deuterium labeled Betaxolol hydrochloride. Betaxolol Hydrochloride is a selective beta1 adrenergic receptor blocker that can be used for the research of hypertension and glaucoma.
EDTA-d12 is the deuterium labeled Ethylenediaminetetraacetic acid[1]. Ethylenediaminetetraacetic acid (EDTA) is a metal chelators (binds to metal divalent and trivalent cations including calcium), which shows activities of anticoagulant and anti-hypercalcemic. Ethylenediaminetetraacetic acid decreases the metal ion-catalyzed oxidative damage to proteins, and allows maintenance of reducing environment during protein purification. Ethylenediaminetetraacetic acid can also decrease the formation of disulfide bonds[2][3][4].
Hyodeoxycholic acid-d5 is the deuterium labeled Hyodeoxycholic acid. Hyodeoxycholic acid is a secondary bile acid formed in the small intestine by the gut flora, and acts as a TGR5 (GPCR19) agonist, with an EC50 of 31.6 µM in CHO cells.
Doxazosin-d8 is a deuterium labeled Doxazosin (UK 33274). Doxazosin is a quinazoline-derivative that selectively antagonizes postsynaptic α1 adrenergic receptors[1].
Sunitinib-d10 is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
Cobicistat-d8 (GS-9350-d8) is a deuterated version of Cobicistat (HY-10493). Cobicistat is a potent and selective inhibitor of cytochrome P450 3A (CYP3A) with IC50 values of 30-285 nM. Cobicistat is a pharmacokinetic enhancer that enhances the absorption of anti-HIV active molecules [3].
Cabergoline-d5 is the deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively)[1][2].
Itopride-d6 (hydrochloride) is deuterium labeled Itopride (hydrochloride). Itopride hydrochloride (HSR803), a gastroprokinetic Benzamide (HY-Z0283) derivative, is an inhibitor of acetylcholinesterase (AChE) and dopamine D2 receptor[1][2].
Chenodeoxycholic Acid-d9 is the deuterium labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
Dacarbazine-d6 is the deuterium labeled Dacarbazine. Dacarbazine(DTIC-Dome; DTIC) is an antineoplastic agent. It has significant activity against melanomas.
Telmisartan-d7 (BIBR 277-d7) is a deuterium labeled Telmisartan (HY-13955). Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
Ponatinib-d8 is a deuterium labeled Ponatinib. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
Flurbiprofen-d4 is deuterated labeled Flurbiprofen (HY-10582). Flurbiprofen (dl-Flurbiprofen) is a potent, orally active nonsteroidal anti-inflammatory agent (NSAIA/NSAID), with antipyretic and analgesic activities. Flurbiprofen is commonly used for the research of inflammatory diseases, including osteoarthritis and rheumatoid arthritis. Flurbiprofen is a non-selective cyclooxygenase (COX) inhibitor that can be used for the research of colorectal cancer [3].
Pranlukast-d4 is deuterium labeled Pranlukast. Pranlukast is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [3H]LTE4, [3H]LTD4, and [3H]LTC4 bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.
Imiquimod-d9 is deuterium labeled Imiquimod. Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19[1][2].
Adenosine- 15N5 (Adenine riboside- 15N5; D-Adenosine- 15N5) is the 15N labled Adenosine (HY-B0228). Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation .
L-Theanine-d5 is the deuterium labeled L-Theanine. L-Theanine (L-Glutamic Acid γ-ethyl amide）is a non-protein amino acid contained in green tea leaves, which blocks the binding of L-glutamic acid to glutamate receptors in the brain, and with neuroprotective and anti-oxidative activities. L-Theanine causes anti-stress effects via the inhibition of cortical neuron excitation by oral intake[1][2][3].
Promethazine-d4 is a deuterated-labeled promethazine (HY-B0781). Promethazine is an orally active H1 receptor and mAChR antagonist with antihistamine (H1), sedative, antiemetic, anticholinergic, and anti-motion sickness properties [3] .
Artemisinin- 13C,d4 is 13C and deuterated labeled Artemisinin (HY-B0094). Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants . Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects .
Vitamin D3- 13C5 is the deuterium labeled Vitamin D3 (HY-15398). Vitamin D3 (Cholecalciferol) is a naturally occuring form of vitamin D. Vitamin D3 induces cell differentiation and prevents proliferation of cancer cells[1][2].
L-Glutamine- 15N2,d5 is the deuterium and 15N-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells[1][2].
Resveratrol- 13C6 is the 13C-labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].
Vitamin K1- 13C6 is the 13C-labeled Vitamin K1. Vitamin K1 a naturally occurring vitamin required for blood coagulation and bone and vascular metabolism.
Adenosine- 13C10 (Adenine riboside- 13C10; D-Adenosine- 13C10) is 13C-labeled Adenosine (HY-B0228). Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation.
17(R)-Resolvin D1-d5 (17(R)-RvD1-d5) is deuterium labeled 17(R)-Resolvin D1. 17R-Resolvin D1 (17R-RvD1; AT-RvD1) is an aspirin-triggered epimer of Resolvin D1, which exhibits anti-inflammatory activity in mice and human PMNs cells . 17R-Resolvin D1 specificially inhibits TRPV3 with an IC50 of 398 nM and exhibits peripheral anti-nociceptive efficacy .
Dihomo-γ-linolenic acid-d6 (DGLA-d6) is the deuterium labeled Dihomo-γ-linolenic acid. Dihomo-γ-linolenic acid (all-cis-8,11,14-Eicosatrienoic acid) is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid attenuates atherosclerosis in the apolipoprotein E deficient mouse model system[1][2][3].
Procainamide- 13C2 hydrochloride is 13C labeled Procainamide. Procainamide hydrochloride is an antiarrhythmic agent used in the study of cardiac arrhythmias.
Dutasteride- 13C6 is the 13C labeled Dutasteride[1]. Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT[2].
D-Sorbitol- 13C6 is the 13C labeled D-Sorbitol[1]. D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and dietary supplement[2].
Adenosine- 13C5 is the 13C labeled Adenosine[1]. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation[2][3].
Pantethine- 15N2 is the 15N2 labeled Pantethine. Pantethine is an orally active lipid-lowering agent. Pantethine has anti-tumor, anti-inflammatory and anti-SARS-COV virus activities. Pantethine is also a neuroprotective agent. Pantethine can be used in the study of Alzheimer's disease, Parkinson's disease, major depression, systemic sclerosis and pantothenate kinase-related neurodegeneration [3] .
Hypoxanthine- 15N4 is the 15N labeled Hypoxanthine[1]. Hypoxanthine, a purine derivative, is a potential free radical generator and could be used as an indicator of hypoxia[2].
Deoxythymidine-5'-triphosphate- 15N2,d15 (dTTP- 15N2,d15) dilithium is deuterium and 15N labeled Deoxythymidine-5'-triphosphate (HY-138615). Deoxythymidine-5'-triphosphate (dTTP) is one of the four nucleoside triphosphates. Deoxythymidine-5'-triphosphate (dTTP) is used in the synthesis of DNA.
Pyridoxine- 13C4 (hydrochloride) is the 13C-labeled Pyridoxine (hydrochloride). Pyridoxine hydrochloride (Pyridoxol; Vitamin B6) is a pyridine derivative. Pyridoxine (Pyridoxol; Vitamin B6) exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
Topiramate-13C6 (McN 4853-13C6) is the 13C labeled isotope of Topiramate (HY-B0122). Topiramate (McN 4853) is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase[3].
Thyroxine hydrochloride- 13C6 is the 13C-labeled L-Thyroxine. L-Thyroxine (Levothyroxine; T4) is a synthetic hormone for the research of hypothyroidism. DIO enzymes convert biologically active thyroid hormone (Triiodothyronine,T3) from L-Thyroxine (T4)[1].
ATP- 15N5,d14 (Adenosine 5'-triphosphate- 15N5,d14) dilithium is deuterium and 15N labeled ATP (HY-B2176). ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation.
Vanillin- 13C6 is the 13C labeled Vanillin[1]. Vanillin (p-Vanillin) is a single molecule extracted from vanilla beans and also a popular odor used widely in perfume, food and medicine[2][3].
Rufinamide- 15N,d2 is the deuterium and 15N labeled Rufinamide[1]. Rufinamide is a new antiepileptic agent that differs structurally from other antiepileptic agents and is approved as adjunctive therapy for Lennox-Gastaut syndrome (LGS)[2][3].
2-Methoxybenzoic acid- 13C6 is the 13C-labeled 2-Methoxybenzoic acid. 2-Methoxybenzoic acid (NSC 3778) is used as an internal standard of salicylic acid and its putative biosynthetic precursors in cucumber leaves. Another known use is in the synthesis of Benextramine.
dGTP- 15N5 (2'-Deoxyguanosine-5'-triphosphate- 15N5) dilithium is 15N labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
1-PalMitoyl-2-arachidoyllecithin-d9-1 (1-Palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine-d9-1) is deuterium labeled 1-PalMitoyl-2-arachidoyllecithin. 1-Palmitoyl-2-arachidonoyl-sn-glycero-3-PC (PAPC) is a phospholipid containing palmitic acid (16:0) and arachidonic acid (20:4) at the sn-1 and sn-2 positions, respectively, that is found in biological membranes. PAPC is oxidized in vivo, and its oxidation products are involved in chronic inflammation and vascular disease. PAPC has been used to study signaling of oxidized phospholipids. Levels of PAPC are decreased in isolated human multiple myeloma cells .
NAD+- 13C5-1 is the 13C labeled NAD+[1]. NAD+ is a coenzyme composed of ribosylnicotinamide 5'-diphosphate coupled to adenosine 5'-phosphate by pyrophosphate linkage.
Ethynyl Estradiol- 13C2 is the 13C-labeled Ethynyl Estradiol. Ethynyl Estradiol-13C2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Allantoin- 13C2, 15N4 is the 13C and 15N labeled Allantoin[1]. Allantoin is a skin conditioning agent that promotes healthy skin, stimulates new and healthy tissue growth[2].
(Rac)-Rivastigmine-d6 is a labelled racemic Rivastigmine. Rivastigmine (ENA 713 free base) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease[1][2].
DL-α-Tocopherol acetate- 13C4,d6 is the deuterium and 13C labeled DL-α-Tocopherol acetate[1]. DL-α-Tocopherol acetate is a vitamin E derivative which is often included in the formulations of enteral nutrition[2][3].
Adenine- 15N5 (6-Aminopurine- 15N5; Vitamin B4- 15N5) is 15N labeled Adenine (HY-B0152). Adenine (6-Aminopurine), a purine, is one of the four nucleobases in the nucleic acid of DNA.
Adenine acts as a chemical component of DNA and RNA. Adenine also plays an important role in biochemistry involved in cellular respiration, the form of both ATP and the cofactors (NAD and FAD), and protein synthesis.
Levoglucosan-d7 is the deuterium labeled Levoglucosan. Levoglucosan (1,6-Anhydro-β-D-glucopyranose) is an anhydrosugar produced through glucan pyrolysis and is widely found in nature[1][2].
Nε,Nε,Nε-Trimethyllysine-d9 (chloride) is the deuterium labeled Nε,Nε,Nε-Trimethyllysine (chloride)[1]. Nε,Nε,Nε-Trimethyllysine chloride serves as a precursor for gut flora-dependent formation of N,N,N-trimethyl-5-aminovaleric acid (TMAVA)[2].
2'-Deoxyadenosine-5'-triphosphate- 15N5,d14 (dATP- 15N5,d14) dilithium is deuterium and 15N labeled 2'-Deoxyadenosine-5'-triphosphate (HY-136648). 2'-Deoxyadenosine-5'-triphosphate (dATP) is a nucleotide used in cells for DNA synthesis (or replication), as a substrate of DNA polymerase.
Adenine-15N5 hydrochloride hydrate (6-Aminopurine-15N5 hydrochloride hydrate) is the deuterium labeled Adenine (HY-B0152). Adenine (6-Aminopurine), a purine, is one of the four nucleobases in the nucleic acid of DNA. Adenine acts as a chemical component of DNA and RNA. Adenine also plays an important role in biochemistry involved in cellular respiration, the form of both ATP and the cofactors (NAD and FAD), and protein synthesis [3].
Adenine- 13C5 (6-Aminopurine- 13C5; Vitamin B4- 13C5) is 13C-labeled Adenine (HY-B0152). Adenine (6-Aminopurine), a purine, is one of the four nucleobases in the nucleic acid of DNA.
Adenine acts as a chemical component of DNA and RNA. Adenine also plays an important role in biochemistry involved in cellular respiration, the form of both ATP and the cofactors (NAD and FAD), and protein synthesis.
(Rac)-1,2-Dimyristoyl-sn-glycero-3-phosphocholine-d72 is deuterium labeled (Rac)-1,2-Dimyristoyl-sn-glycero-3-phosphocholine. 1,2-Dimyristoyl-sn-glycero-3-phosphocholine (DMPC) is a synthetic phospholipid used in liposomes. 1,2-Dimyristoyl-sn-glycero-3-ph
Dapsone- 13C12 is the 13C12 labeled Dapsone (HY-B0688). Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al [3] .
Cobimetinib- 13C6 (GDC-0973- 13C6; XL518- 13C6) racemate is the deuterium labeled Cobimetinib (racemate) (HY-13078) . Cobimetinib racemate (GDC-0973 racemate; XL518 racemate) is the racemate of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor .
Ethyl linoleate- 13C18 is the 13C labeled Ethyl linoleate. Ethyl linoleate inhibit the development of atherosclerotic lesions and the expression of inflammatory mediators[1].
Dabigatran- 13C6 is the 13C labeled Dabigatran[1]. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[2][3].
Riboflavin- 13C5 is the 13C-labeled Riboflavin. Riboflavin is an easily absorbed micronutrient with a key role in maintaining health in humans and other animals.
Neopterin- 13C5 (D-(+)-Neopterin- 13C5; D-erythro-Neopterin- 13C5) is the deuterium labeled Neopterin (HY-W040055) . Neopterin (D-(+)-Neopterin), a catabolic product of guanosine triphosphate (GTM), serves as a marker of cellular immune system activation .
dGTP- 15N5,d14 (2'-Deoxyguanosine-5'-triphosphate- 15N5,d14) dilithium is deuterium and 15N labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
N-Acetyl-D-glucosamine- 13C3, 15N is the 13C and 15N labeled N-Acetyl-D-glucosamine. N-Acetyl-D-Glucosamine (N-Acetyl-2-amino-2-deoxy-D-glucose) is a monosaccharide derivative of gluc[1][2].
Menaquinone-7- 13C6 is the 13C-labeled Menaquinone-7. Menaquinone-7 (Vitamin K2-7), belongs to a class of K2-vitamin homologs, is originally discovered as the anti-hemorrhagic factors[1]. Menaquinone-7 (Vitamin K2-7) is identified as the most bioactive cofactor for the carboxylation reaction of Gla-proteins [2]. Supplementation with Menaquinone-7 (Vitamin K2-7) is a pharmacological option for activating matrix Gla protein and intervening in the progression of calcific aortic valve stenosis (CAVS)[3].
Tenofovir alafenamide-d6 (GS-7340-d6) is deuterium labeled Tenofovir alafenamide. Tenofovir alafenamide (GS-7340) is an investigational oral proagent of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor .
Lansoprazole sulfone-d4 (AG-1813-d4) is the deuterium labeled Lansoprazole sulfone. Lansoprazole sulfone-d4 is an orally active and selective inhibitor of H +, K +-ATPase. Lansoprazole sulfone-d4 can significantly stimulates gastric acid secretion by inhibiting H +, K +-ATPase. Lansoprazole sulfone-d4 has potential applications in duodenal ulcer, gastric ulcer, gastroesophageal reflux disease and Zolinger Ellison disease [3].
Etiocholanolone-d2 is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2][3].
Myrcene-d6 is the deuterium labeled Myrcene. Myrcene (β-Myrcene) is a type of aromatic compound that inhibits TNFα and NF-κB activity. Myrcene has anti-invasive action, inhibits cell cycle, and leads to cancer cell apoptosis. Myrcene has strong blood protection effect, anti-inflammation, and anti-inflammatory activity [3] .
Tiludronate-d5 (sodium)mis the deuterium labeled Tiludronate disodium. Tiludronate (Tiludronic Acid) disodium, an orally active bisphosphonate, can act an osteoregulator. Tiludronate is used for the research of the metabolic bone disorders. Tiludronate is a potent inhibitor of the osteoclast vacuolar H(+)-ATPase. Antiresorptive and anti-inflammatory properties[1][2][3][4].
Sorafenib-d4 is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
Cromoglicic acid-d5 is the deuterium labeled Cromolyn[1]. Cromolyn is a mast cell stabilizer. Cromolyn has the potential for the research of bronchial asthma, allergic rhinitis, and certain allergic eye conditions such as vernal conjunctivitis, keratitis, and keratoconjunctivitis[2].
25-Hydroxycholesterol-d6 (25-OHC-d6) is the deuterium labeled 25-Hydroxycholesterol. 25-Hydroxycholesterol is a metabolite of cholesterol that is produced and secreted by macrophages in response to Toll-like receptor (TLR) activation. 25-hydroxycholesterol is a potent (EC50≈65 nM) and selective suppressor of IgA production by B cells[1][2].
5-Fluorouracil-d is the deuterium labeled 5-Fluorouracil. 5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer[1][2]. 5-Fluorouracil also inhibits HIV[3].
DPPC-d62 is the deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers[1]. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in mice[2].
Diethyl succinate-d4 is the deuterium labeled Diethyl succinate[1]. Diethyl succinate (Diethyl Butanedioate) is used at physiological pH and crosses biological membranes, incorporates into cells in tissue culture and is metabolized by the TCA cycle. Diethyl succinate is known to be non-toxic and used in fragrances and flavoring[2].
Octanoic acid-d15 is the deuterium labeled Octanoic acid. Octanoic acid (Caprylic acid) is an oily liquid with a slightly unpleasant rancid taste and used commercially in the production of esters used in perfumery and also in the manufacture of dyes.
Piperonyl butoxide-d9 is the deuterium labeled Piperonyl butoxide.Piperonyl butoxide (ENT-14250) is a pesticide synergist and food additive. Piperonyl butoxide has adverse effects on reproduction, development and behavior in mice. Piperonyl butoxide can activate c-Jun and ATF-2 in mouse hepatocytes. Piperonyl butoxide is a liver cancer carcinogen in rats and mice [3] .
Kynurenic acid-d5 is the deuterium labeled Kynurenic acid. Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8 .
CX516-d10 is the deuterium labeled CX516. CX516 (BDP 12) is an ampakine and acts as an AMPA receptor positive allosteric modulator for the research of Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI)[1].
Dolutegravir-d5 is deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2].
Deruxtecan-d5 is deuterium labeled Deruxtecan (HY-13631E). Deruxtecan is an ADC drug-linker conjugate composed of an DX-8951 derivative (DXd) and a maleimide-GGFG peptide linker, used for synthesizing DS-8201 and U3-1402.
DPPC-d66 is deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in
Alfuzosin-d7 (hydrochloride) is the deuterium labeled Alfuzosin hydrochloride. Alfuzosin hydrochloride is an α1 adrenergic receptor antagonist used to treat benign prostatic hyperplasia (BPH).
Aztreonam-d6 is deuterium labeled Aztreonam. Aztreonam (SQ-26,776) is a synthetic monocyclic beta-lactam antibiotic, which has a very high affinity for penicillin-binding protein 3 (PBP-3).
cis-Atovaquone-d4 is deuterium labeled Atovaquone. Atovaquone (Atavaquone) is a potent, selective and orally active inhibitor of the parasite’s mitochondrial cytochrome bc1 complex. Atovaquone is against human and P. falciparum cytochrome bc1 activity with IC50 values of 460 nM and 2.0 nM, respectively. Atovaquone is an antimalarial agent and has the potential for the investigation of neumocystis pneumonia, toxoplasmosis, malaria, and babesia[1][2].
Daurisoline-d2 is the deuterium labeled Daurisoline (HY-N0221). Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on hERG and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer .
Nonanoic acid-d4 is the deuterium labeled Nonanoic acid. Nonanoic acid is a naturally-occurring saturated fatty acid with nine carbon atoms. Nonanoic acid significantly reduces bacterial translocation, enhances antibacterial activity, and remarkably increases the secretion of porcine β-defensins 1 (pBD-1) and pBD-2[1].
Minodronic acid-d4 is deuterium labeled Minodronic acid. Minodronic acid (YM-529) is a third-generation bisphosphonate that directly and indirectly prevents proliferation, induces apoptosis, and inhibits metastasis of various types of cancer cells. Minodronic acid (YM-529) is an antagonist of purinergic P2X2/3 receptors involved in pain[1][2].
Ulipristal acetate-d6 is deuterium labeled Ulipristal acetate. Ulipristal acetate (CDB-2914) is an orally active, selective progesterone receptor modulator (SPRM). Ulipristal acetate stimulates the autophagic response selectively in leiomyoma cells. Ulipristal acetate has the potential for benign gynecological conditions treatment, such as uterine myoma[1][2].
Metformin-d6 hydrochloride is a deuterium labeled Metformin hydrochloride. Metformin hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin hydrochloride also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, metformin hydrochloride regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo .
Stigmasterol-d5-1 is deuterium labeled Stigmasterol. Stigmasterol is a plant sterol which has been focused on the cholesterol-lowering activity and is valued as an anti-stiffness factor in the therapy of rheumatic diseases[1].
DPPC-d75 is deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in
Suberic acid-d4 is the deuterium labeled Suberic acid[1]. Suberic acid (Octanedioic acid) is found to be associated with carnitine-acylcarnitine translocase deficiency, malonyl-Coa decarboxylase deficiency[2].
Cyfluthrin-d6 (β-Cyfluthi-d6) is deuterium labeled Cyfluthrin. Cyfluthrin is a type II pyrethroid and has effects on various insects. Cyfluthrin is a modulator of Nav1.8 sodium channels by repetitive stimulation. Cyfluthrin can be applied in agriculture,veterinary, insecticide,pyrethroid and stored product .
4-Methylanisole-d4 is the deuterium labeled 4-Methylanisole[1]. 4-Methylanisole (4-Methoxytoluene) is food flavoring agent and can be naturally found in Ylang Ylang fragrance oil[2].
Solifenacin-d5 (succinate) is deuterium labeled Solifenacin (Succinate). Solifenacin Succinate (YM905) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
Taurine-d4 is the deuterium labeled Taurine. Taurine, a sulphur-containing amino acid and an organic osmolyte involved in cell volume regulation, provides a substrate for the formation of bile salts, and plays a role in the modulation of intracellular free calcium concentration. Taurine has the ability to activate autophagy in adipocytes[1][2][3].
trans-Stilbene-d10 is the deuterium labeled trans-Stilbene[1]. trans-Stilbene ((E)-Stilbene) is used in the manufacturing of dye lasers, optical brighteners, non-steroidal synthetic estrogens[2].
D-Leucine-d10 is the deuterium labeled D-Leucine. D-Leucine is a more potent anti-seizure agent than L-leucine. D-leucine potently terminates seizures even after the onset of seizure activity. D-leucine, but not L-leucine, reduces long-term potentiation but had no effect on basal synaptic transmission in vitro[1].
Arachidic acid-d2 is the deuterium labeled Arachidic acid. Arachidonic acid (Icosanoic acid), a long-chain fatty acid, is present in all mammalian cells, typically esterified to membrane phospholipids, and is one of the most abundant polyunsaturated fatty acids present in human tissue[1][2].
Daurisoline-d11 is the deuterium labeled Daurisoline (HY-N0221). Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on hERG and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer .
4-Vinylphenol-d4 is deuterated labeled Losartan (potassium) (HY-17512A). Losartan potassium (DuP-753 potassium) is an angiotensin II receptor type 1 (AT1) antagonist, competing with the binding of angiotensin II to AT1 with an IC50 of 20 nM.
Parecoxib-d5 (sodium) is the deuterium labeled Parecoxib sodium. Parecoxib Sodium (SC 69124A) is a highly selective and orally active COX-2 inhibitor, the proagent of Valdecoxib (HY-15762). Parecoxib Sodium is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits prostaglandin (PG) synthesis. Parecoxib Sodium can be used for the relief of acute postoperative pain and symptoms of chronic inflammatory conditions such as osteoarthritis and rheumatoid arthritis in vivo[1][2].
Levocarnitine propionate-d9 (hydrochloride) (L-Propionylcarnitine-d9 (chloride)) is deuterium labeled Levocarnitine propionate (hydrochloride). Levocarnitine propionate hydrochloride (L-Propionylcarnitine chloride) is used to study diseases such as renal function deterioration, congestive heart failure, and intermittent claudication .
Homovanillic acid-d5 is the deuterium labeled Homovanillic acid. Homovanillic acid is a dopamine metabolite found to be associated with aromatic L-amino acid decarboxylase deficiency, celiac disease, growth hormone deficiency, and sepiapterin reductase deficiency.
Montelukast-d6 is the deuterium labeled Montelukast (sodium). Montelukast sodium is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (Cysltr1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage[1].
N-Arachidonylglycine-d8 is a deuterated labeled N-Arachidonylglycine . N-Arachidonylglycine (NA-Gly), a carboxylic analog of the endocannabinoid anandamide (AEA), is a GPR18 agonist (EC50 = 44.5 nM). Unlike AEA, N-Arachidonylglycine has no activity at either CB1 or CB2 receptors. N-Arachidonylglycine inhibits GLYT2 (IC50 = 5.1 μM). N-Arachidonylglycine also is an effective activator of endometrial cell migration [3].
Banoxantrone-d12 is the deuterium labeled banoxantrone. Banoxantrone is a novel bioreductive agent that can be reduced to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor.
Isobutylparaben-d4 is the deuterium labeled Isobutylparaben[1]. Isobutylparaben (Isobutyl 4-hydroxybenzoate) is a constitutive androstane receptor (CAR) activator. Isobutylparaben has a broad-spectrum antimicrobial activity and widely used in personal care products and cosmetics[2].
Moxifloxacin-d4 hydrochloride (BAY 12-8039-d4) is the hydrochloride salt form of deuterium labeled Moxifloxacin (Moxifloxacin). Moxifloxacin is an orally active antimicrobial, that can be used in the research of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia [3].
Tetrabenazine-d6 (Deutetrabenazine) is a deuterium-labled Tetrabenazine (HY-B0590), is the first deuterium approved worldwide for the research of Huntington's disease, or other hyperkinetic movement disorders .
Fosetyl-aluminum-d15 (Fosetyl-Al-d15) is the deuterium labeled Fosetyl-aluminum. Fosetyl-aluminum (Fosetyl-Al) is an active ingredient in many fungicides against downy mildew. Fosetyl-aluminum is used to control many diseases caused by Phytophthora spp. on agricultural and horticultural crops .
Climbazole-d4 is the deuterium labeled Climbazole. Climbazole (BAY-e 6975) is a potent antifungal agent. Climbazole also is a potent inducer of rat hepatic cytochrome P450[2].
Prednisolone acetate-d8 is the deuterium labeled Prednisolone acetate. Prednisolone acetate (Prednisolone 21-acetate) is an adrenal cortico hormones, with anti-inflammatory, anti-allergic and immune suppressive effects.
Docosanoic acid-d2 (Behenic acid-d2) is deuterium labeled Docosanoic acid (HY-W013049).
Docosanoic acid (Behenic acid) is a long-chain saturated fatty acid. Docosanoic acid inhibits the double-stranded DNA (dsDNA) binding activity of p53 DNA binding domain, with a Kd of 12 nM. Docosanoic acid has low bioavailability and can increase cholesterol in humans [3].
Taurocholic acid-d4 (sodium) is the deuterium labeled Taurocholic acid. Taurocholic acid (N-Choloyltaurine) is a bile acid involved in the emulsification of fats.
Lignoceric acid-d47 is the deuterium labeled Lignoceric acid. Lignoceric acid (Tetracosanoic acid) is a 24-carbon saturated (24:0) fatty acid, which is synthesized in the developing brain. Lignoceric acid is also a by-product of lignin production. Lignoceric acid can be used for Zellweger cerebro‐hepato‐renal syndrome and adrenoleukodystrophy research[1][2].
Abiraterone acetate-d4 is the deuterium labeled Abiraterone acetate. Abiraterone acetate (CB7630) is an oral, potent, selective, and irreversible inhibitor of CYP17A1 with antiandrogen activity. Abiraterone acetate is a proagent form of Abiraterone (CB7598).
SAH-d4 is the deuterium labeled SAH. SAH (S-Adenosylhomocysteine) is an amino acid derivative and a modulartor in several metabolic pathways. It is an intermediate in the synthesis of cysteine and adenosine[1]. SAH is an inhibitor for METTL3-METTL14 heterodimer complex (METTL3-14) with an IC50 of 0.9 µM[2].
Ospemifene-d4 is a deuterium labeled Ospemifene. Ospemifene is a selective and orally active estrogen receptor modulator for the prevention of osteoporosis with IC50 values of 827 nM and 1633 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene has bone-sparing, antitumor, and cholesterol-lowering effects[1][2].
Cefadroxil-d4 (hydrate) is the deuterium labeled Cefadroxil. Cefadroxil is a broad-spectrum antibiotic of the cephalosporin type, effective in Gram-positive and Gram-negative bacterial infections.
Azelaic acid-d14 is the deuterium labeled Azelaic acid[1]. Azelaic acid is an organic compound produced by the ozonolysis of oleic acid;component of a number of hair and skin conditioners[2][3].
4-Methylanisole-d7 is the deuterium labeled 4-Methylanisole[1]. 4-Methylanisole (4-Methoxytoluene) is food flavoring agent and can be naturally found in Ylang Ylang fragrance oil[2].
Tricaine-d5 (methanesulfonate) is the deuterium labeled Tricaine-d5 methanesulfonate. Tricaine methanesulfonate (MS-222) is a commonly used agent that can suppress or relieve pain. agent for immobilization of aquatic species. Tricaine methanesulfonate, the most widely used agent that can suppress or relieve pain. in fish, has been shown to induce embryotoxic effects in zebrafish .
Phenylglyoxylic acid-d5 (Benzoylformic acid-d5) is a deuterium labeled Phenylglyoxylic acid (HY-W010255). Phenylglyoxylic acid (Benzoylformic acid) is a metabolite of ethylbenzene and styrene (EB/S) and can be used as a biomarker of exposure to EB/S in human .
Rivaroxaban-d4 is a deuterium labeled Rivaroxaban. Rivaroxaban is a highly potent，selective and direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM)[1][2].
Theobromine-d6 is the deuterium labeled Theobromine. Theobromine is a methylxanthine found in cacao beans which can inhibit adenosine receptor A1 (AR1) signaling.
1-Phenylpyrrole-d9 (N-Phenylpyrrole-d9) is the deuterium labeled 1-Phenylpyrrole (HY-124891). 1-Phenylpyrrole (N-Phenylpyrrole) has dual fluorescent properties. 1-Phenylpyrrole displays a single band in nonpolar solvents and a second red-shifted fluorescent band in polar solvents .
1-Eicosanol-d41 is the deuterium labeled 1-Eicosanol[1]. 1-Eicosanol is a natural compound with antioxidant activity isolated from Hypericum carinatum[2].
Octanoic acid-d2 is the deuterium labeled Octanoic acid. Octanoic acid (Caprylic acid) is an oily liquid with a slightly unpleasant rancid taste and used commercially in the production of esters used in perfumery and also in the manufacture of dyes.
Oxcarbazepine-d8-1 is a deuterium of Oxcarbazepine. Oxcarbazepine is a sodium channel blocker . Oxcarbazepine significantly inhibits glioblastoma cell growth and induces apoptosis or G2/M arrest in glioblastoma cell lines . Oxcarbazepine-d8-1 has anti-cancer and anticonvulsant effects .
(S)-Verapamil-d7 (hydrochloride) is a deuterium labeled (S)-Verapamil hydrochloride. (S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells[1][2].
Ethyl acetoacetate-d5 is the deuterium labeled Ethyl acetoacetate[1]. Ethyl acetoacetate (Ethyl acetylacetate) is an ester widely used as an intermediate in the synthesis of many varieties of compounds[2][3][4]. Ethyl acetoacetate is an inhibitor of bacterial biofilm[5].
L-Arginine-d7 (hydrochloride) is the deuterium labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
Arbutin-d4 is deuterium labeled Arbutin. Arbutin (β-Arbutin) is a competitive inhibitor of tyrosinase in melanocytes, with Kiapp values of 1.42 mM for monophenolase; 0.9 mM for diphenolase. Arbutin is also used as depigmenting agents[1]. Arbutin is a natural polyphenol isolated from the bearberry plant Arctostaphylos uvaursi, possesses with anti-oxidant, anti-inflammatory and anti-tumor properties[2][3].
Octanoic acid-d5 is the deuterium labeled Octanoic acid[1]. Octanoic acid (Caprylic acid) is an oily liquid with a slightly unpleasant rancid taste and used commercially in the production of esters used in perfumery and also in the manufacture of dyes.
Uridine-d12 (β-Uridine-d12) is the deuterium labeled Uridine (HY-B1449). Uridine is a glycosylated pyrimidine-analog containing uracil attached to a ribose ring (or more specifically, aribofuranose) via a β-N1-glycosidic bond .
Tolcapone-d4 is the deuterium labeled Tolcapone. Tolcapone (Ro 40-7592) is a selective, orally active and powerful mixed (peripheral and central) COMT inhibitor with an IC50 of 773 nM in the liver[1]. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis[2]. Tolcapone induces oxidative stress leading to apoptosis and inhibition of tumor growth in neuroblastoma[3].
Nifedipine-d4 is the deuterium labeled Nifedipine. Nifedipine (BAY-a-1040) is a potent calcium channel blocker and agent of choice for cardiac insufficiencies.
Docosanoic acid-d43 (Behenic acid-d43) is the deuterium labeled Docosanoic acid (HY-W013049). Docosanoic acid (Behenic acid) is a long-chain saturated fatty acid. Docosanoic acid inhibits the double-stranded DNA (dsDNA) binding activity of p53 DNA binding domain, with a Kd of 12 nM. Docosanoic acid has low bioavailability and can increase cholesterol in humans [3].
Taurochenodeoxycholic acid-d5 (sodium) is the deuterium labeled Taurochenodeoxycholic acid sodium. Taurochenodeoxycholic acid sodium salt (12-Deoxycholyltaurine sodium salt) is one of the main bioactive substances of animals' bile acid. Taurochenodeoxycholic acid induces apoptosis and shows obvious anti-inflammatory and immune regulation properties[1][2].
DSG Crosslinker-d4 is the deuterium labeled DSG Crosslinker. Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Methyl Salicylate-d4 is the deuterium labeled Methyl Salicylate[1]. Methyl Salicylate (Wintergreen oil) is a topical analgesic and anti-inflammatory agent. Also used as a pesticide, a denaturant, a fragrance ingredient, and a flavoring agent in food and tobacco products[2]. A systemic acquired resistance (SAR) signal in tobacco[3]. A topical nonsteroidal anti-inflammatory agent (NSAID). Methyl salicylate lactoside is a COX inhibitor[5].
Isradipine-d6 is the deuterium labeled Isradipine[1]. Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease[2][3][4].
Homovanillic acid-d2 is the deuterium labeled Homovanillic acid. Homovanillic acid is a dopamine metabolite found to be associated with aromatic L-amino acid decarboxylase deficiency, celiac disease, growth hormone deficiency, and sepiapterin reductase deficiency.
Ethyl palmitate-d31 is the deuterium labeled Ethyl palmitate. Ethyl palmitate, a fatty acid ethyl ester (FAEE), shows a marked preference for the synthesis of ethyl palmitate and ethyl oleate over other FAEEs in human subjects after ethanol consumption. Ethyl palmitate is used as a hair- and skin-conditioning agent[1].
Succinic acid-d6 is the deuterium labeled Succinic acid. Succinic acid is an intermediate product of the tricarboxylic acid cycle, as well as one of fermentation products of anaerobic metabolism.
N,N-Dimethylacetamide-d6 is the deuterium labeled N,N-Dimethylacetamide[1]. N,N-Dimethylacetamide (DMAc) is an inexpensive, common aprotic organic solvent[2].
5-Methoxytryptamine-d4 (O-Methylserotonin-d4) is the deuterium labeled 5-Methoxytryptamine (HY-W015169). 5-Methoxytryptamine, a metabolite of Melatonin, is a nonselective 5-HT receptor agonist. 5-Methoxytryptamine has no affinity for the 5-HT3 receptor. 5-Methoxytryptamine is also a potent antioxidant and has radioprotective action [3].
trans-Stilbene-d12 is the deuterium labeled trans-Stilbene[1]. trans-Stilbene ((E)-Stilbene) is used in the manufacturing of dye lasers, optical brighteners, non-steroidal synthetic estrogens[2].
Mefatinib-d6 free base (Mifanertinib-d6) is the deuterium labeled Mefatinib. Mefatinib is a potent tyrosine kinase inhibitor with antineoplastic activity .
Vortioxetine-d4 (Lu AA 21004-d4) is the deuterium labeled Vortioxetine (HY-15414). Vortioxetine is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial agonist of 5-HT1B (Ki: 15 nM, 33 nM) .
Daurisoline-d5 is the deuterium labeled Daurisoline (HY-N0221). Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on hERG and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer .
Sitafloxacin-d4 (DU6859a-d4) is deuterium labeled Sitafloxacin. Sitafloxacin (DU6859a) is a potent, orally active fluoroquinolone antibiotic. Sitafloxacin shows antichlamydial activity and antibacterial activities against a broad range of gram-positive and gram-negative bacteria, including anaerobic bacteria, as well as against atypical pathogens. Sitafloxacin can be used for the research of respiratory tract infection and urinary tract infection .
Taurochenodeoxycholic acid-d4 (sodium) is the deuterium labeled Taurochenodeoxycholic acid. Taurochenodeoxycholic acid (12-Deoxycholyltaurine) is one of the main bioactive substances of animals' bile acid. Taurochenodeoxycholic acid induces apoptosis and shows obvious anti-inflammatory and immune regulation properties[1][2].
Cletoquine-d4-1 is the deuterium labeled Cletoquine. Cletoquine (Desethylhydroxychloroquine) is a major active metabolite of Hydroxychloroquine. Cletoquine is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune diseases treatment[1][2].
Taurochenodeoxycholic acid-d9 (sodium) is the deuterium labeled Taurochenodeoxycholic acid sodium. Taurochenodeoxycholic acid sodium salt (12-Deoxycholyltaurine sodium salt) is one of the main bioactive substances of animals' bile acid. Taurochenodeoxycholic acid induces apoptosis and shows obvious anti-inflammatory and immune regulation properties[1][2].
Prosulfocarb-d7 (S-Benzyl dipropylthiocarbamate-d7) is deuterium labeled Prosulfocarb. Prosulfocarb is a herbicide with a rapidly growing use trend. Prosulfocarb is used in winter cereals to help address the problem of increasing biotic resistance of weeds to certain pesticides. Environmental and food effects of prosulfocarb have been observed, and its transfer pattern from target crops to non-target areas has been studied. The volatility effect of prosulfocarb is an important factor explaining the inefficiency of isolated area contamination and marginal protection against residue spread .
Tolcapone-d7 is a deuterium labeled Tolcapone. Tolcapone is a selective, potent and orally active COMT inhibitor. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis and protect against extracellular toxicity induced by the aggregation of both proteins in PC12 cells[1][2].
Ramatroban-d4 is deuterium labeled Ramatroban. Ramatroban is a selective thromboxane A2 (TxA2, IC50=14 nM) antagonist, which also antagonizes CRTH2 (IC50=113 nM) by inhibiting PGD2 binding.
Fluvastatin-d6 (sodium) is deuterium labeled Fluvastatin sodium. Fluvastatin sodium (XU 62320) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM.
DPPC-d71 is deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in
Butamben-d9 is the deuterium labeled Butamben. Butamben (Butyl 4-aminobenzoate) results in long-lasting relief from pain, without impairing motor function or other sensory functions[1][2].
Trihydroxycholestanoic acid-d5 (Coprocholic acid-d5) is deuterium labeled Trihydroxycholestanoic acid. Trihydroxycholestanoic acid is an endogenous metabolite present in Blood that can be used for the research of Zellweger Syndrome, Refsum Disease, D Bifunctional Protein Deficiency and Infantile Refsum Disease [3][3] .
Arachidic acid-d4 is the deuterium labeled Arachidic acid. Arachidonic acid (Icosanoic acid), a long-chain fatty acid, is present in all mammalian cells, typically esterified to membrane phospholipids, and is one of the most abundant polyunsaturated fatty acids present in human tissue[1][2].
Tazarotenic acid-d6 is deuterium labeled Tazarotenic acid. Tazarotenic acid is the metabolite of Tazarotene. Tazarotenic acid binding to retinoic acid receptors (RARs) is the probable molecular target of retinoid action. Tazarotenic acid has the potential for the research of warty dyskeratoma [3].
Docosanoic acid-d4 (Behenic acid-4) is deuterium labeled Docosanoic acid (HY-W013049). Docosanoic acid (Behenic acid) is a long-chain saturated fatty acid. Docosanoic acid inhibits the double-stranded DNA (dsDNA) binding activity of p53 DNA binding domain, with a Kd of 12 nM. Docosanoic acid has low bioavailability and can increase cholesterol in humans [3].
Suberic acid-d12 is the deuterium labeled Suberic acid[1]. Suberic acid (Octanedioic acid) is found to be associated with carnitine-acylcarnitine translocase deficiency, malonyl-Coa decarboxylase deficiency[2].
Banoxantrone-d12 (dihydrochloride) is the deuterium labeled Banoxantrone dihydrochloride. Banoxantrone is a novel bioreductive agent that can be reduced to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor.
Nisoldipine-d6 is the deuterium labeled Nisoldipine. Nisoldipine(BAY-k 5552; Sular) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with an IC50 of 10 nM.
Finerenone-d5 (BAY 94-8862-d5) is deuterium labeled Finerenone. Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
Lansoprazole sulfide-d4 is a deuterium labeled Lansoprazole Sulfide. Lansoprazole Sulfide is an active metabolite of the proton pump inhibitor Lansoprazole. Lansoprazole Sulfide is an orally active anti-TB (Mycobacterium tuberculosis) agent with IC50 values of 0.59 µM intracellularly and 0.46 µM in broth[1].
Mexiletine-d6 (hydrochloride) is a deuterium labeled Mexiletine hydrochloride (KOE-1173 hydrochloride). Mexiletine hydrochloride, a Class IB antianhythmic, is a non-selective voltage-gated sodium channel blocker[1].
Gliquidone-d6 is deuterium labeled Gliquidone. Gliquidone (AR-DF 26) is an anti-diabetic agent in the sulfonylurea class, used in the treatment of diabetes mellitus type 2.
Benazepril-d5 hydrochloride is deuterium labeled Benazepril hydrochloride. Benazepril hydrochloride is an orally active angiotensin-converting enzyme (ACE) inhibitor to reduce angiotensin-II production. Benazepril hydrochloride inhibits oxidative stress and inhibits apoptosis by the PI3K/Akt signaling pathway. In addition, Benazepril hydrochloride improves diabetic nephropathy and decreases proteinuria. Benazepril hydrochloride can be used in the study of hypertension, heart failure and diabetic nephropathy [3].
4',7-Dimethoxyisoflavone-d6 (Dimethoxydaidzein-d6) is the deuterium labeled 4',7-Dimethoxyisoflavone (HY-N2145). 4',7-Dimethoxyisoflavone is isolated from the leaves of Albizzia lebbeck, which shows antifungal activity .
Tempol-d17 is the deuterium labeled Tempol[1]. Tempol is a general superoxide dismutase (SOD)-mimetic agent that efficiently neutralizes reactive oxygen species (ROS)[2][3].
Tetrahydrocurcumin-d6 is a deuterium labeled Tetrahydrocurcumin. Tetrahydrocurcumin is a Curcuminoid which displays inhibitory activity for CYP2C9 and CYP3A4[1].
Phenytoin-d10 is the deuterium labeled Phenytoin. Phenytoin (5,5-Diphenylhydantoin) is a potent Voltage-gated Na+ channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice[1][2].
(±)-Carnitine-d9 (chloride) is the deuterium labeled (±)-Carnitine chloride. (±)-Carnitine chloride exists in two isomers, known as D and L. L-carnitine plays an essential role in the β-oxidation of fatty acids and also shows antioxidant, and anti-inflammatory activities.
Clofibric acid-d4 is the deuterium labeled Clofibric acid. Clofibric acid (Chlorofibrinic acid), the pharmaceutically active metabolite of lipid regulators Clofibrate, Etofibrate and Etofyllinclofibrate, is a PPARα agonist which exhibits hypolipidemic effects. Clofibric acid also is an herbicide[1][2][3].
Arachidic acid-d39 is the deuterium labeled Arachidic acid. Arachidonic acid (Icosanoic acid), a long-chain fatty acid, is present in all mammalian cells, typically esterified to membrane phospholipids, and is one of the most abundant polyunsaturated fatty acids present in human tissue[1][2].
Nitrendipine-d5 is the deuterium labeled Nitrendipine. Nitrendipine (BAY-E-5009), an analogue of Nifedipine (HY-B0284), is a dihydropyridine calcium channel blocker with vasodilator action. Nitrendipine has antihypertensive effect[1][2][3][4].
(Rac)-Rotigotine-d7 (hydrochloride) is deuterium labeled (Rac)-Rotigotine (hydrochloride). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
Asoxime-d4 (dichloride) is the deuterium labeled Asoxime dichloride. Asoxime dichloride (HI-6) is an antagonist to acetylcholine receptors (AChRs) including the nicotinic receptor, α7 nAChR. Asoxime dichloride involves in modulating immunity response. Asoxime dichloride (HI-6) can be used as an antigen and improves vaccination efficacy in the nervous system[1].
trans-Stilbene-d2 is the deuterium labeled trans-Stilbene[1]. trans-Stilbene ((E)-Stilbene) is used in the manufacturing of dye lasers, optical brighteners, non-steroidal synthetic estrogens[2].
Hydroxy Itraconazole-d8 is the deuterium labeled Hydroxy Itraconazole. Hydroxy Itraconazole is an active metabolite of Itraconazole (ITZ), which is a triazole antifungal agent.
Salmeterol-d5 is a deuterated labeled Salmeterol . Salmeterol (GR33343X) is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively .
Deuruxolitinib, a deuterated Ruxolitinib (HY-50856), is an orally active JAK1 and JAK2 inhibitor. Deuruxolitinib demonstrates significant hair regrowth effects. Deuruxolitinib can be used for the research of alopecia areata .
N4-Acetylsulfamethoxazole-d4 is the deuterium labeled N4-Acetylsulfamethoxazole. N4-Acetylsulfamethoxazole (Acetylsulfamethoxazole) is a metabolite of Sulfamethoxazole (HY-B0322). Sulfamethoxazole is a sulfonamide bacteriostatic antibiotic, used for bacterial infections[1].
(-)-Huperzine A-d4 hydrochloride is deuterated labeled (-)-Huperzine A (HY-17387). (-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease [3] .
SAR405838-d10 (MI-77301-d10) is the deuterium labeled SAR405838 (HY-18986). SAR405838 (MI-77301), an analog of MI-773, is a highly potent and selective MDM2-p53 interaction inhibitor. SAR405838 binds to MDM2 with a Ki of 0.88 nM. SAR405838 induces apoptosis and has potent antitumor activity [3].
Berberine-d6 (chloride) is the deuterium labeled Berberine chloride. Berberine chloride is an alkaloid that acts as an antibiotic. Berberine chloride induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Antineoplastic properties[1].
Muscarine-d9 (iodide) is the deuterium labeled Muscarine iodide. Muscarine ((+)-Muscarine) iodide is a toxin that can stimulate the parasympathetic nervous system. Muscarine iodide is a prototype muscarinic acetylcholine receptor agonist[1][2].
Tazarotenic acid-d8 (AGN 190299-d8) is the deuterium labeled Tazarotenic acid (HY-101108). Tazarotenic acid is the metabolite of Tazarotene (HY-15388) .
Vortioxetine-d6 (Lu AA 21004-d6) is the deuterium labeled Vortioxetine (HY-B1490A). Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial agonist of 5-HT1B (Ki: 15 nM, 33 nM) .
DPPC-d13 is deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in
N,N-Dimethylacetamide-d9 is the deuterium labeled N,N-Dimethylacetamide[1]. N,N-Dimethylacetamide (DMAc) is an inexpensive, common aprotic organic solvent[2].
N6-Benzyladenosine-d5 (Benzyladenosine-d5) is deuterium labeled N6-Benzyladenosine. N6-Benzyladenosine is an adenosine receptor agonist, has a cytoactive activity. N6-Benzyladenosine arrests cell cycle at G0/G1 phase and induces cell apoptosis. N6-Benzyladenosine also exerts inhibitory effect on T. gondii adenosine kinase and glioma [3] .
Isradipine-d7 is deuterated labeled Isradipine (HY-B0233). Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease [3].
Genistein-d4 is the deuterium labeled Genistein. Genistein, a soy isoflavone, is a multiple tyrosine kinases (e.g., EGFR) inhibitor which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis[1][2].
Deruxtecan-d4 is deuterium labeled Deruxtecan (HY-13631E). Deruxtecan is an ADC drug-linker conjugate composed of an DX-8951 derivative (DXd) and a maleimide-GGFG peptide linker, used for synthesizing DS-8201 and U3-1402.
Dihydrodiol-Ibrutinib-d5 is the deuterium labeled Dihydrodiol-Ibrutinib (HY-100659). Dihydrodiol-Ibrutinib is a dihydrodiol active metabolite of Ibrutinib (HY-10997), has inhibitory activity towards BTK approximately 15 times lower than that of ibrutinib .
DPPC-d4 is deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in m
Nonanoic acid-d17 is the deuterium labeled Nonanoic acid. Nonanoic acid is a naturally-occurring saturated fatty acid with nine carbon atoms. Nonanoic acid significantly reduces bacterial translocation, enhances antibacterial activity, and remarkably increases the secretion of porcine β-defensins 1 (pBD-1) and pBD-2[1].
DPPC-d9 is the deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers[1]. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in mice[2].
Rimsulfuron-d6 is deuterium labeled Rimsulfuron. Rimsulfuron (DPX-E9636) is a sulfonylurea herbicide for postemergence use in maize to control grasses and some broadleaf weeds[1][2].
DL-Dipalmitoylphosphatidylcholine-d62 is deuterium labeled DL-Dipalmitoylphosphatidylcholine. DL-Dipalmitoylphosphatidylcholine (DL-DPPC) is a biochemical reagent .
(R)-Verapamil-d7 (hydrochloride) is a deuterium labeled (R)-Verapamil hydrochloride. (R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer agents[1][2].
Ciclopirox-d11 is the deuterium labeled Ciclopirox. Ciclopirox (HOE296b) is a synthetic antifungal agent that can be used for superficial mycoses reseaech. Ciclopirox olamine has a very broad spectrum of activity and inhibits dermatophytes, yeasts, molds, and many Gram-positive and Gram-negative species pathogenic[1].
N6-Methyladenosine- 13C4 (6-Methyladenosine- 13C4; N-Methyladenosine- 13C4) is 13C-labeled N6-Methyladenosine (HY-N0086). N6-Methyladenosine is the most prevalent internal (non-cap) modification present in the messenger RNA (mRNA) of all higher eukaryotes. N6-Methyladenosine can modifies viral RNAs and has antiviral activities.
Pregnenolone- 13C2,d2 is the deuterium and 13C labeled Pregnenolone (HY-B0151). Pregnenolone is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[1][2][3][4].
Dihydrouracil- 13C4, 15N2 is the 13C and 15N labeled Dihydrouracil[1]. Dihydrouracil (5,6-Dihydrouracil), a metabolite of Uracil, can be used as a marker for identification of dihydropyrimidine dehydrogenase (DPD)-deficient[2][3].
Exemestane- 13C,d2 is 13C and deuterated labeled Exemestane (HY-13632). Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research .
ATP- 13C10, 15N5 is the 13C and 15N labeled ATP[1]. ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation[2][3].
Mitotane- 13C6 is the 13C labeled Mitotane . Mitotane (2,4′-DDD), an isomer of DDD and derivative of dichlorodiphenyltrichloroethane (DDT), is an antineoplastic agent, can be used to research adrenocortical carcinoma. Mitotane exert its adrenocorticolytic effect at least in part through lipotoxicity induced by intracellular free cholesterol (FC) accumulation. Mitotane can have direct pituitary effects on corticotroph cells. Mitotane can induce CYP3A4 gene expression via steroid and xenobiotic receptor (SXR) activation, and has agent-agent interactions [3] .
Uridine-13C9,15N2 (β-Uridine-13C9,15N2) is 13C and 15N labeled Uridine (HY-B1449). Uridine is a glycosylated pyrimidine-analog containing uracil attached to a ribose ring (or more specifically, aribofuranose) via a β-N1-glycosidic bond .
5-Fluorouracil- 13C4, 15N2 is the 13C and 15N labeled 5-Fluorouracil[1]. 5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer[2][3]. 5-Fluorouracil also inhibits HIV[4].
Cytidine-d2-1 is the deuterium labeled Cytidine. Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catech
Ethyl Paraben- 13C6 (Ethyl parahydroxybenzoate- 13C6) is 13C labeled Ethylparaben. Ethylparaben is the ethyl ester of paraben and is used as an antifungal preservative and food additive .
Folic acid-13C6 is a deuterated labeled Folic acid . Folic acid (Vitamin B9) is a orally active essential nutrient from the B complex group of vitamins. Folic acid shows antidepressant-like effect. Folic acid sodium reduces the risk of neonatal neural tube defects. Folic acid can be used to the research of megaloblastic and macrocytic anemias due to folic deficiency [3] .
L-Ascorbic acid- 13C6 is the 13C-labeled L-Ascorbic acid. L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor[1][2][3]. L-Ascorbic acid exhibits anti-cancer effects through the generation of reactive oxygen species (ROS) and selective damage to cancer cells[4].
Hydrochlorothiazide- 15N2, 13C,d2 is 15N and deuterated labeled Hydrochlorothiazide (HY-B0252). Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect [3].
rU Phosphoramidite- 13C2,d1 (DMT-2'O-TBDMS-rU phosphoramidite- 13C2,d1) is deuterium and 13C-labeled rU Phosphoramidite (HY-W048482). rU Phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
Folic acid- 13C5 is the 13C-labeled Folic acid. Folic acid (Vitamin M; Vitamin B9) is a B vitamin; is necessary for the production and maintenance of new cells, for DNA synthesis and RNA synthesis.
Ornidazole- 13C2, 15N2 is the 13C, 15N labeled Ornidazole. Ornidazole(Ro 7-0207) is a 5-nitroimidazole derivative with antiprotozoal and antibacterial properties against anaerobic bacteria.
Zearalenone- 13C18 (Mycotoxin F2- 13C18; Toxin F2- 13C18) is the 13C labeled Zearalenone (HY-103447) . Zearalenone is a mycotoxin produced mainly by fungi belonging to the genus Fusarium in foods and feeds. Possess oestrogenic activity in pigs, cattle and sheep, with low acute toxicity. Causes precocious development of mammae and other estrogenic effects in young gilts [3].
L-Arginine- 13C6, 15N4 (hydrochloride) is the 13C- and 15N-labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
Uridine 5'-monophosphate- 15N2,d11 (5'-?Uridylic acid- 15N2,d11) dilithium is deuterium and 15N labeled Uridine 5'-monophosphate (HY-101981). Uridine 5'-monophosphate (5'-?Uridylic acid), a monophosphate form of UTP, can be acquired either from a de novo pathway or degradation products of nucleotides and nucleic acids in vivo and is a major nucleotide analogue in mammalian milk.
2-Methoxyestradiol- 13C6 is the 13C-labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa[1][2][3][4][5][6].
Mitotane- 13C12 (2,4′-DDD- 13C12) is 13C labeled Mitotane. Mitotane (2,4′-DDD), an isomer of DDD and derivative of dichlorodiphenyltrichloroethane (DDT), is an antineoplastic agent, can be used to research adrenocortical carcinoma. Mitotane exert its adrenocorticolytic effect at least in part through lipotoxicity induced by intracellular free cholesterol (FC) accumulation. Mitotane can have direct pituitary effects on corticotroph cells. Mitotane can induce CYP3A4 gene expression via steroid and xenobiotic receptor (SXR) activation, and has agent-agent interactions [3][3] .
Propyl paraben- 13C6 (Propyl parahydroxybenzoate- 13C6) is 13C labeled Propylparaben. Propylparaben (Propyl parahydroxybenzoate) is an antibacterial preservative that can be produced by plants and bacteria. Propylparaben is commonly used in cosmetics, pharmaceuticals and foods. Propylparaben disrupts follicular growth and steroidogenic function by altering cell cycle, apoptosis and steroidogenic pathways. Propylparaben also reduced sperm count and motility in rats [3] .
β-Caryophyllene- 13C,d2 is 13C and deuterated labeled trans,trans-2,4-Decadienal (HY-W013627). trans,trans-2,4-Decadienal is a lipid peroxidation product of linolieic acid .
2-Deoxy-D-glucose- 13C6 (2-DG- 13C6) is 13C labeled 2-Deoxy-D-glucose. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase .
13,14-Dihydro-15-keto prostaglandin D2-d4 (DK-PGD2-d4) is deuterium labeled 13,14-Dihydro-15-keto prostaglandin D2. 13, 14-Dihydro-15-keto prostaglandin D2 (DK-PGD2) is a PGD2 metabolite formed by the 15-hydroxyl PGDH pathway. 13, 14-Dihydro-15-keto prostaglandin D2 is a selective agonist for the DP2 receptor. 13, 14-Dihydro-15-keto prostaglandin D2 can inhibit ion flux in canine colonic mucosa preparation .
α-Hydroxyglutaric acid- 13C5 (sodium) is the 13C labeled α-Hydroxyglutaric acid sodium[1]. α-Hydroxyglutaric acid (2-Hydroxyglutarate) sodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid sodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases[2].
13,14-Dihydro-15-keto prostaglandin D2-d9 (DK-PGD2-d9) is deuterium labeled 13,14-Dihydro-15-keto prostaglandin D2. 13, 14-Dihydro-15-keto prostaglandin D2 (DK-PGD2) is a PGD2 metabolite formed by the 15-hydroxyl PGDH pathway. 13, 14-Dihydro-15-keto prostaglandin D2 is a selective agonist for the DP2 receptor. 13, 14-Dihydro-15-keto prostaglandin D2 can inhibit ion flux in canine colonic mucosa preparation .
1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d4 is deuterium labeled 1,2-Distearoyl-sn-glycero-3-phosphorylcholine. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine (1,2-Distearoyl-sn-glycero-3-PC; DSPC) is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-glyc
1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d9 is deuterium labeled 1,2-Distearoyl-sn-glycero-3-phosphorylcholine. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine (1,2-Distearoyl-sn-glycero-3-PC; DSPC) is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-glyc
L-Valine- 13C5, 15N,d8 is the deuterium, 13C-, and 15-labeled L-Valine. L-Valine is one of 20 proteinogenic amino acids. L-Valine is an essential amino acid[1].
D-(+)-Trehalose-13C12 is a 13C isotope labeled version of D-(+)-Trehalose (HY-N1132). D-(+)-Trehalose,which is widespread, can be used as a food ingredient and pharmaceutical excipient .
1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d74 is deuterium labeled 1,2-Distearoyl-sn-glycero-3-phosphorylcholine. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine (1,2-Distearoyl-sn-glycero-3-PC; DSPC) is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-gly
Guanosine triphosphate- 13C10, 15N5 (tetraammonium) is the 13C and 15N labeled Guanosine triphosphate tetraammonium[1]. Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19[2].
1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d70 is the deuterium labeled 1,2-Distearoyl-sn-glycero-3-phosphorylcholine. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine (1,2-Distearoyl-sn-glycero-3-PC; DSPC) is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine is used to synthesize liposomes, and is the lipid component in the lipid nanoparticle (LNP) system[1][2].
Adenosine monophosphate- 13C10, 15N5 (AMP- 13C10, 15N5) disodium is 13C and 15N-labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction [3].
1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d13 is deuterium labeled 1,2-Distearoyl-sn-glycero-3-phosphorylcholine. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine (1,2-Distearoyl-sn-glycero-3-PC; DSPC) is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-gly
1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d79 is deuterium labeled 1,2-Distearoyl-sn-glycero-3-phosphorylcholine. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine (1,2-Distearoyl-sn-glycero-3-PC; DSPC) is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-gly
L-Thyroxine- 13C6-1 (Levothyroxine- 13C6-1; T4- 13C6-1) is a 13C labeled L-Thyroxine (HY-18341). L-Thyroxine (Levothyroxine; T4) is a synthetic hormone for the research of hypothyroidism. DIO enzymes convert biologically active thyroid hormone (Triiodothyronine,T3) from L-Thyroxine (T4) .
p-Anisic acid- 13C6 is the 13C-labeled p-Anisic acid. p-Anisic acid (4-Methoxybenzoic acid) is one of the isomers of anisic acid, with anti-bacterial and antiseptic properties[1].
L-Valine- 13C5, 15N,d2 is the deuterium, 13C-, and 15-labeled L-Valine. L-Valine is one of 20 proteinogenic amino acids. L-Valine is an essential amino acid[1].
Imidazole- 15N2 (Glyoxaline- 15N2) is 15N labeled Imidazole. Imidazole (Glyoxaline; 1,3-Diaza-2,4-cyclopentadiene) is a heterocyclic aromatic compound. Imidazole bearing molecules have been used as corrosion, acetylcholinesterase (AChEI) and xanthine oxidase (XO) inhibitors, performing biological activities such as antifungal, antituberculosis, anti-inflammatory, antioxidant, and analgesic, amongst many others. Imidazole inhibits the enzymatic conversion of the endoperoxides (PGG2 and PGH2) to thromboxane A2 by platelet microsomes. Imidazole derivatives exhibits inhibition on SARS-CoV-2 3CL Pro enzyme, which is promising for research in the field of Alzheimer’s disease, gout, COVID-19 and thrombo-embolic disease [3] .
1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d83 is deuterium labeled 1,2-Distearoyl-sn-glycero-3-phosphorylcholine. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine (1,2-Distearoyl-sn-glycero-3-PC; DSPC) is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine is used to synthesize liposomes, and is the lipid component in the lipid nanoparticle (LNP) system[1][2].
LysoPC(14:0/0:0)-d7 (14:0 Lyso PC-d7) is deuterium labeled LysoPC(14:0/0:0). LysoPC(14:0/0:0) is a lysophospholipid (LyP). It is a monoglycerophospholipid in which a phosphorylcholine moiety occupies a glycerol substitution site. LysoPC(14:0/0:0) has potent antispasmodic effect .
Lamivudine-13C,15N2,d2 (BCH-189-13C,15N2,d2) is a 13C, 15N, and deuterium labeled Lamivudine (HY-B0250). Lamivudine is an orally active and blood-brain barrier permeable nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine inhibits HIV reverse transcriptase 1 and 2 and hepatitis B virus (HBV) reverse transcriptase [3] .
Adenosine monophosphate- 13C10, 15N5(AMP- 13C10, 15N5) is the 13C-labeled and 15N-labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction [3].
Talazoparib- 13C,d4 is 13C and deuterated labeled Talazoparib (HY-16106). Talazoparib is an orally active PARP 1/2 inhibitor with Ki values of 1.2 nM and 0.87 nM for inhibiting PARP1 and PARP2 enzymatic activities, respectively. Has anti-tumor activity.
Thymidine-5'-monophosphate- 13C10, 15N2 (disodium) is the 13C and 15N labeled Thymidine-5'-monophosphate disodium salt[1]. Thymidine-5'-monophosphate disodium salt is an endogenous metabolite.
Mirogabalin-13C2,d1 (Mixture of Diastereomers) is a C13 and deuterium labeled Mirogabalin. Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS .
5'-Methylthioadenosine- 13C6 is the 13C-labeled 5'-Methylthioadenosine. 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis[1]. 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis[2].
Eliglustat-d15 (tartrate) is the deuterium labeled Eliglustat. Eliglustat tartrate is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC50 of 24 nM.
Vitamin D4-d5 is the deuterium labeled Vitamin D4. Vitamin D4 (22-Dihydroergocalciferol) is a Vitamin D derived from fungi. The precursor of Vitamin D4 is 22,23-dihydroergosterol[1].
(R)-Carvedilol-d4 is deuterium labeled (R)-Carvedilol. (R)-Carvedilol ((R)-BM 14190), the R-enantiomer of Carvedilol, is a non-selective β/α-1 blocker. (R)-Carvedilol exerts protection against the vascular or cardiac toxicity of Doxorubicin (DOX)[1].
Palmitoyl serinol-d5 is the deuterium labeled Palmitoyl serinol[1]. Palmitoyl serinol (N-Palmitoyl serinol) is an analog of the endocannabinoid N-palmitoyl ethanolamine (PEA). Palmitoyl serinol improves the epidermal permeability barrier in both normal and inflamed skin[2][3].
Sphingosine-1-phosphate-d7 is the deuterium labeled Sphingosine-1-phosphate. Sphingosine-1-phosphate (S1P) is an agonist of S1P1-5 receptors and a ligand of GPR3, GPR6 and GPR12. Sphingosine-1-phosphate is an intracellular second messenger and mobilizes Ca2+ as an extracellular ligand for G protein-coupled receptors[1]. Sphingosine-1-phosphate is an important lipid mediator generated from Sphingomyelin (HY-113498) or other membrane phospholipids[2].
Methyl cinnamate-d7 is deuterated labeled Cinnamyl Alcohol (HY-Y0078). Cinnamyl Alcohol is an active component from chestnut flower, inhibits increased PPARγ expression, with anti-obesity activity .
Cholestenone-d7 is deuterium labeled Cholestenone. Cholestenone (4-Cholesten-3-one), the intermediate oxidation product of cholesterol, is metabolized primarily in the liver. Cholestenone is highly mobile in membranes and influences cholesterol flip-flop
Elacestrant-d4-1 is the deuterium labeled Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively .
Sildenafil (citrate)-d8 is the deuterium labeled Sildenafil citrate[1]. Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 5.22 nM.
7-Ethoxyresorufin-d5 is deuterium labeled 7-Ethoxyresorufin. 7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase[1][2].
Oxcarbazepine-d4-1 is deuterium labeled Oxcarbazepine. Oxcarbazepine is a sodium channel blocker[1]. Oxcarbazepine significantly inhibits glioblastoma cell growth and induces apoptosis or G2/M arrest in glioblastoma cell lines[2]. Anti-cancer and anticonvulsant effects[2][3].
Resolvin D3-d5 is the deuterium labeled Resolvin D3. Resolvin D3 (RvD3) is a docosahexaenoic acid (DHA) derived mediator. Resolvin D3 is dysregulated in arthritis and reduces arthritic inflammation[1][2].
Azilsartan mepixetil-d5 (QR-01019-d5) is deuterium labeled Azilsartan mepixetil. Azilsartan mepixetil is the antagonist of angiotensin II receptor. Azilsartan mepixetil has stronger and longer blood pressure effect, more abvious and longer lasting heart rate lowering effect and high safety. Azilsartan mepixetil achieves ideal protective effect for heart and kidney functions. Azilsartan mepixetil has the potential for the research of hypertension, chronic heart failure and diabetic nephropathy (extracted from patent CN107400122A) .
Melatonin-d4 is deuterium labeled Melatonin. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Antioxidative and anti-inflammatory properties [3]. Melatonin is a selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation .
(S)-Carvedilol-d4 is deuterium labeled (S)-Carvedilol. (S)-Carvedilol, the S-enantiomer of Carvedilol, is a non-selective β/α-1 blocker. (S)-Carvedilol exerts protection against the vascular or cardiac toxicity of Doxorubicin (DOX)[1].
Guaiacol-d4-1 is the deuterium labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
Vilanterol-d4 (trifenatate) is deuterium labeled Vilanterol (trifenatate). Vilanterol trifenatate (GW642444 trifenatate) is a long-acting β2-adrenoceptor (β2-AR) agonist with inherent 24-hour activity. The pEC50s for β2-AR, β1-AR and β3-AR are 10.37, 6.98 and 7.36, respectively.
Tridecanoic acid-d25 is the deuterium labeled Tridecanoic acid. Tridecanoic acid (N-Tridecanoic acid), a 13-carbon medium-chain saturated fatty acid, can serve as an antipersister and antibiofilm agent that may be applied to research bacterial infections. Tridecanoic acid inhibits Escherichia coli persistence and biofilm formation[1].
Folinic acid-d4-1 (Leucovorin-d4-1) calcium hydrate is deuterated labeled Folinic acid (HY-17556). Folinic acid (Leucovorin) is a biological folic acid and is generally administered along with Methotrexate (MTX) (HY-14519) as a rescue agent to decrease MTX-induced toxicity.
Mono(3-carboxypropyl) phthalate-d4 (MCPP-d4) is a deuterium labeled Mono(3-carboxypropyl) phthalate (HY-133673). Mono(3-carboxypropyl) phthalate (MCPP) is a metabolite of Di-n-octyl phthalate. Di-n-octyl phthalate (DnOP) is a plasticizer used in polyvinyl chloride plastics, cellulose esters, and polystyrene resins .
Fingolimod-d4 is the deuterium labeled Fingolimod. Fingolimod (FTY720 free base) is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant[1].
Melatonin-d7 is the deuterium labeled Melatonin (HY-B0075). Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties [3]. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation . Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress .
(Rac)-Valsartan-d9 is deuterium labeled Valsartan. Valsartan (CGP 48933) is an angiotensin II receptor antagonist and has the potential for high blood pressure and heart failure research[1].
1,4-Dibromobenzene-d4 is a deuterium labeled 1,4-Dibromobenzene. 1,4-Dibromobenzene is used as a fumigant and as a chemical intermediate for pharmaceuticals. Inhalation exposure gives rise to dizziness and chokingwhereas contact with skin or eye produces inflammation and burning in humans[1].
Hippuric acid-d2 is the deuterium labeled Hippuric acid. Hippuric Acid (2-Benzamidoacetic acid), an acyl glycine produced by the conjugation of benzoic acid and glycine, is a normal component in urine as a metabolite of aromatic compounds from food.
Tridecanoic acid-d2 is the deuterium labeled Tridecanoic acid. Tridecanoic acid (N-Tridecanoic acid), a 13-carbon medium-chain saturated fatty acid, can serve as an antipersister and antibiofilm agent that may be applied to research bacterial infections. Tridecanoic acid inhibits Escherichia coli persistence and biofilm formation[1].
Brexpiprazole S-oxide-d8 is a deuterium labeled Brexpiprazole S-oxide. Brexpiprazole S-oxide is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM[1][2][3].
N-Desmethyl Selegiline-dd5 hydrochloride is the deuterium labeled N-Desmethyl Selegiline hydrochloride[1]. N-Desmethyl Selegiline-d5 hydrochloride is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Methyl paraben-d4 is the deuterium labeled Methyl Paraben[1]. Methyl Paraben, isolated from the barks of Tsuga dumosa the methyl ester of p-hydroxybenzoic acid, is a standardized chemical allergen. Methyl Paraben is a stable, non-volatile compound used as an antimicrobial preservative in foods, agents and cosmetics. The physiologic effect of Methyl Paraben is by means of increased histamine release, and cell-mediated immunity[2].
Degarelix-d7 (FE 200486-d7 free base) is deuterium labeled Degarelix. Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist.
2-Phenylglycine-d5 is the deuterium labeled 2-Phenylglycine. 2-Phenylglycine (DL-α-Phenylglycine) is a metabolite in breast milk during the W2 to W4 lactation period[1].
4-Hydroxypropranolol-d7 is the deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol. 4-Hydroxypropranolol hydrochlorid is of comparable potency to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties[1][2][3].
Leukotriene B4-d5 (LTB4-d5) is deuterium labeled Leukotriene B4. Leukotriene B4 (LTB4) is known as one of the most potent chemoattractants and activators of leukocytes and is involved in inflammatory diseases. Leukotriene B4 is also an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs [3] .
(E)-4-Hydroxytamoxifen-d5 ((E)-Afimoxifene-d5) is the deuterium labeled (E)-4-Hydroxytamoxifen. (E)-4-Hydroxytamoxifen ((E)-Afimoxifene), the less active isomer of (Z)-4-hydroxytamoxifen, is an estrogen receptor modulator.
Methyl tetradecanoate-d27 is the deuterium labeled Methyl myristate. Methyl myristate is a saturated fatty acid methyl ester obtained from the esterification of myristic acid. Methyl myristate shows a high melanin induction in B16F10 melanoma[1].
Docosahexaenoic acid ethyl ester-d5 is the deuterium labeled Docosahexaenoic acid ethyl ester. Docosahexaenoic acid ethyl ester (Ethyl docosahexaenoate) is a 90% concentrated ethyl ester of docosahexaenoic acid manufactured from the microalgal oil. Docosahexaenoic acid ethyl ester enhances 6-hydroxydopamine-induced neuronal damage by induction of lipid peroxidation in mouse striatum. Docosahexaenoic acid (DHA) is a key component of the cell membrane, and its peroxidation is inducible due to the double-bond chemical structure. Docosahexaenoic acid has neuroprotective effects[1][2].
Pimozide-d4-1 is the deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5[1][2][3][4].
Indole-3-acetyl glutamate-d4 (IAGlu-d4) is deuterium labeled Indole-3-acetyl glutamate. Indole-3-acetyl glutamate (IAGlu) is a derivative of the plant hormone indole-3-acetic acid (IAA). As a conjugated form of IAA, Indole-3-acetyl glutamate involves in the transport, storage, and homeostatic regulation of IAA within the plant. Indole-3-acetyl glutamate can be used for research into the effects of plant hormones on the growth and development of plants .
Simvastatin acid-d6 (ammonium)mis the deuterium labeled Simvastatin acid ammonium. Simvastatin ammonium is an active metabolite of simvastatin lactone mediated by CYP3A4/5 in the intestinal wall and liver (pKa=5.5). Simvastatin ammonium reduces indoxyl sulfate-mediated reactive oxygen species and modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene[1].
(±)-Darifenacin-d4 (hydrobromide) is deuterium labeled (±)-Darifenacin. (±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist[1].
PIPES-d18 is the deuterium labeled PIPES[1]. PIPES (1,4-Piperazinediethanesulfonic acid) is an important component of PIPES buffer agent used in biochemistry[2].
(Rac)-Mirabegron-d5 is a deuterium labeled (Rac)-Mirabegron. (Rac)-Mirabegron is the racemate of Mirabegron. Mirabegron is a selective β3-adrenoceptor agonist[1].
Lipoxin A4-d5 is the deuterium labeled Lipoxin A4. Lipoxin A4 (LXA4), an endogenous lipoxygenase-derived eicosanoid mediator, has potent dual pro-resolving and anti-inflammatory properties[1]. Lipoxin A4 inhibits proliferation and inflammatory cytokine/chemokine production of human epidermal keratinocytes (NHEKs) associated with the ERK1/2 and NF-kB pathways[2]. Lipoxin A4 inhibits serum amyloid A (SAA)-mediated IL-8 release with an IC50 value of 25.74 nM[3].
Tiotropium-d6 (bromide) is deuterium labeled Tiotropium (Bromide). Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
Resolvin D1-d5 is the deuterium labeled Resolvin D1. Resolvin D1 (RvD1), an endogenous pro-resolving mediator of inflammation, is derived from omega-3 docosahexaenoic acid during the resolution phase of acute inflammation. Resolvin D1 blocks proinflammatory neutrophil migration by regulating actin polymerization, reduces TNF-α–mediated inflammation in macrophages, and enhances phagocytosis of apoptotic cells by macrophages[1][2].
4-Hydroxypropranolol-d7 (hydrochloride) is a deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol, with potency comparable to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties[1][2][3].
Leukotriene E4-d5 is the deuterium labeled Leukotriene E4. Leukotriene E4 (LTE4) is produced by the action of dipeptidase on LTD4. Leukotriene E4 is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A). Leukotriene E4 accumulates in both plasma and urine and urinary excretion of Leukotriene E4 is most often used as an indicator of asthma.
Triclocarban-d4 is the deuterium labeled Triclocarban. Triclocarban (3,4,4′-Trichlorocarbanilide), a broad spectrum antibacterial compound, is widely used in a broad range of applications such as the production of soaps, skin creams, toothpastes and deodorants. Triclocarban is a potential endocrine-disrupting chemical with the capacity to modulate androgen and estrogen activities as well as other hormone-mediated biological processes[1][2][3].
(R)-Pioglitazone-d1 ((R)-U 72107-d1) is a stabilized and deuterated R-enantiomer of pioglitazone, exhibiting pharmacological properties that are beneficial for NASH treatment, including modulation of mitochondrial function, non-steroidal anti-inflammatory effects, and glucose-lowering capabilities.
L-Histidine-d5 (hydrochloride hydrate) is the deuterium labeled L-Histidine hydrochloride hydrate. L-Histidine hydrochloride hydrate (H-His-OH.HCl.H2O) is an endogenous metabolite.
Latanoprost ethyl amide-d4 (Lat-NEt-d4) is deuterium labeled Latanoprost ethyl amide. Latanoprost ethyl amide (Lat-NEt) is a latanoprost analog in which the C-1 carboxyl group has been modified to an N-ethyl amide. Prostaglandin esters have been shown to have ocular hypotensive activity.1 Prostaglandin N-ethyl amides were recently introduced as alternative prostaglandin ocular hypotensive prodrugs. Although it has been claimed that prostaglandin ethyl amides are not converted to the free acids in vivo, studies in our laboratories have shown that bovine and human corneal tissue converts the N-ethyl amides of various prostaglandins to the free acids with a conversion rate of about 2.5 μg/g corneal tissue/hr. Lat-NEt would be expected to show the typical intraocular effects of Latanoprost free acid, but with the much slower hydrolysis pharmacokinetics of the prostaglandin N-amides .
Mindeudesivir (JT001; VV116; GS-621763-d1) hydrobromide is a deuterated version of Remdesivir (HY-104077), a highly orally active nucleoside antiviral against SARS-CoV-2 and respiratory syncytial virus (RSV). Mindeudesivir hydrobromide retains the antiviral activity of Remdesivir against COVID-19, and is the first domestically produced deuterium targeting the COVID-19 .
Bendamustine-d4 is the deuterium labeled Bendamustine. Bendamustine is a DNA cross-linking agent that causes DNA breaks, with alkylating and antimetabolite properties.
Gemfibrozil-d6-1 (CI-719-d6-1) is the deuterium labeled Gemfibrozil (HY-B0258). Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively .
GS-621763-d1 is the deuterium labeled GS-621763 (HY-145119) . GS-621763, an orally bioavailable proagent of GS-441524, shows antiviral activity against SARS-CoV-2 pathogenesis in mice .
Resolvin D2-d5 is the deuterium labeled Resolvin D2. Resolvin D2 is a metabolite of docosahexaenoic acid (DHA), with anti-inflammatory, anti-infective activities. Resolvin D2 is a potent regulator of leukocytes and controls microbial sepsis. Resolvin D2 is a remarkably potent inhibitor of TRPV1 (IC50 = 0.1 nM) and TRPA1 (IC50 = 2 nM) in primary sensory neurons[1][2][3].
Asymmetric dimethylarginine-d7 (hydrochloride hydrate) is the deuterium labeled Asymmetric dimethylarginine. Asymmetric dimethylarginine is an endogenous inhibitor of nitric oxide synthase (NOS), and functions as a marker of endothelial dysfunction in a num
4-Methylanisole-d7-1 is the deuterium labeled 4-Methylanisole[1]. 4-Methylanisole (4-Methoxytoluene) is food flavoring agent and can be naturally found in Ylang Ylang fragrance oil[2].
Venlafaxine-d6-1 is deuterium labeled Venlafaxine. Venlafaxine (Wy 45030) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant[1].
11-Oxo etiocholanolone-d5 is the deuterium labeled 11-Oxo etiocholanolone. 11-Oxo etiocholanolone (11-Ketoetiocholanolone) is a metabolite of Etiocholanolone. Etiocholanolone is the excreted metabolite of testosterone and has anticonvulsant activity[1][2][3].
4-Methylpentanoic acid-d12 is the deuterium labeled 4-Methylpentanoic acid. 4-Methylpentanoic acid (Isocaproic Acid) is a Short chain fatty acid (SCFA)[1].
Umeclidinium-d5 (bromide) is the deuterium labeled Umeclidinium bromide. Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.
Bethanechol-d6 (chloride) is the deuterium labeled Bethanechol chloride. Bethanechol chloride (Carbamyl-β-methylcholine chloride), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system[1].
Prostaglandin D2-d4 is the deuterium labeled Prostaglandin D2. Prostaglandin D2 (PGD2) is one of the major PGs actively produced in the brain of various mammals[1]. Prostaglandin D2 is one of the most potent endogenous sleep promoting substances[2]. PGD2 plays a protective role by suppressing inflammation[3].
(rel)-Lopinavir-d8 ((rel)-ABT-378-d8) is the deuterium labeled Lopinavir (HY-14588) . Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity [3]. Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
DL-dithiothreitol-d10-1 is the deuterated form of DL-dithiothreitol. DL-dithiothreitol (DTT) is a strong reductant with anti-disulfidptosis activity. DL-dithiothreitol is oxidized to form a stable six-membered ring with an internal disulfide bond .
Ezetimibe-d4-1 is deuterium labeled Ezetimibe. Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
o-Phenanthroline-d8 is the deuterium labeled o-Phenanthroline. o-Phenanthroline (1,10-Phenanthroline), a metal chelator, prevents the induction of chromosomal aberrations in streptozotocin-treated cells. o-Phenanthroline (1,10-Phenanthroline) forms a red chelate with Fe2+ that absorbs maximally at 510 nm. o-Phenanthroline (1,10-Phenanthroline) is also a MMP inhibitor[1][2].
Brexpiprazole-d8-1 (OPC-34712-d8-1) is the deuterium labeled Brexpiprazole (HY-15780) . Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM) [3].
Meropenem-d6-1 (SM 7338-d6-1) is the deuterium labeled Meropenem. Meropenem (SM 7338) is a carbapenem antibiotic with broad-spectrum antibacterial activity. Meropenem has activity against susceptible and resistant N. gonorrhoeae (MIC value of 0.02-0.06 mg/mL), H. influenzae (MIC value of 0.03-0.12 mg/mL), and H. ducreyi (MIC value of 0.015-0.12 mg/mL) .
Delamanid-d4-1 is deuterated labeled Delamanid.Delamanid, a newer mycobacterial cell wall synthesis inhibitor, inhibits the synthesisi of mucolic acids .
Sudan I-d5 is a the deuterated Sudan I. Sudan I is a diazo-conjugate red dye and can be used as an additive to products such as oils, solvents or polishes. Sudan I inhibits growth of bacterial strains Clostridium perfringens and L. rhamnosus[1].
1-Octanol-d2-1 is deuterated labeled Cinnamyl acetate (HY-N7125). Cinnamyl acetate has a wide application in the flavor and fragrance industry . Cinnamyl acetate is a new broad spectrum antibacterial agent .
Sacubitril-d4 hemicalcium salt is the deuterium labeled Sacubitril hemicalcium salt (HY-15407A). Sacubitril hemicalcium salt is a potent NEP inhibitor with an IC50 of 5 nM [3] .
Sarafloxacin-d8 (hydrochloride trihydrate) is the deuterium labeled Sarafloxacin hydrochloride trihydrate. Sarafloxacin hydrochloride trihydrate is a quinolone antibiotic compound[1][2].
Amprenavir-d4-1 is deuterium labeled Amprenavir. Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.09 μM.
Hippuric acid-d5 is the deuterium labeled Hippuric acid. Hippuric Acid (2-Benzamidoacetic acid), an acyl glycine produced by the conjugation of benzoic acid and glycine, is a normal component in urine as a metabolite of aromatic compounds from food.
Adenosine monophosphate-d12 (AMP-d12) dilithium is deuterium labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction [3].
Hydroxy Bosentan-d6 is deuterium labeled Hydroxy bosentan. Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver. Ro 48-5033 assists BOS pharmacologically, retaining 10%-20% activities[1].
Bendamustine-d8 is the deuterium labeled Bendamustine[1]. Bendamustine (SDX-105 free base), a purine analogue, is a DNA cross-linking agent. Bendamustine activates DNA-damage stress response and apoptosis. Bendamustine has potent alkylating, anticancer and antimetabolite properties[2].
rac-Trandolapril-d5 (rac-RU44570-d5) is deuterium labeled Trandolapril. Trandolapril (RU44570) is a nonsulfhydryl proagent that is hydrolysed to the active diacid Trandolaprilat. Trandolapril is an orally administered angiotensin converting enzyme (ACE) inhibitor that has been used in the treatment of hypertension and congestive heart failure (CHF), and after myocardial infarction (MI) .
Umeclidinium-d10 (bromide) is the deuterium labeled Umeclidinium bromide. Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.
Cholestenone-d5 is the deuterium labeled Cholestenone. Cholestenone (4-Cholesten-3-one), the intermediate oxidation product of cholesterol, is metabolized primarily in the liver. Cholestenone is highly mobile in membranes and influences cholesterol flip-flop and efflux. Cholestenone may cause long-term functional defects in cells[1][2][3].
4-(Trifluoromethyl)aniline-d4 is deuterium labeled 4-(Trifluoromethyl)aniline. 4-(Trifluoromethyl)aniline is a DYRK1A and DYRK1B kinase inhibitor with IC50s of 54.84 nM and 186.40 nM, respectively[1].
Prostaglandin D2-d9 is the deuterium labeled Prostaglandin D2. Prostaglandin D2 (PGD2) is one of the major PGs actively produced in the brain of various mammals[1]. Prostaglandin D2 is one of the most potent endogenous sleep promoting substances[2]. PGD2 plays a protective role by suppressing inflammation[3].
Bimatoprost-d5 is a deuterium labeled Bimatoprost. Bimatoprost is a prostaglandin analog and is a topical hypotensive agent frequently used for treating ocular hypertension and glaucoma. Bimatoprost also has an antiadipogenic effect[1][2].
Tridecanoic acid-d9 is the deuterium labeled Tridecanoic acid. Tridecanoic acid (N-Tridecanoic acid), a 13-carbon medium-chain saturated fatty acid, can serve as an antipersister and antibiofilm agent that may be applied to research bacterial infections. Tridecanoic acid inhibits Escherichia coli persistence and biofilm formation[1].
Pemetrexed-d5 (disodium) is the deuterium labeled Pemetrexed disodium. Pemetrexed disodium (LY231514 disodium) is an antifolate, the Kis of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively[1].
Amlodipine-d4 (besylate) is the deuterium labeled Amlodipine besylate. Amlodipine besylate (Amlodipine benzenesulfonate), an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure and cancer[1][2][3].
Dxd-d5 is a deuterium labeled Dxd. Dxd is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a) [1].
Desloratadine-d4 hydrobromide is deuterated labeled Desloratadine (HY-B0539). Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities .
Sumatriptan-d6 succinate is the deuterium labeled Sumatriptan succinate. Sumatriptan succinate is an orally active 5-HT1 receptor agonist with Kis of 17 nM, 27 nM and 100 nM for 5-HT1D, 5-HT1B and 5-HT1A receptors, respectively. Sumatriptan succinate can be used for migraine headache research [3].
Simvastatin acid-d9 ammonium is deuterated labeled Simvastatin acid ammonium (HY-119695A). Simvastatin acid (Tenivastatin) ammonium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid ammonium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid ammonium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
Prostaglandin D1-d4 (PGD1-d4) is deuterium labeled Prostaglandin D1. Prostaglandin D1 is a prostanoid which causes contractile and relaxant on isolated human pial arteries, it is also an inhibitor of ADP-induced platelet aggregation with an IC50 value of 320 ng/ml. Prostaglandin D1 can be used for metabolic research .
Docetaxel-d5 (trihydrate) is the deuterium labeled Docetaxel (Trihydrate). Docetaxel Trihydrate (RP-56976 Trihydrate) is an antineoplastic agent and inhibits microtubule depolymerization with an IC50 value of 0.2 μM[1]. Docetaxel Trihydrate is a semisynthetic analog of taxol and attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel Trihydrate arrests the cell cycle at G2/M and leads to cell apoptosis[1][3].
N-Desethyl Sunitinib-d5 (hydrochloride) is a deuterated labeled N-Desethyl Sunitinib . N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively .
N-Desmethyl Pimavanserin-d9 hydrochloride (AC-279-d9 hydrochloride) is the deuterium labeled N-Desmethyl Pimavanserin (HY-135392). N-Desmethyl Pimavanserin is the active metabolite of Pimavanserin. Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC50 and pKd of 8.73 and 9.3, respectively .
Lurasidone-d8-1 (hydrochloride) is deuterium labeled Lurasidone (Hydrochloride). Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM .
Hydroxy Bosentan-d4 is deuterium labeled Hydroxy bosentan. Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver. Ro 48-5033 assists BOS pharmacologically, retaining 10%-20% activities[1].
22-Hydroxy Mifepristone-d6 is the deuterium labeled 22-Hydroxy Mifepristone[1]. 22-Hydroxy Mifepristone-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Kinetin riboside-d5 (N6-Furfuryladenosine-d5) is the deuterium labeled Kinetin riboside (HY-101055). Kinetin riboside, a cytokinin analog, can induce apoptosis in cancer cells. It inhibits the proliferation of HCT-15 cells with an IC50 of 2.5 μM .
Donepezil-d5 is deuterium labeled Donepezil. Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively[1].
Norethindrone acetate-d8 is the deuterium labeled Norethindrone acetate. Norethindrone acetate is a female hormone used for the research of endometriosis[1]. Norethindrone acetate-d8 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Miconazole-d5 (nitrate) is the deuterium labeled Miconazole. Miconazole (R18134) is an imidazole antifungal agent. Miconazole also has antibacterial effects[2].
Ipratropium-d7 (bromide)eis the deuterium labeled Ipratropium bromide. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with binding IC50 values of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma[1][2][3].
Paroxetine-d6-1 is a deuterated labeled Paroxetine . Paroxetine, a phenylpiperidine derivative, is a potent and selective serotonin reuptake inhibitor (SSRI). Paroxetine is a very weak inhibitor of norepinephrine (NE) uptake but it is still more potent at this site than the other SSRIs .
Benzyl benzoate-d12 is the deuterium labeled Benzyl benzoate[1]. Benzyl benzoate (Benzoic acid benzyl ester) is a fragrance ingredient in cosmetic products. Benzyl benzoate can be used for the research of Scabies and Demodex-associated inflammatory skin conditions[2][3][4].
L-Glutamine- 13C5, 15N2 is the 13C- and 15N-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells .
Uridine triphosphate- 15N2 (UTP- 15N2 dilithium; Uridine 5'-triphosphate- 15N2) dilithium is 15N labeled Uridine triphosphate (HY-107372). Uridine triphosphate (UTP;Uridine 5'-triphosphate) is a nucleotide that regulates the functions of the pancreas in endocrine and exocrine secretion, proliferation, channels, transporters, and intracellular signaling under normal and disease states.
5-Methyltetrahydrofolic acid- 13C5 is the 13C-labeled 5-Methyltetrahydrofolic acid. 5-Methyltetrahydrofolic acid (5-Methyl THF) is a biologically active form of folic acid. 5-Methyltetrahydrofolic acid is a methylated derivate of tetrahydrofolate. 5-Methyltetrahydrofolic acid is the predominant natural dietary folate and the principal form of folate in plasma and cerebrospinal fluid[1].
p,p'-DDE- 13C12 is 13C labeled p,p'-DDE. p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent androgen receptor antagonist, with an IC50 of 5 μM and a Ki of 3.5 μM .
Deoxythymidine-5'-triphosphate- 13C10, 15N2 (dTTP- 13C10, 15N2) dilithium is 13C and 15N-labeled Deoxythymidine-5'-triphosphate (HY-138615). Deoxythymidine-5'-triphosphate (dTTP) is one of the four nucleoside triphosphates. Deoxythymidine-5'-triphosphate (dTTP) is used in the synthesis of DNA.
DL-Lysine- 13C6, 15N2 hydrochloride ((±)-2,6-Diaminocaproic acid- 13C6, 15N2 hydrochloride) is 13C and 15N-labeled DL-Lysine (HY-B2236). DL-Lysine is a racemic mixture of the D-Lysine and L-Lysine. Lysine is an α-amino acid that is used in the biosynthesis of proteins.
Uridine triphosphate- 13C9 (UTP- 13C9 dilithium; Uridine 5'-triphosphate- 13C9) dilithium is 13C-labeled Uridine triphosphate (HY-107372). Uridine triphosphate (UTP;Uridine 5'-triphosphate) is a nucleotide that regulates the functions of the pancreas in endocrine and exocrine secretion, proliferation, channels, transporters, and intracellular signaling under normal and disease states.
Guanosine 5'-diphosphate- 13C10, 15N5 (GDP- 13C10, 15N5) dilithium is 13C and 15N-labeled Guanosine 5'-diphosphate (HY-113066). Guanosine 5'-diphosphate (GDP) is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K + channel. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Guanosine 5'-diphosphate can be used in the research of inflammation, such as anemia of inflammation (AI).
2'-Deoxyguanosine 5'-monophosphate- 13C10, 15N5 (disodium) is the 13C and 15N labeled 2'-Deoxyguanosine 5'-monophosphate disodium[1]. 2'-Deoxyguanosine 5'-monophosphate disodium (5′-dGMP disodium) is a mononucleotide having guanine as the nucleobase. 2'-Deoxyguanosine 5'-monophosphate disodium is a nucleic acid guanosine triphosphate (GTP) derivative[2].
4,4'-Sulfonyldiphenol- 13C12 (Bisphenol S- 13C12) is 13C labeled 4,4'-Sulfonyldiphenol. 4,4'-Sulfonyldiphenol (Bisphenol S; Bis(4-hydroxyphenyl) sulfone) is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Calcitonin- 13C6, 15N4 (salmon) (Salmon calcitonin- 13C6, 15N4) TFA is 13C and 15N-labeled Calcitonin (salmon) (HY-P0090). Calcitonin (salmon) , a calcium regulating hormone, is a dual-action amylin and calcitonin receptor agonist, could stimulate bone formation and inhibit bone resorption .
Trifluridine- 13C, 15N2 is the 13C and 15N labeled Trifluridine[1]. Trifluridine (Trifluorothymidine;5-Trifluorothymidine;TFT) is an irreversible thymidylate synthase inhibitor, and thereby suppresses DNA synthesis. Trifluridine is an antiviral agent for herpes simplex virus (HSV) infection. Trifluorothymidine also has anti-orthopoxvirus activity[2].
Cytidine-5'-triphosphate- 13C9 (Cytidine triphosphate- 13C9 dilithium; 5'-CTP- 13C9) dilithium is 13C-labeled Cytidine-5'-triphosphate (HY-125818). Cytidine 5′-triphosphate (Cytidine triphosphate; 5'-CTP) is a nucleoside triphosphate and serves as a building block for nucleotides and nucleic acids, lipid biosynthesis. Cytidine triphosphate synthase can catalyze the formation of cytidine 5′-triphosphate from uridine 5′-triphosphate (UTP). Cytidine 5′-triphosphate is an essential biomolecule?in the de novo?pyrimidine biosynthetic pathway in?T. gondii.
Deoxycytidine triphosphate- 13C9 (dCTP- 13C9 dilithium; 2′-Deoxycytidine-5′-triphosphate- 13C9) dilithium is 13C-labeled Deoxycytidine triphosphate (HY-101400). Deoxycytidine triphosphate (dCTP) is a nucleoside triphosphate that can be used for DNA synthesis. Deoxycytidine triphosphate has many applications, such as real-time PCR, cDNA synthesis, and DNA sequencing.
DMT-dA(bz) Phosphoramidite- 13C10, 15N5 is the 13C and 15N labeled DMT-dA(bz) Phosphoramidite[1]. DMT-dA(bz) Phosphoramidite is typically used in the synthesis of DNA[2].
Menaquinone-4- 13C6 is the 13C-labeled Menaquinone-4. Menaquinone-4 is a vitamin K, used as a hemostatic agent, and also a adjunctive therapy for the pain of osteoporosis.
Bisphenol AF- 13C12 is an isotopic label of Bisphenol AF. Bisphenol AF is used in polycarbonate plastic and epoxy resin manufacturing. Bisphenol AF can significantly increase intracellular ROS levels .
Thymine- 13C5, 15N2 (5-Methyluacil- 13C5, 15N2) is 13C and 15N labeled Thymine. Thymine is one of the four nucleobases in the nucleic acid of DNA and can be a target for actions of 5-fluorouracil (5-FU) in cancer treatment, with a Km of 2.3 μM .
dGTP- 13C10, 15N5 (2'-Deoxyguanosine-5'-triphosphate- 13C10, 15N5) dilithium is 13C and 15N-labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
2'-Deoxyadenosine-5'-triphosphate- 13C10, 15N5 (dATP- 13C10, 15N5) dilithium is 13C and 15N-labeled 2'-Deoxyadenosine-5'-triphosphate (HY-136648). 2'-Deoxyadenosine-5'-triphosphate (dATP) is a nucleotide used in cells for DNA synthesis (or replication), as a substrate of DNA polymerase.
5-Hydroxymethylfurfural- 13C6 (2-Hydroxymethyl-5-furfural- 13C6; 2-Formyl-5-hydroxymethylfuran- 13C6) is a 13C labeled 5-Hydroxymethylfurfural (HY-Y0051). 5-Hydroxymethylfurfural (2-Hydroxymethyl-5-furfural), derived from Cornus officinalis, inhibits yeast growth and fermentation as stressors.
p,p'-DDD- 13C12 is 13C labeled p,p'-DDD. p,p'-DDD is a major metabolite of p,p'-DDT. p,p'-DDD occurs in the feces and livers of rats, that are given p,p'-DDT by stomach tube, but not of rats injected intraperitoneally with p,p'-DDT [3].
Oleic acid- 13C18 is the 13C labeled Oleic acid (HY-N1446). Oleic acid (9-cis-Octadecenoic acid) is an abundant monounsaturated fatty acid . Oleic acid is a Na+/K+ ATPase activator .
3-Methoxytyramine-d4 (hydrochloride) is the deuterium labeled 3-Methoxytyramine hydrochloride. 3-Methoxytyramine hydrochloride is an inactive metabolite of dopamine which can activate trace amine associated receptor 1 (TAAR1)[1][2].
Eprosartan-d6 is deuterated labeled Eprosartan (HY-117743). Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively .
p-Toluic acid-d4 is the deuterium labeled p-Toluic acid[1]. p-Toluic acid (4-Methylbenzoic acid) is a substituted benzoic acid and can be used as an intermediate for the synthesis of para-aminomethylbenzoic acid (PAMBA), p-tolunitrile, etc.
Taurochenodeoxycholic acid-d4-1 (sodium) is the deuterium labeled Taurochenodeoxycholic acid. Taurochenodeoxycholic acid (12-Deoxycholyltaurine) sodium is one of the main bioactive substances of animals' bile acid. Taurochenodeoxycholic acid sodium induces apoptosis and shows obvious anti-inflammatory and immune regulation properties[1][2].
Sulfachloropyridazine- 13C6 is the 13C6 labeled Sulfachloropyridazine. Sulfachloropyridazine is a broad spectrum sulfonamide used against both Gram-positive and Gram-negative aerobic bacteria.
Lignoceric acid-d4-2 is the deuterium labeled Lignoceric acid. Lignoceric acid (Tetracosanoic acid) is a 24-carbon saturated (24:0) fatty acid, which is synthesized in the developing brain. Lignoceric acid is also a by-product of lignin production. Lignoceric acid can be used for Zellweger cerebro‐hepato‐renal syndrome and adrenoleukodystrophy research[1][2].
D-Glutamic acid-d5 is the deuterium labeled D-Glutamic acid. D-glutamic acid, an enantiomer of L- glutamic acid, is widely used in pharmaceuticals and foods[1].
Risperidone-d6 (R 64 766-d6) is the deuterium labeled Risperidone (HY-11018). Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively .
4-Aminohippuric acid-d4 is the deuterium labeled 4-Aminohippuric acid. 4-Aminohippuric acid is a diagnostic agent, useful in medical tests involving the kidney, used in the measurement of renal plasma flow.
5,6-Dihydro-5-methyluracil-d6 is the deuterium labeled 5,6-Dihydro-5-methyluracil. 5,6-Dihydro-5-methyluracil (Dihydrothymine), an intermediate breakdown product of thymine, comes from animal or plants. 5,6-Dihydro-5-methyluracil (Dihydrothymine) can be toxic when present at abnormally high levels[1].
Docosanoic acid-d4-1 (Behenic acid-d4-1) is the deuterium labeled Docosanoic acid (HY-W013049). Docosanoic acid (Behenic acid) is a long-chain saturated fatty acid. Docosanoic acid inhibits the double-stranded DNA (dsDNA) binding activity of p53 DNA binding domain, with a Kd of 12 nM. Docosanoic acid has low bioavailability and can increase cholesterol in humans [3].
Moxifloxacin-d4 is the deuterium labeled Moxifloxacin. Moxifloxacin is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia[1][2].
Valerylcarnitine-d9 (C5:0 L-carnitine-d9) is the deuterium labeled Valerylcarnitine (HY-113266). Valerylcarnitine is an endogenous metabolite, belonging to the short-chain acylcarnitines .
L-Alanine-d7 is the deuterium labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
Betamethasone dipropionate-d10 is the deuterium labeled Betamethasone dipropionate. Betamethasone dipropionate is a glucocorticoid steroid with anti-inflammatory and immunosuppressive abilities.
Risperidone-d4 is the deuterium labeled Risperidone. Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
ATP-d14 (Adenosine 5'-triphosphate-d14) dilithium is deuterium labeled ATP (HY-B2176). ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation.
Vortioxetine-d8 (Lu AA 21004-d8) is a deuterated version of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM) .
L-Glutamine-d5 is the deuterium labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells[1][2].
Abemaciclib metabolite M2-d6 is the deuterium labeled Abemaciclib metabolite M2. Abemaciclib metabolite M2 (LSN2839567) is a metabolite of Abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50s in the range of 1-3 nM. Anti-cancer activity[1][2].
(2R)-Isopropyl 2-((((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)amino)propanoate-d5 is the deuterium labeled (2R)-isopropyl 2-((((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)amino)propanoate [
Indolelactic acid-d5 is the deuterium labeled Indolelactic acid. Indolelactic acid is a tryptophan (Trp) catabolite in Azotobacter vinelandii cultures.
Adenosine-d is the deuterium labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation[1][2].
O-Toluic acid-d7 is the deuterium labeled o-Toluic acid[1]. o-Toluic acid (2-Methylbenzoic acid) is a benzoic acid substituted by a methyl group at position 2. O-Toluic acid plays a role as a xenobiotic metabolite.
Tropisetron-d5 (SDZ-ICS-930-d5 (free base)) is deuterium labeled Tropisetron. Tropisetron (SDZ-ICS-930 free base) is an orally active anti-inflammatory and antiemetic agent. Tropisetron is 5-HT3R antagonists with a Ki of 5.3 nM. Tropisetron is also a partial agonist of α7 nicotinic receptor (α7 nAChR) with an EC50 of 1.3 μM. In addition, Tropisetron has antitumor and neuroprotective effects [3] .
Diethyl phosphate-d10-1 is the deuterium labeled Diethyl phosphate. Diethylphosphate (Diethyl phosphoric acid) is an orally active organophosphorus pesticides metabolite. Diethylphosphate can interfere with thyroid hormone-related mechanisms and affect intestinal microbes in rats .
L-Alanine-d4 is the deuterium labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
(±)11(12)-EET-d11 is the deuterium labeled (±)11(12)-EET. (±)11(12)-EET is a NLRP3 inflammasome inhibitor. (±)11(12)-EET can be used for the research of anti-inflammatory, angiogenic and cardioprotective[1][2][3][4][6].
Ribavirin- 13C5 is the 13C-labeled Ribavirin. Ribavirin (ICN-1229) is an antiviral agent against a broad spectrum of viruses including HCV, HIVl, and RSV.
Abemaciclib metabolite M18-d8 is the deuterium labeled Abemaciclib metabolite M18. Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader[1][2].
Glycerol- 13C2 is the 13C labeled Glycerol[1]. Glycerol is used in sample preparation and gel formation for polyacrylamide gel electrophoresis[2][3][4].
2-Hydroxy Ibuprofen-d6 is the deuterium labeled 2-Hydroxy Ibuprofen. 2-Hydroxy Ibuprofen is a metabolite of Ibuprofen. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively[1][2].
Norethindrone- 13C2 (Norethisterone- 13C2) is the 13C labeled Norethindrone (HY-B0554) . Norethindrone is a female progestin approved by FDA for the treatment of endometriosis, uterine bleeding caused by abnormal hormone levels, and secondary amenorrhea [3] .
TCEP-d12 (hydrochloride) (Tris(2-?carboxyethyl)?phosphine hydrochloride-d12) is deuterium labeled TCEP (hydrochloride). TCEP hydrochloride (Tris(2-carboxyethyl)phosphine hydrochloride) is a non-thiol reducing agent that is more stable and produces a faster S-S reductive reaction than other chemical reductants. TCEP hydrochloride is a trialkylphosphine, selectively reduces protein disuldes without altering the properties or interacting with thiol-directed agents in the reaction mixture. TCEP hydrochloride is also a commonly used reducing agent in the DNA/AuNP chemistry [3] .
Docosanoic acid-d4-2 (Behenic acid-d4-2) is the deuterium labeled Docosanoic acid (HY-W013049). Docosanoic acid (Behenic acid) is a long-chain saturated fatty acid. Docosanoic acid inhibits the double-stranded DNA (dsDNA) binding activity of p53 DNA binding domain, with a Kd of 12 nM. Docosanoic acid has low bioavailability and can increase cholesterol in humans [3].
DL-Lysine-4,4,5,5-d4 (dihydrochloride) is the deuterium labeled DL-Lysine. DL-Lysine is a racemic mixture of the D-Lysine and L-Lysine. Lysine is an α-amino acid that is used in the biosynthesis of proteins[1].
D-Threonine-d2 is the deuterium labeled D-Threonine. D-Threonine (H-D-Thr-OH) is an enantiomer of L-threonine. D-Threonine is a metabolite of Saccharomyces cerevisiae.
14(S)-HDHA-d5 (14(S)-HDoHE-d5) is deuterium labeled 14(S)-HDHA. 14(S)-HDHA (14(S)-HDoHE) is an oxygenation product of Docosahexaenoic acid (DHA). 14(S)-HDHA is a marker reflecting activation of a Docosahexaenoic acid carbon 14-lipoxygenation pathway .
p-Cresol sulfate-d4 (potassium) is deuterium labeled p-Cresyl sulfate (potassium). p-Cresyl sulfate potassium is a uremic toxin that binds to a prototype protein. p-Cresyl sulfate potassium activates the JNK and p38 MAPK signaling pathways. p-Cresyl sulfate potassium has pro-inflammatory activity [3].
1-Butynylbenzene-d5 is the deuterium labeled 1-Butynylbenzene[1]. 1-Butynylbenzene-d5 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Sulfadimethoxine- 13C6 is the 13C-labeled Sulfadimethoxine. Sulfadimethoxine (Sulphadimethoxine) is a sulfonamide antibiotic used to treat many infections[1][2].
Hydrochlorothiazide- 13C6 is the 13C labeled Hydrochlorothiazide[1]. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect[2][3][4].
Ciraparantag-d8 tetrahydrochloride diacetate (PER977-d8 tetrahydrochloride diacetate) is the deuterium labeled Ciraparantag (HY-18660). Ciraparantag is a thrombin and factor Xa inhibitor. Ciraparantag is a broad-spectrum reversal agent for anticoagulants, including low-molecular-weight heparin, unfractionated heparin, and certain direct oral anticoagulants. It is reported to antagonize the effects of all coagulants except VKAs and agratroban [3] .
(E)-β-Farnesene-d6 is deuterated labeled Nerol (HY-N7063). Nerol is a constituent of neroli oil. Nerol Nerol triggers mitochondrial dysfunction and induces apoptosis via elevation of Ca 2+ and ROS. Antifungal activity .
Afatinib-d6 (dimaleate) is the deuterium labeled Afatinib dimaleate. Afatinib dimaleate is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively[1][2].
Veratric acid-d6 is deuterium labeled Veratric acid. Veratric acid (3,4-Dimethoxybenzoic acid) is an orally active phenolic compound derived from vegetables and fruits, has antioxidant[1] and anti-inflammatory activities[3]. Veratric acid also acts as a protective agent against hypertension-associated cardiovascular remodelling[2]. Veratric acid reduces upregulated COX-2 expression, and levels of PGE2, IL-6 after UVB irradiation[3].
Abemaciclib metabolite M20-d8 is the deuterium labeled Abemaciclib metabolite M20. Abemaciclib metabolite M20 (LSN3106726), the active metabolite of Abemaciclib, is a selective CDK4/6 inhibitor[1].
Patulin- 13C7 (Terinin- 13C7) is the 13C labeled Patulin (HY-N6779) . Patulin (Terinin) is a mycotoxin produced by fungi including the Aspergillus, Penicillium, and Byssochlamys species, is suspected to be clastogenic, mutagenic, teratogenic and cytotoxic. Patulin induces autophagy-dependent apoptosis through lysosomal-mitochondrial axis, and causes DNA damage [3] .
Calcifediol-d6 monohydrate is the deuterium labeled Calcifediol monohydrate. Calcifediol monohydrate (25-hydroxy Vitamin D3 monohydrate), is an effective VDR ligand and VD supplement. Calcifediol is a prohormone of the vitamin D endocrine system (VDES) and is hydroxylated in the liver to produce the active form, calcitriol. Calcifediol can rapidly increase serum VD levels [3].
2-Hydroxypalmitic acid-d30 (2-Hydroxyhexadecanoic acid-d30) is deuterium labeled 2-Hydroxypalmitic acid. 2-Hydroxypalmitic acid is an intermediate in phytosphingosine metabolism .
H-D-Trp-OH-d5 (D-Tryptophan-d5) is the deuterium labeled H-D-Trp-OH. H-D-Trp-OH is a D-stereoisomer of tryptophan and occasionally found in naturally produced peptides such as the marine venom peptide.
Vortioxetine-d8 (Lu AA 21004-d8) hydrobromide is the deuterated form of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM) .
Perospirone-d8 (SM-9018-d8 (free base)) is deuterium labeled Perospirone. Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT2A receptor (Ki=0.6 nM) and dopamine D2 receptor (Ki=1.4 nM), and also a partial agonist of 5-HT1A receptor (Ki=2.9 nM). Perospirone is an atypical antipsychotic agent and has the potential for schizophrenic disease research [3].
DPPC-d9-1 is the deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers[1]. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in mice[2].
4-Oxofenretinide-d4 (4-Oxo-4-HPR-d4) is deuterium labeled 4-Oxofenretinide. 4-Oxofenretinide (4-Oxo-4-HPR) is a metabolite of Fenretinide (HY-15373). 4-Oxofenretinide induces cell growth inhibition in ovarian, breast, and neuroblastoma tumor cell lines. 4-Oxofenretinide causes a marked accumulation of cells in G2-M. 4-Oxofenretinide induces cancer cell apoptosis through caspase-9 .
Ibuprofen- 13C6 ((±)-Ibuprofen- 13C6) is a 13C labeled Ibuprofen (HY-78131). Ibuprofen ((±)-Ibuprofen) is a potent, orally active, selective COX-1 inhibitor with an IC50 value of 13 μM. Ibuprofen inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen ((±)-Ibuprofen) can be used in the research of pain, swelling, inflammation, infection, immunology, cancers [3] .
Histamine- 13C5 is the 13C labeled Histamine (HY-B1204). Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter .
(Rac)-DPPC-d6 is a deuterated labeled DPPC . DPPC (129Y83) is a phosphoglyceride that can be used to prepare lipid monolayers, bilayers, and liposomes. DPPC is the main lipid component of pulmonary surfactant. Dppc-liposome can be effectively used as a delivery vector to induce an immune response against GSL antigen in mice [3] .
p-Toluic acid-d7 is the deuterium labeled p-Toluic acid[1]. p-Toluic acid (4-Methylbenzoic acid) is a substituted benzoic acid and can be used as an intermediate for the synthesis of para-aminomethylbenzoic acid (PAMBA), p-tolunitrile, etc.
Monomethyl phthalate-d4 (2-(Methoxycarbonyl)benzoic acid-d4) is the deuterium labeled Monomethyl phthalate. Monomethyl phthalate is a phthalate metabolite. Monomethyl phthalate acts as a urinary biomarker of phthalates exposure and can be used as a standard for the determination of thyroid cancer and benign nodule .
Sulfacetamide- 13C6 (Sulphacetamide 13C6) is the 13C6 labeled Sulfacetamide (HY-N7123). Sulfacetamide (Sulphacetamide) is a sulfonamide antibiotic that can be used for the study of ocular infections. Sulfacetamide has antifungal and antibacterial activities .
Monooctyl phthalate-d4 (Mono-n-octyl phthalate-d4) is a deuterium labeled Monooctyl phthalate (HY-133671). Monooctyl phthalate (Mono-n-octyl phthalate) exhibits antimycobacterial activity with a MIC of 20 μg/mL .
2-Phenylethyl isothiocyanate-d5 isothiocyanate-d5 is the deuterium labeled 2-Phenylethyl isothiocyanate[1]. 2-Phenylethyl isothiocyanate is a potent antifungal agent. 2-Phenylethyl isothiocyanate significantly inhibited spore germination and mycelial growth of Alternaria alternata, with a MIC (minimum inhibitory concentration) of 1.22 mM. The antifungal effect of 2-Phenylethyl isothiocyanate against Alternaria alternata might be via reduction in toxin content and breakdown of cell membrane integrity[2][3].
Cytidine 5′-monophosphate- 13C9 (5'-Cytidylic acid- 13C9 dilithium; 5'-CMP- 13C9) dilithium is 13C-labeled Cytidine 5'-monophosphate (HY-W009162). Cytidine 5'-monophosphate (5'-Cytidylic acid) is a nucleotide which is used as a monomer in RNA. Cytidine 5'-monophosphate consists of the nucleobase cytosine, the pentose sugar ribose, and the phosphate group.
5'-Guanylic acid- 13C10 (5'-GMP- 13C10 dilithium; 5'-guanosine monophosphate- 13C10) dilithium is 13C-labeled 5'-Guanylic acid (HY-N5134). 5'-Guanylic acid (5'-GMP) is involved in several metabolic disorders, including the AICA-ribosiduria pathway, adenosine deaminase deficiency, adenine phosphoribosyltransferase deficiency (aprt), and the 2-hydroxyglutric aciduria pathway.
N-Acetyl mesalazine-13C6 is a deuterated labeled N-Acetyl mesalazine . N-Acetyl mesalazine (N-Acetyl-5-aminosalicylic acid) is the metabolite of 5-Aminosalicylic Acid (HY-15027) with endoscopic activity. N-Acetyl mesalazine can be used for the research of ulcerative colitis .
Cytidine- 13C9 (Cytosine β-D-riboside- 13C9; Cytosine-1-β-D-ribofuranoside- 13C9) is 13C labeled Cytidine (HY-B0158). Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catecholamine synthesis, and mitochondrial function [3].
rU Phosphoramidite- 13C9, 15N2 (DMT-2'O-TBDMS-rU phosphoramidite- 13C9, 15N2) is 13C and 15N-labeled rU Phosphoramidite (HY-W048482). rU Phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
Uridine 5'-monophosphate- 13C9, 15N2 (5'- Uridylic acid- 13C9, 15N2) dilithium is 13C and 15N-labeled Uridine 5'-monophosphate (HY-101981). Uridine 5'-monophosphate (5'- Uridylic acid), a monophosphate form of UTP, can be acquired either from a de novo pathway or degradation products of nucleotides and nucleic acids in vivo and is a major nucleotide analogue in mammalian milk.
Pregnenolone monosulfate (sodium)- 13C2,d2 is the 13C- and deuterium labeled Pregnenolone monosulfate sodium. Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium salt acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium salt can protect the brain from cannabis intoxication[1][2]. Pregnenolone monosulfate sodium salt is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
Droxidopa- 13C2, 15N (hydrochloride) is deuterium labeled Droxidopa. Droxidopa(L-DOPS), the mixture of Droxidopa (w/w80%) and Pharmaceutical starch (w/w20%), acts as a proagent to the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline); Droxidopa(L-DOPS) is capable of crossing the protective blood–brain barrier[1][2].
Acetaminophen- 13C2, 15N is the 13C and 15N labeled Acetaminophen[1]. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM;is a widely used antipyretic and analgesic agent[2][3][4]. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor[5].
15-Deoxy-Δ-12,14-prostaglandin J2-d4 is the deuterium labeled 15-Deoxy-Δ-12,14-prostaglandin J2. 15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2. 15-Deoxy-Δ-12,14-prostaglandin J2 is a selective PPARγ (EC50 of 2 µM) and a covalent PPARδ agonist. 15-Deoxy-Δ-12,14-prostaglandin J2 promotes efficient differentiation of C3H10T1/2 fibroblasts to adipocytes with an EC50 of 7 μM[1][2].
(R)-3-Hydroxybutanoic acid- 13C4 sodium is a 13C labeled (R)-3-Hydroxybutanoic acid (HY-W051723). (R)-3-Hydroxybutanoic acid is a metabolite converted from acetoacetic acid catalyzed by 3-hydroxybutyrate dehydrogenase. (R)-3-Hydroxybutanoic acid can function as a nutrition source, and as a precursor for vitamins, antibiotics and pheromones .
(R)-3-Hydroxybutanoic acid- 13C2 (sodium) is the 13C labeled (R)-3-Hydroxybutanoic acid (sodium) (HY-W015851). (R)-3-Hydroxybutanoic acid (sodium) is a metabolite converted from acetoacetic acid catalyzed by 3-hydroxybutyrate dehydrogenase. (R)-3-Hydroxybutanoic acid sodium can function as a nutrition source, and as a precursor for vitamins, antibiotics and pheromones[1][2][3].
1,2-Dioleoyl-3-lauroyl-rac-glycerol- 13C3 is the 13C-labeled 1,2-Dioleoyl-3-lauroyl-rac-glycerol (HY-165089), 1,2-Dioleoyl-3-lauroyl-rac-glycerol (1,2-Olein-3-laurin) is a triglyceride identified by specific analytical methods in human milk, infant formula, other mammalian milk, and vegetable oils, with specific structural and distribution characteristics.
Fmoc-Gly-OH- 13C2, 15N is a 15N-labeled and 13C-labled Crystal Violet. Crystal violet (Basic Violet 3) is a triarylmethane dye. Crystal Violet (Gentian Violet) has antiviral effects against H1N1 and also has prominent bactericidal activities.
2-Hydroxyestrone- 13C6 is the 13C-labeled 2-Hydroxyestrone. 2-Hydroxyestrone (Catecholestrone) is a specific receptor-mediated antiestrogenic agent. 2-Hydroxyestrone is anticarcinogenic[1][2].
3-Hydroxybutyric acid-d2 (sodium) is the deuterium labeled 3-Hydroxybutyric acid sodium[1]. 3-Hydroxybutyric acid sodium (β-Hydroxybutyric acid sodium) is a metabolite that is elevated in type I diabetes. 3-Hydroxybutyric acid sodium can modulate the properties of membrane lipids[2].
Mycophenolic acid-13C17 (Mycophenolate-13C17) is the 13C labeled Mycophenolic acid (HY-B0421). Mycophenolic acid is a potent uncompetitive inosine monophosphate dehydrogenase (IMPDH) inhibitor with an EC50 of 0.24 μM. Mycophenolic acid demonstrates antiviral effects against a wide range of RNA viruses including influenza. Mycophenolic acid is an immunosuppressive agent. Antiangiogenic and antitumor effects.
γ-Aminobutyric acid-d2 is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
N-Nitrosodibutylamine-d18 is the deuterium labeled N-Nitrosodibutylamine[1]. N-Nitrosodibutylamine (N-Nitroso-di-n-butylamine) is a nitrosamine enriched in the drinking water[2].
Progesterone-d9 is the deuterium labeled Progesterone. Progesterone is a steroid hormone that regulates the menstrual cycle and is crucial for pregnancy.
trans-Cinnamic acid-d7 is the deuterium labeled trans-Cinnamic acid[1]. trans-Cinnamic acid is a natural antimicrobial, with minimal inhibitory concentration (MIC) of 250 μg/mL against fish pathogen A. sobria, SY-AS1[2].
2'-Deoxyadenosine-5'-triphosphate-d14 (dATP-d14) dilithium is deuterium labeled 2'-Deoxyadenosine-5'-triphosphate (HY-136648). 2'-Deoxyadenosine-5'-triphosphate (dATP) is a nucleotide used in cells for DNA synthesis (or replication), as a substrate of DNA polymerase.
Niclosamide- 13C6 (monohydrate) is the 13C labeled Niclosamide monohydrate[1]. Niclosamide (BAY2353) monohydrate is an orally active antihelminthic agent used in parasitic infection research[2]. Niclosamide monohydrate is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells[5]. Niclosamide monohydrate has biological activities against cancer, and inhibits DNA replication in Vero E6 cells[3][4][6].
p-Cresol sulfate-d7 (potassium) is the deuterium labeled p-Cresyl sulfate potassium. p-Methylphenyl potassium sulfate is a prototype protein-bound uremic toxin[1][2].
Sucrose-13C6 is the 13C labeled Sucrose[1]. Sucrose (D-(+)-Saccharose) is a disaccharide which is composed of two monosaccharides, glucose and fructose. Sucrose can be applied in some animal models, including metabolic disease, obesity, diet on preference, and diabetes, et al[2].
N-desmethyl Enzalutamide-d6 is a deuterium labeled N-desmethyl Enzalutamide. N-desmethyl Enzalutamide is an active metabolite of Enzalutamide. N-desmethyl Enzalutamide is the active metabolite of Enzalutamide. N-desmethyl Enzalutamide demonstrates primary and secondary pharmacodynamics of similar potency to Enzalutamide and circulates at approximately the same plasma concentrations as enzalutamide[1].
Adenosine monophosphate- 13C5 (AMP- 13C5) is 13C labeled Adenosine monophosphate. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction .
Bis(1-chloro-2-propyl) phosphate-d12 is deuterium labeled Bis(1-chloro-2-propyl) phosphate. Bis(1-chloro-2-propyl) phosphate (BCIPP) is a metabolite of organophosphate flame retardants (OPFR) that may alter energy metabolism by influencing the levels of steroid hormones, such as cortisol and cortisone. Bis(1-chloro-2-propyl) phosphate holds potential for research on metabolism-related diseases caused by environmental exposure .
N-Dodecyl-β-D-maltoside-d25 (Lauryl Maltoside-d25) is deuterium labeled N-Dodecyl-β-D-maltoside (HY-128974). N-Dodecyl-β-D-maltoside is a non-ionic detergent. N-Dodecyl-β-D-maltoside has strong adsorption on alumina, titanium dioxide and hematite. N-Dodecyl-β-D-maltoside can promote the reactivation of various proteins. N-Dodecyl-β-D-maltoside can effectively stabilize photoactive reaction center complexes (RCs) and inhibit the degradation of Rhodopseudomonas spheroides R-26 reaction center in solution. N-Dodecyl-β-D-maltoside can be used for purification and stabilization of RNA polymerase and for detection of protein-lipid interactions [3] .
N-Nitrosodibutylamine-d9 is the deuterium labeled N-Nitrosodibutylamine[1]. N-Nitrosodibutylamine (N-Nitroso-di-n-butylamine) is a nitrosamine enriched in the drinking water[2].
Erdosteine- 13C4 is a 13C-labeled Erdosteine. Erdosteine inhibits lipopolysaccharide (LPS)-induced NF-κB activation[1][2]. Erdosteine has muco-modulatory, anti-bacterial, anti-inflammatory and anti-oxidant effects[3].
Prasugrel-13C6 is a deuterated labeled Prasugrel . Prasugrel (PCR 4099), a thienopyridine and proagent, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation .
Sacubitril-13C4 (AHU-377-13C4) is a 13C-labeled version of Sacubitril (HY-15407). Sacubitril is an orally active inhibitor of neprilysin NEP (IC50=5 nM). Sacubitril is used in research on heart failure, hypertension and COVID-19 [3] .
trans-Cinnamic acid-d5 is the deuterium labeled trans-Cinnamic acid[1]. trans-Cinnamic acid is a natural antimicrobial, with minimal inhibitory concentration (MIC) of 250 μg/mL against fish pathogen A. sobria, SY-AS1[2].
2-Ketoglutaric acid-d4 is the deuterium labeled 2-Ketoglutaric acid[1]. 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM)[2].
8-Isoprostaglandin E2-d4 (iPE2-III-d4) is deuterium labeled 8-Isoprostaglandin E2. 8-Isoprostaglandin E2 (iPE2-III) is a member of the isoprostane class of prostanoids. 8-Isoprostaglandin E2 acts at the receptor for thromboxane A2 (the TP) in vivo to induce vasoconstriction and platelet aggregation. 8-Isoprostaglandin E2 enhances receptor-activated NFkappa B ligand (RANKL)-dependent osteoclastic potential of marrow hematopoietic precursors via the cAMP pathway .
N-Palmitoyl-D-sphingomyelin-d9 (Sphingomyelin 16:0-d9) is deuterium labeled N-Palmitoyl-D-sphingomyelin. N-Palmitoyl-D-sphingomyelin (Sphingomyelin 16:0) (Compound SM-03) can be used for the synthesis of lipid nanoparticles .
9-Aminoacridine-13C6 is the 13C-labeled 9-Aminoacridine(HY-B1422). 9-Aminoacridine, a fluorescent probe, acts as an indicator of pH for quantitative determination of transmembrane pH gradients (inside acidic). 9-Aminoacridine is an antimicrobial. 9-Aminoacridine exerts its antimicrobial activity by interacting with specific bacterial DNA and disrupting the proton motive force in K. pneumoniae. 9-Aminoacridine is a HIV-1 inhibitor and inhibits HIV LTR transcription highly dependent on the presence and location of the amino moiety. 9-Aminoacridine inhibits virus replication in HIV-1 infected cell lines. 9-Aminoacridine is used as a Rifampin (RIF; HY-B0272) adjuvant for the multidrug-resistant K. pneumoniae infections [3].
Arachidonic acid- 13C4 (Immunocytophyt- 13C4) is 13C labeled Arachidonic acid. Arachidonic acid (Immunocytophyt) is a polyunsaturated omega-6 fatty acid and a major constituent of biomembranes. Arachidonic acid also acts as the substrate for various lipid mediators, such as prostaglandins (PGs). Arachidonic acid improves cognitive response and cardiovascular function .
Estradiol valerianate-d4 is the deuterium labeled Estradiol valerianate. Estradiol valerianate (β-estradiol 17-valerate) is a synthetic estrogen widely used in combination with other steroid hormones in hormone replacement therapy agents.
Diclofenac- 13C6 (Sodium) is the 13C6 labeled Diclofenac (Sodium). Diclofenac Sodium (GP 45840) is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac Sodium induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
Lactate-d4 sodium (60% in water) is the deuterium labeled Lactate sodium (60% in water). Lactate sodium (60% in water) is the product of glycogenolysis and glycolysis. Lactate sodium (60% in water) functions in a variety of biochemical processes .
Resolvin E1-d4-1 is the deuterium labeled Resolvin E1. Resolvin E1 (RvE1), a potent endogenous pro-resolving mediator of inflammation, is derived from omega-3 fatty acid eicosapentaenoic acid (EPA). Resolvin E1 is endogenously biosynthesized from EPA in the presence of Aspirin during the spontaneous resolution phase of acute inflammation, where specific cell-cell interactions occur. Resolvin E1 possesses unique counterregulatory actions that inhibit polymorphonuclear leukocyte (PMN) transendothelial migration. Resolvin E1 also acts as a potent inhibitor of leukocyte infiltration, dendritic cell migration, and IL-12 production[1][2].
Penicillin V- 13C6 (potassium) is the 13C6 labeled Penicillin V (potassium). Penicillin V Potassium (Phenoxymethylpenicillin potassium salt) is an orally active antibiotic. Penicillin V Potassium inhibits the growth of Streptococci, C. difficile and S. aureus. Penicillin V Potassium can be used for the research of otitis, sinusitis, pharyngitis and tonsillitis.
Odevixibat- 13C6 is 13C labeled Odevixibat (HY-109120). Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis .
Docosahexaenoic acid ethyl ester-d5-1 is the deuterium labeled Docosahexaenoic acid ethyl ester. Docosahexaenoic acid ethyl ester (Ethyl docosahexaenoate) is a 90% concentrated ethyl ester of docosahexaenoic acid manufactured from the microalgal oil. Docosahexaenoic acid ethyl ester enhances 6-hydroxydopamine-induced neuronal damage by induction of lipid peroxidation in mouse striatum. Docosahexaenoic acid (DHA) is a key component of the cell membrane, and its peroxidation is inducible due to the double-bond chemical structure. Docosahexaenoic acid has neuroprotective effects[1][2][3].
Methyl(E)-cinnamate-d7 is the deuterium labeled Methyl (E)-cinnamate[1]. Methyl (E)-cinnamate (EMC), a phytochemical constituent isolated from Alpinia katsumadai Hayata, is a natural flavor compound with anti-inflammatory properties. Methyl (E)-cinnamate is widely used in the food and commodity industry[2].
Guaiacol- 13C6 is the 13C labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
dGTP-d14 (2'-Deoxyguanosine-5'-triphosphate-d14) dilithium is deuterium labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
Vandetanib-13C6 is a deuterated labeled Vandetanib . Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) .
p-Coumaric acid-d6 is the deuterium labeled p-Coumaric acid (HY-N0351). p-Coumaric acid is the abundant isomer of cinnamic acid which has antitumor and anti-mutagenic activities[1][2].
Anthracene-9-carboxylic acid-d9 is the deuterium labeled Anthracene-9-carboxylic acid[1]. Anthracene-9-carboxylic acid (9-Anthracenecarboxylic acid) is an anthracene derivative traditionally used to block and identify Ca2+-activated Cl- currents (CaCCs) in various cell types, like diverse smooth muscle cells, epithelial cells and salivary gland cells[2].
Mead acid-d6 is the deuterium labeled Mead acid. Mead acid (5,8,11-Eicosatrienoic acid), an unsaturated (Omega-9) fatty acid, is an indicator of essential fatty acid deficiency[1].
Niclosamide- 13C6 is the 13C6 labeled Niclosamide. Niclosamide (BAY2353) is an orally bioavailable chlorinated salicylanilide, with anthelmintic and potential antineoplastic activity. Niclosamide (BAY2353) inhibits STAT3 with IC50 of 0.25 μM in HeLa cells and inhibits DNA replication in a cell-free assay.
Gallic acid-d2 is the deuterium labeled Gallic acid[1]. Gallic acid (3,4,5-Trihydroxybenzoic acid) is a natural polyhydroxyphenolic compound and an free radical scavenger to inhibit cyclooxygenase-2 (COX-2)[2]. Gallic acid has various activities, such as antimicrobial, antioxidant, antimicrobial, anti-inflammatory, and anticance activities[3].
Pragliflozin- 13C6 (ASP1941- 13C6) is 13C labeled Ipragliflozin. Ipragliflozin (ASP1941) is an orally active and selective SGLT2 inhibitor with IC50s of 7.38 and 1876 nM, 6.73 and 1166 nM, 5.64 and 1380 nM for human SGLT2 and SGLT1, rat SGLT2 and SGLT1, mouse SGLT2 and SGLT1, respectively. Antidiabetic agent .
Mono(5-carboxy-2-ethylpentyl) phthalate-d4 (MECPP-d4) is a deuterium labeled Mono(5-carboxy-2-ethylpentyl) phthalate (HY-133675). Mono(5-carboxy-2-ethylpentyl) phthalate (MECPP) is a metabolite of Di-(2-ethylhexyl) phthalate (DEHP). Di(2-ethylhexyl) phthalate is the predominant plasticizer added to rigid polyvinyl chloride (PVC) to impart flexibility, temperature tolerance, optical clarity, strength and resistance to kinking [3].
DMT-dA(bz) Phosphoramidite-d9 (DA-CE phosphoramidite-d9) is deuterium labeled DMT-dA(bz) Phosphoramidite (HY-W013059). DMT-dA(bz) Phosphoramidite is typically used in the synthesis of DNA.
Enzalutamide carboxylic acid-d6 is the deuterium labeled Enzalutamide carboxylic acid (MDV3100 carboxylic acid). Enzalutamide carboxylic acid is an inactive metabolite of Enzalutamide[1].
c is deuterium labeled Exatecan mesylate (HY-13631A). Exatecan mesylate is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL). Exatecan mesylate can be used in cancer research .
Eltrombopag- 13C4 (SB-497115- 13C4) is 13 sup>C-labeled Z-Eltrombopag. Z-Eltrombopag is an orally active thrombopoietin-receptor non-peptide agonist with platelet-stimulating activity for the study of chronic immune thrombocytopenia. Eltrombopag also has strong inhibitory effects on multidrug-resistant Staphylococcus aureus (Staphylococcus aureus) and can induce apoptosis (apoptosis) in liver cancer cells [3] .
Sumatriptan-d5 is deuterated labeled Sumatriptan (HY-B0121B). Sumatriptan (GR 43175) is an orally active 5-HT1 receptor agonist with IC50s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT1D, 5-HT1B and 5-HT1F receptors, respectively. Sumatriptan can be used for migraine headache research [3] .
Meclofenamic acid- 13C6 is the 13C6 labeled Meclofenamic acid. Meclofenamic Acid (Meclofenamate), a non-steroidal, anti-inflammatory agent, is a highly selective fat mass and obesity-associated (FTO) enzyme inhibitor. Meclofenamic Acid competes with FTO binding for the m(6)A-containing nucleic acid. Meclofenamic acid is a non-selective gap-junction blocker.
Methyl (E)-cinnamate-d5 is the deuterium labeled Methyl (E)-cinnamate[1]. Methyl (E)-cinnamate (EMC), a phytochemical constituent isolated from Alpinia katsumadai Hayata, is a natural flavor compound with anti-inflammatory properties. Methyl (E)-cinnamate is widely used in the food and commodity industry[2].
Mono(2-ethyl-5-hydroxyhexyl) phthalate-d4 (MEHHP-d4) is a deuterium labeled Mono(2-ethyl-5-hydroxyhexyl) phthalate (HY-133677). Mono(2-ethyl-5-hydroxyhexyl) phthalate (MEHHP) is an oxidative metabolite of Di(2-ethylhexyl) phthalate (DEHP). Mono(2-ethyl-5-hydroxyhexyl) phthalate may protective sperm DNA damage. Di(2-ethylhexyl) phthalate is the predominant plasticizer added to rigid polyvinyl chloride (PVC) to impart flexibility, temperature tolerance, optical clarity, strength and resistance to kinking [3].
DL-Phenylalanine-d5 (hydrochloride) is the deuterium labeled DL-Phenylalanine hydrochloride. L-Phenylalanine hydrochloride is an essential amino acid isolated from Escherichia coli. L-Phenylalanine hydrochloride is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine hydrochloride is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine hydrochloride is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
(R)-Bromoenol lactone-d7 ((R,E)-Bromoenol lactone-d7) is deuterium labeled (R)-Bromoenol lactone. (R)-Bromoenol lactone ((R)-BEL) is an irreversible, chiral, mechanism-based inhibitor of calcium-independent phospholipase γ (iPLA2γ). (R)-BEL inhibits human recombinant iPLA2γ with an IC50 of approximately 0.6 μM .
γ-Aminobutyric acid-d6 is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
Isosorbide dinitrate- 13C6 is the 13C labeled Isosorbide dinitrate[1]. Isosorbide dinitrate (ISDN) is an NO donor that prevents LV remodeling and degradation of cardiac function following myocardial infarction (MI)[2].
trans-2-Decenal-d2 is deuterated labeled Coumarin (HY-N0709). Coumarin is a potent and orally active anti-inflammatory agent. Coumarin shows an antinociceptive effect. Coumarin shows antibacterial, antifungal and anticancer activity .
Monobenzyl phthalate-d4 is the deuterium labeled Monobenzyl phthalate. Monobenzyl phthalate (2-((Benzyloxy)carbonyl)benzoic acid) is the urinary metabolite exposuring to phthalates, such as, diethylhexyl phthalate (DEHP)[1].
L-Phenylalanine- 13C9, 15N,d8 is the deuterium, 13C-, and 15-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
Levoglucosan- 13C6 is the 13C labeled Levoglucosan[1]. Levoglucosan (1,6-Anhydro-β-D-glucopyranose) is an anhydrosugar produced through glucan pyrolysis and is widely found in nature[2].
Angiotensin II human- 13C6, 15N TFA (Ang II- 13C6, 15N TFA) is 13C- and 15N-labeled Angiotensin II human (TFA) (HY-13948B). Angiotensin II human (Angiotensin II) TFA is a vasoconstrictor and a major bioactive peptide of the renin/angiotensin system. Angiotensin II human TFA plays a central role in regulating human blood pressure, which is mainly mediated by interactions between Angiotensin II and the G-protein-coupled receptors (GPCRs) Angiotensin II type 1 receptor (AT1R) and Angiotensin II type 2 receptor (AT2R). Angiotensin II human TFA stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions [3].
Liothyronine- 13C9, 15N is the 13C and 15N labeled Liothyronine[1]. Liothyronine is an active form of thyroid hormone. Liothyronine is a potent thyroid hormone receptors TRα and TRβ agonist with Kis of 2.33 nM for hTRα and hTRβ, respectively[2][3][4].
AICAR- 13C2, 15N (Acadesine- 13C2, 15N; AICA Riboside- 13C2, 15N) is the 13C and 15N labeled AICAR (HY-13417) . AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor [3].
Glucosamine- 13C6, 15N (hydrochloride) is the 13C and 15N labeled Glucosamine hydrochloride. Glucosamine hydrochloride (D-Glucosamine hydrochloride) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids,
Avibactam sodium salt- 13C5 (NXL-104- 13C5) is 13C labeled Avibactam (sodium). Avibactam sodium (NXL-104) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively .
1,2-Distearoyl-sn-glycero-3-phosphorylethanolamine-d70 is deuterium labeled 1,2-Distearoyl-sn-glycero-3-phosphorylethanolamine. 1,2-Distearoyl-sn-glycero-3-phosphorylethanolamine (DSPE) is a phosphoethanolamine (PE) lipid that can be used in the synthesis
Oxiran-2-ylmethyl hexadecanoate-d31 is deuterium labeled Glycidyl palmitate. Glycidyl Palmitate is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Taurine- 13C2 is the 13C-labeled Taurine. Taurine, a sulphur-containing amino acid and an organic osmolyte involved in cell volume regulation, provides a substrate for the formation of bile salts, and plays a role in the modulation of intracellular free calcium concentration. Taurine has the ability to activate autophagy in adipocytes[1][2][3].
Uridine 5'-monophosphate-d11 (5'-?Uridylic acid-d11) dilithium is deuterium labeled Uridine 5'-monophosphate (HY-101981). Uridine 5'-monophosphate (5'-?Uridylic acid), a monophosphate form of UTP, can be acquired either from a de novo pathway or degradation products of nucleotides and nucleic acids in vivo and is a major nucleotide analogue in mammalian milk.
L-Phenylalanine-d is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
L-Phenylalanine-d2 is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
3-Hydroxybutyric acid-d4 (sodium) is the deuterium labeled 3-Hydroxybutyric acid. 3-Hydroxybutyric acid (β-Hydroxybutyric acid) is a metabolite that is elevated in type I diabetes. 3-Hydroxybutyric acid can modulate the properties of membrane lipids[1].
Pregnenolone-d4 is the deuterium labeled Pregnenolone. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication[1][2]. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
(S)-2-Aminohexanedioic acid-d4 is the deuterium labeled (S)-2-Aminohexanedioic acid. (S)-2-Aminohexanedioic acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
L-Arginine- 13C6 (hydrochloride) is the 13C-labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
Norverapamil-d7 (hydrochloride) is a deuterium labeled Norverapamil. Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor[1][2].
SAH- 13C5 is the 13C-labeled SAH. SAH (S-Adenosylhomocysteine) is an amino acid derivative and a modulartor in several metabolic pathways. It is an intermediate in the synthesis of cysteine and adenosine[1]. SAH is an inhibitor for METTL3-METTL14 heterodimer complex (METTL3-14) with an IC50 of 0.9 µM[2].
trans-2-Nonenal-d2 is deuterated labeled Acetylpyrazine (HY-W007692). Acetylpyrazine (2-Acetylpyrazine) is used to form many polycyclic compounds, as useful structures in pharmaceuticals and perfumes. Acetylpyrazine is a component of the folates (vitamin B compounds) .
Phosphoenolpyruvic acid (potassium)- 13C2 is the 13C labeled Phosphoenolpyruvic acid potassium (HY-W008807) . Phosphoenolpyruvic acid (Phosphoenolpyruvate) potassium is a glycolysis metabolite with a high-energy phosphate group. Phosphoenolpyruvic acid potassium is involved in glycolysis and gluconeogenesis, and used as energy source to produce ATP, under the energy-limited conditions. Phosphoenolpyruvic acid potassium also exhibits cytoprotective and anti-oxidative properties .
L-Arginine- 15N2 (hydrochloride) is the 15N-labeled L-Arginine (hydrochloride). L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
Pseudane IX-d4 (2-Nonylquinolin-4(1H)-one-d4) is deuterium labeled Pseudane IX. Pseudane IX, a compound isolated from the leaves of Ruta angustifolia, has strong anti-HCV activity with an IC50 value of 1.4 μg/mL. Pseudane IX reduces HCV RNA replication and viral protein synthesis levels .
7α,25-Dihydroxycholesterol-d6 is deuterium labeled 7α,25-Dihydroxycholesterol. 7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly
Risperidone-d4-1 (R 64 766-d4-1) is the deuterium labeled Risperidone (HY-11018). Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
L-Arginine- 15N4 (hydrochloride) is the 15N-labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis[1].
(Rac)-Moxifloxacin-d4 ((Rac)-BAY 12-8039-d4 (free base)) is deuterium labeled (Rac)-Moxifloxacin. (Rac)-Moxifloxacin ((Rac)-BAY 12-8039 free base) is the isoform of Moxifloxacin Hydrochloride (HY-66011), which is an oral 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia .
L-Phenylalanine-d7 is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
Nifedipine-13C8 is a deuterated labeled Nifedipine . Nifedipine (BAY-a-1040) is a potent calcium channel blocker and agent of choice for cardiac insufficiencies.
L-Phenylalanine-d8 is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
1,2-Dioleoyl-sn-glycero-3-phosphocholine-d9 is deuterium labeled 1,2-Dioleoyl-sn-glycero-3-phosphocholine. 1,2-Dioleoyl-sn-glycero-3-phosphocholine (DOPC) is a phospholipid and is commonly used alone, or with other components, in the generation of micelle
Diethylene glycol-d8(2,2'-Oxybis(ethan-1-ol)-d8) is the deuterium labeled Diethylene glycol (HY-B1952). Diethylene glycol has excellent solubility and reactivity in certain chemical reactions and can help accelerate the activation of certain reactants.
Tolfenamic acid- 13C6 is the 13C6 labeled Tolfenamic acid. Tolfenamic Acid (GEA 6414) is a non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1.
Octanoic acid- 13C4 is the 13C labeled Octanoic acid. Octanoic acid (Caprylic acid) is an oily liquid with a slightly unpleasant rancid taste and used commercially in the production of esters used in perfumery and also in the manufacture of dyes.
N-(Phenylacetyl-d5)glycine is the deuterium labeled Phenylacetylglycine. Phenylacetylglycine is a gut microbial metabolite that can activate β2AR. Phenylacetylglycine protects against cardiac injury caused by ischemia/reperfusion[1][2].
rac cis-Moxifloxacin-d4 (hydrochloride) is the deuterium labeled Moxifloxacin hydrochloride. Moxifloxacin Hydrochloride (BAY 12-8039) is an oral 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia[1][2].
DPPC-13C2 is a deuterated labeled DPPC . DPPC (129Y83) is a phosphoglyceride that can be used to prepare lipid monolayers, bilayers, and liposomes. DPPC is the main lipid component of pulmonary surfactant. Dppc-liposome can be effectively used as a delivery vector to induce an immune response against GSL antigen in mice [3] .
Hydrochlorothiazid- 13C,d2 is the 13C- and deuterium labeled Hydrochlorothiazide. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect[1][2][3].
Glycolic acid- 13C2 is the 13C-labeled Glycolic acid (HY-W015967). Glycolic acid- 13C2 is an inhibitor of tyrosinase, suppressing melanin formation and lead to a lightening of skin colour.
Secalciferol-d6 is the deuterium labeled Secalciferol. Secalciferol is a metabolite of Vitamin D, a possibly anti-inflammatory steroid which is involved in bone ossification[1][2].
Triacetonamine-d17 (2,2,6,6-Tetramethyl-4-piperidone-d17) is the deuterium labeled Triacetonamine. Triacetonamine has oral activity and can induce acute liver failure (ALF) in rats [3].
Diphenyl ether- 13C12 is 13C labeled Diphenyl ether. Oxydibenzene is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Methyl arachidonate- 13C4 (Arachidonic acid methyl ester- 13C4) is 13C labeled Methyl arachidonate. Methyl arachidonate (Arachidonic acid methyl ester) is a fatty acid methyl ester resulting from the formal condensation of the carboxy group of arachidonic acid with methanol. Methyl arachidonate has activity of human blood serum metabolite .
Uridine- 13C5 (β-Uridine- 13C5) is a 13C labeled Uridine (HY-B1449). Uridine (β-Uridine) is a nucleoside compound consisting of uracil and a ribose ring, which are linked by a β-N1- glycosyl bond.
Octachlorodibenzo-p-dioxin- 13C12 is Octachlorodibenzo-p-dioxin- 13 C-labeled octachlorodibenzo-p-dioxin- 13C. Octachlorodibenzo-p-dioxin is a widespread environmental pollutant .
6-Mercaptopurine- 13C2, 15N is the 13C- and 15N-labeled 6-Mercaptopurine. 6-Mercaptopurine is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive agent.
Entecavir- 13C2, 15N (BMS200475- 13C2, 15N; SQ34676- 13C2, 15N) is a 13C- and 15N-labeled Entecavir (HY-13623). Entecavir (SQ 34676; BMS 200475) is a potent and selective inhibitor of HBV, with an EC50 of 3.75 nM in HepG2 cell.
4-(4-Fluorobenzylamino)-1-methylpiperidine-d2(N-[(4-Fluorophenyl)methyl]-1-methyl-4-piperidinamine-d2) is the deuterium labeled 4-(4-Fluorobenzylamino)-1-methylpiperidine.
Mandelic acid-2,3,4,5,6-d5 is the deuterium labeled Mandelic acid. Mandelic acid ((±)-Mandelic acid), an alpha-hydroxycarboxylic acid, has been widely used as an intermediate of pharmaceutical and fine chemicals. Mandelic acid shows antimicrobial activity and has been used for the research of urinary tract infections and vaginal trichomoniasis. Mandelic acid exhibits high sperm-immobilizing activity and low vaginal irritation[1][2].
Hypoxanthine- 13C, 15N2 is a 15N-labeled and 13C-labled Furaltadone. Furaltadone, a nitrofuran agent, has the potential for the study in infections of chickens with salmonella enteritidis. Furaltadone is inhibitory and bactericidal in vitro for staphylococci
Cefdinir- 13C, 15N2 (FK-482- 13C, 15N2) is 13C and 15N labeled Cefdinir. Cefdinir (FK-482) is a semi-synthetic, broad-spectrum antibiotic in the third generation of the cephalosporin class, which is proved to be effective for infections caused by several Gram-negative and Gram-positive bacteria. Cefdinir can be used for the research of common bacterial infections of the ear, sinus, throat, and skin .
Zileuton- 13C2, 15N is 15N and 13C labeled Zileuton (HY-14164). Zileuton is a potent and selective inhibitor of 5-lipoxygenase with antiasthmatic properties.
Vildagliptin- 13C5, 15N (LAF237- 13C5, 15N; NVP-LAF 237- 13C5, 15N) is a 13C- and 15N-labeled Vildagliptin (HY-14291). Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity .
4-Trifluoromethylsalicylic acid- 13C6 is the 13C labeled 4-Trifluoromethylsalicylic acid[1]. 4-Trifluoromethylsalicylic acid is a platelet aggregation inhibitor[2].
4-Methyl-2-oxopentanoic acid-d7 (α-Ketoisocaproic acid-d7) sodium is the deuterium labeled 4-Methyl-2-oxopentanoic acid (HY-W012722).4-Methyl-2-oxopentanoic acid is a metabolite of L-leucine and is involved in energy metabolism. 4-Methyl-2-oxopentanoic acid increases endoplasmic reticulum stress, promotes lipid accumulation in preadipocytes and insulin resistance by impairing mTOR and autophagy signaling pathways .
Oxaloacetic acid- 13C4 is the 13C-labeled Oxaloacetic acid. Oxaloacetic acid (2-Oxosuccinic acid) is a metabolic intermediate involved in several ways, such as citric acid cycle, gluconeogenesis, the urea cycle, the glyoxylate cycle, amino acid synthesis, and fatty acid synthesis[1][2][3].
N-Lactoyl-Phenylalanine- 13C6 (Lac-Phe- 13C6) is 13C labeled N-Lactoyl-Phenylalanine. N-Lactoyl-Phenylalanine is a blood-derived signaling metabolite that can be induced by exercise. N-Lactoyl-Phenylalanine can reduce obesity and improve glucose tolerance .
Isoallolithocholic acid-d4 (3β-Hydroxy-5α-cholanic acid-d4) is deuterium labeled Isoallolithocholic acid. Isoallolithocholic acid (3β-Hydroxy-5α-cholanic acid), a derivative of Lithocholic acid (HY-10219), is a T cell regulator. Isoallolithocholic acid enhances regulatory T cells (Tregs) differentiation .
Tauro-α-muricholic acid-d4-1 (sodium) is deuterium labeled Tauro-α-muricholic acid (sodium). Tauro-α-muricholic acid (T-α-MCA) sodium is a FXR (Farnesoid X receptor) antagonist (IC50=28μM). Tauro-α-muricholic acid sodium is also a endogenous metabolite that can be found in cecal [3].
Zafirlukast- 13C,d6 is the 13C- and deuterium labeled Zafirlukast. Zafirlukast (ICI 204219) is a potent orally active leukotriene D4 (LTD4) receptor antagonist. Zafirlukast shows anti-asthmatic, anti-inflammatory and anti-bacterial effects.
Sucrose- 13C6-1 is 13C labeled Sucrose. Sucrose (D-(+)-Saccharose) is a disaccharide which is composed of two monosaccharides, glucose and fructose. Sucrose?can be applied in some animal models, including metabolic disease, obesity,?diet on preference,?and diabetes, et al .
Adenosine-d-2 is the deuterium labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular phys
Upadacitinib- 15N,d2 (ABT-494- 15N,d2) is the deuterium-labeled Upadacitinib (HY-19569). Upadacitinib- 15N,d2 (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib- 15N,d2 (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib- 15N,d2 (ABT-494) can be used for several autoimmune disorders research .
Emtricitabine- 15N,d2 is a 15N-labeled and deuterium labeled Emtricitabine. Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with an EC50 of 0.01 μM in PBMC cell. It is an antiviral agent for the treatment of HIV infection.
NH2-C2-NH-Boc-d4 is the deuterium labeled NH2-C2-NH-Boc[1]. NH2-C2-NH-Boc (PROTAC Linker 22) is a alkyl chain-based PROTAC linker can be used in the synthesis of PROTACs[2].
Adenosine-d-1 is the deuterium labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular phys
Guanosine triphosphate- 15N5 (GTP- 15N5) dilithium is 15N labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19.
1-Palmitoyl-2-oleoyl-sn-glycero-3-PC-d31 is deuterium labeled 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC (POPC), a phospholipid, is a major component of biological membranes. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC is used for
Levomefolic acid- 13C5 is the 13C labeled Levomefolic acid[1]. Levomefolic acid (L-5-MTHF) is an orally active, brain-penetrant natural active form of folic acid and is one of the most widely used folic acid food supplements[2][3].
Isoallolithocholic acid-d2 is the deuterium labeled Isoallolithocholic acid (HY-B0172A). Isoallolithocholic acid is a T cell regulator and enhances regulatory T cells (Tregs) differentiation[1][2].
Apatinib-d8 (free base) is the deuterium labeled Apatinib free base[1]. Apatinib free base (YN968D1 free base) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 (IC50=1 nM). Apatinib free base (YN968D1 free base) is an anti-angiogenic drug for the research of advanced or metastatic gastric cancer. Apatinib free base (YN968D1 free base) potently inhibits Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. It also inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ[2][3][4].
Saxagliptin-15N,d2 Hydrochloride (BMS-477118-15N,d2 Hydrochloride) is the 15N and deuterium labeled isotope of Saxagliptin (HY-10285). Saxagliptin (BMS-477118) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin has the peotential for type 2 diabetes mellitus research [3].
Guanosine triphosphate- 13C10 (GTP- 13C10) dilithium is 13C-labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19.
Cholestenone- 13C2 is the 13C labeled Cholestenone. Cholestenone (4-Cholesten-3-one), the intermediate oxidation product of cholesterol, is metabolized primarily in the liver. Cholestenone is highly mobile in membranes and influences cholesterol flip-flop and efflux. Cholestenone may cause long-term functional defects in cells[1][2][3].
rac-1-Linoleoyl-3-chloropropanediol-d5 is deuterium labeled 1-Linoleoyl-3-chloropropanediolte. 1-Linoleoyl-3-chloropropanediolte (3-Chloro-2-hydroxypropyl (9Z,12Z)-octadeca-9,12-dienoate) is an ester product .
1-Palmitoyl-2-oleoyl-sn-glycero-3-PC-d82 is deuterium labeled 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC (POPC), a phospholipid, is a major component of biological membranes. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC is used for
Thiabendazole- 13C6 is the 13C6 labeled Thiabendazole. Thiabendazole inhibites the mitochondrial helminth-specific enzyme, fumarate reductase, with anthelminthic property.
Riociguat- 13C,d6 is the 13C and deuterium labeled Riociguat (HY-14779). Riociguat is an oral stimulator of soluble guanylate cyclase (sGC) used in the treatment of pulmonary hypertension.
Salicylic acid- 13C6 is the 13C-labeled Salicylic acid (HY-B0167). Salicylic acid is a precursor to and a metabolite of Aspirin (HY-14654), can inhibit cyclo-oxygenase-2 (COX-2) activity .
17β-Estradiol sulfate-d4 (sodium) is the deuterium labeled 17β-Estradiol sulfate 17β-Estradiol sulfate (sodium), also known as β-Estradiol 3-sulfate sodium salt, is a neuroactive steroid[1][2].
2-Nonyl-3-hydroxy-4-quinolone-d4 (C9-PQS-d4) is deuterium labeled 2-Nonyl-3-hydroxy-4-quinolone. 2-nonyl-3-hydroxy-4-Quinolone (C9-PQS) is a quinolone compound produced by P. aeruginosa and other related bacterias. 2-nonyl-3-hydroxy-4-Quinolone is a quorum sensing (QS) signal molecule that controls the expression of many virulence genes as a function of cell population density .
5-Methylcytidine 5'-triphosphate-d8 trisodium is the deuterium-labeled form of 5-Methylcytidine 5'-triphosphate trisodium (HY-147338A). 5-Methylcytidine 5'-triphosphate (5-Methyl-CTP) trisodium is a modified nucleoside triphosphate. 5-Methylcytidine 5'-triphosphate trisodium can be used to replace unmodified mRNA, resulting in the increase of translational properties and stability, as well as the reduction of innate immune responses in human and other mammalian cells .
Lamivudine- 15N,d2 is 15N and deuterated labeled Lamivudine (HY-B0250). Lamivudine (BCH-189) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS .
Methyl arachidonate- 13C5 (Arachidonic acid methyl ester- 13C5) is 13C labeled Methyl arachidonate. Methyl arachidonate (Arachidonic acid methyl ester) is a fatty acid methyl ester resulting from the formal condensation of the carboxy group of arachidonic acid with methanol. Methyl arachidonate has activity of human blood serum metabolite .
Triclocarban- 13C13 (3,4,4'-Trichlorocarbanilide- 13C13) is 13C labeled Triclocarban. Triclocarban (3,4,4′-Trichlorocarbanilide), a broad spectrum antibacterial compound, is widely used in a broad range of applications such as the production of soaps, skin creams, toothpastes and deodorants. Triclocarban is a potential endocrine-disrupting chemical with the capacity to modulate androgen and estrogen activities as well as other hormone-mediated biological processes [3][3] .
Adenosine monophosphate- 13C10 (AMP- 13C10) dilithium is 13C-labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction [3].
Sumatriptan-d6 (formate) (GR 43175 free base-d6 (formate)) is deuterium labeled Sumatriptan. Sumatriptan (GR 43175) is an orally active 5-HT1 receptor agonist with IC50s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT1D, 5-HT1B and 5-HT1F receptors, respectively. Sumatriptan can be used for migraine headache research [3] .
Sacubitril- 13C4 (hemicalcium salt) is a 13C-labeled and deuterium labeled Sacubitril hemicalcium salt. Sacubitril (AHU-377) hemicalcium salt is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril hemicalcium salt is a component of the heart failure medicine LCZ696[1].
L-Histidine- 13C6 (hydrochloride hydrate) is the 13C-labeled L-Histidine hydrochloride hydrate. L-Histidine hydrochloride hydrate (H-His-OH.HCl.H2O) is an endogenous metabolite.
Methyl Paraben- 13C6 (Methyl 4-hydroxybenzoate- 13C6) is a 13C labeled Methyl Paraben (HY-N0349) . Methyl Paraben, isolated from the barks of Tsuga dumosa the methyl ester of p-hydroxybenzoic acid, is a standardized chemical allergen. Methyl Paraben is a stable, non-volatile compound used as an antimicrobial preservative in foods, agents and cosmetics. The physiologic effect of Methyl Paraben is by means of increased histamine release, and cell-mediated immunity .
4-Hydroxyestrone- 13C6 is a 13C-labeled Hypoxanthine. Hypoxanthine, a purine derivative, is a potential free radical generator and could be used as an indicator of hypoxia.
Orotic acid- 13C, 15N2 (monohydrate) is the 13C and 15N labeled Orotic acid[1]. Orotic acid (6-Carboxyuracil), a precursor in biosynthesis of pyrimidine nucleotides and RNA, is released from the mitochondrial dihydroorotate dehydrogenase (DHODH) for conversion to UMP by the cytoplasmic UMP synthase enzyme. Orotic acid is a marker for measurement in routine newborn screening for urea cycle disorders. Orotic acid can induce hepatic steatosis and hepatomegaly in rats[2][3][4].
Pregnenolone monosulfate-d4 (sodium) is the deuterium labeled Pregnenolone monosulfate. Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium can protect the brain from cannabis intoxication[1][2]. Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
(2R)-Octyl-α-hydroxyglutarate-d17 ((2R)-Octyl-2-HG-d17) is deuterium labeled (2S)-Octyl-α-hydroxyglutarate. (2S)-Octyl-α-hydroxyglutarate ((2S)-Octyl-2-HG) is a modified form of S-isomer 2-Hydroxyglutarate .
Indole-3-carboxaldehyde- 13C8 (3-Formylindole- 13C8) is the 13C-labeled Indole-3-carboxaldehyde (HY-W007376). Indole-3-carboxaldehyde, a banlangen extract, is the product of the oxidative degradation of indole-3-acetic acid (IAA) by crude enzyme preparations from etiolated pea seedlings. Indole-3-carboxaldehyde is a biochemical used to prepare analogs of the indole phytoalexin cyclobrassinin. Indole-3-carboxaldehyde also enhances the epithelial barrier and anti-inflammatory activity in the intestinal tract .
L-Glutamine- 13C5 is the 13C-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells[1][2].
(Z)-Aconitic acid- 13C6 is the 13C-labeled (Z)-Aconitic acid (HY-W016814). (Z)-Aconitic acid- 13C6 (cis-Aconitic acid) is the cis-isomer of Aconitic acid. (Z)-Aconitic acid- 13C6 (cis-Aconitic acid) is an intermediate in the tricarboxylic acid cycle produced by the dehydration of citric acid.
Calcifediol- 13C5 monohydrate is the 13C-labeled Calcifediol monohydrate. Calcifediol monohydrate (25-hydroxy Vitamin D3 monohydrate), is an effective VDR ligand and VD supplement. Calcifediol is a prohormone of the vitamin D endocrine system (VDES) and is hydroxylated in the liver to produce the active form, calcitriol. Calcifediol can rapidly increase serum VD levels [3].
Deoxythymidine-5'-triphosphate- 15N2 (dTTP- 15N2) dilithium is 15N labeled Deoxythymidine-5'-triphosphate (HY-138615). Deoxythymidine-5'-triphosphate (dTTP) is one of the four nucleoside triphosphates. Deoxythymidine-5'-triphosphate (dTTP) is used in the synthesis of DNA.
ATP- 13C10 (Adenosine 5'-triphosphate- 13C10) dilithium is 13C-labeled ATP (HY-B2176). ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation.
Benzisothiazolinone-13C5 (1,2-Benzothiazol-3-one-13C5) is a 13C-labeled Benzisothiazolinone. Benzisothiazolinone is widely used as an antiseptic and antibacterial agent .
MCPA- 13C8 is the 13C-labeled MCPA. MCPA is a phenoxy herbicide, and widely used to control annual and perennial broad leaved weeds, including poppy, thistles and docks, in crops such as cereals, rice, linseed, flax, grassland and turf[1][2].
Pyruvic acid- 13C,d4 is the deuterium and 13C labeled Pyruvic acid[1]. Pyruvic acid is an intermediate metabolite in the metabolism of carbohydrates, proteins, and fats[2].
Flavin adenine dinucleotide- 13C5 (FAD- 13C5) ammonium is 13C labeled Flavin adenine dinucleotide (HY-B1654). Flavin adenine dinucleotide (FAD) is a redox cofactor, more specifically a prosthetic group of a protein, involved in several important enzymatic reactions in metabolism.
SN-38 glucuronide- 13C6 is the 13C labeled SN-38 glucuronide (HY-126373) . SN-38 glucuronide is an inactive metabolite of the cancer agent Irinotecan. Irinotecan is a topoisomerase I inhibitor which can be used for researching colon and rectal cancer .
Guanosine 5'-diphosphate- 13C10 (GDP- 13C10) dilithium is 13C-labeled Guanosine 5'-diphosphate (HY-113066). Guanosine 5'-diphosphate (GDP) is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K + channel. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Guanosine 5'-diphosphate can be used in the research of inflammation, such as anemia of inflammation (AI).
DL-Lysine- 15N2 hydrochloride ((±)-2,6-Diaminocaproic acid- 15N2 hydrochloride) is 15N labeled DL-Lysine (HY-B2236). DL-Lysine is a racemic mixture of the D-Lysine and L-Lysine. Lysine is an α-amino acid that is used in the biosynthesis of proteins.
Pyridinium bisretinoid A2E-d4 TFA is the deuterium-labeled Pyridinium bisretinoid A2E (HY-134928). Pyridinium bisretinoid A2E (A2E)is an initiator of blue-light-induced apoptosis. Photoactivation of Pyridinium bisretinoid A2E mediates autophagy and the production of reactive oxygen species [3] .
Uridine 5'-monophosphate-15N2 is the 15N labeled Uridine 5'-monophosphate[1]. Uridine 5'-monophosphate (5'- Uridylic acid), a monophosphate form of UTP, can be acquired either from a de novo pathway or degradation products of nucleotides and nucleic acids in vivo and is a major nucleotide analogue in mammalian milk[2].
6-(γ,γ-Dimethylallylamino)purine-d6 is the deuterium labeled 6-(γ,γ-Dimethylallylamino)purine (HY-112103). 6-(γ,γ-Dimethylallylamino)purine is a plant growth substance[1][2].
L-Alanine- 13C2 is the 13C-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
DL-Lysine- 13C6 hydrochloride ((±)-2,6-Diaminocaproic acid- 13C6 hydrochloride) is 13C-labeled DL-Lysine (HY-B2236). DL-Lysine is a racemic mixture of the D-Lysine and L-Lysine. Lysine is an α-amino acid that is used in the biosynthesis of proteins.
L-Glutamine- 15N2 is the 15N-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells .
Salmeterol- 13C6 (xinafoate) is the 13C6 labeled Salmeterol (xinafoate). Salmeterol (GR 33343X) xinafoate is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively.
Pregnenolone-d4-1 is the deuterium labeled Pregnenolone. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication[1][2]. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
ATP- 15N5 (Adenosine 5'-triphosphate- 15N5) dilithium is 15N labeled ATP (HY-B2176). ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation.
Tempol-d17, 15N is the deuterium labeled Tempol[1]. Tempol is a general superoxide dismutase (SOD)-mimetic agent that efficiently neutralizes reactive oxygen species (ROS)[2][3].
Deoxythymidine-5'-triphosphate- 13C10 (dTTP- 13C10) dilithium is 13C-labeled Deoxythymidine-5'-triphosphate (HY-138615). Deoxythymidine-5'-triphosphate (dTTP) is one of the four nucleoside triphosphates. Deoxythymidine-5'-triphosphate (dTTP) is used in the synthesis of DNA.
2′,2′-Difluorodeoxyuridine- 13C, 15N2 (dFdU- 13C, 15N2; 2',2'-Difluoro-2'-deoxyuridine- 13C, 15N2) is a 13C- and 15N-labeled compound. 2’,2’-Difluorodeoxyuridine (dFdU; 2',2'-Difluoro-2'-deoxyuridine) is the main metabolite of Gemcitabine (HY-17026). 2’,2’-Difluorodeoxyuridine causes a concentration- and schedule- dependent radiosensitising effect in vitro. 2’,2’-Difluorodeoxyuridine arrests cell cycle at the early S phase and induces apoptosis in cancer cells [3] .
(Rac)-Folic acid- 13C5, 15N is the 13C-labeled and 15N-labeled Folic acid. Folic acid (Vitamin M; Vitamin B9) is a B vitamin; is necessary for the production and maintenance of new cells, for DNA synthesis and RNA synthesis.
Lysophosphatidylcholine 18:2-d9 is deuterium labeled Lysophosphatidylcholine 18:2. Lysophosphatidylcholine 18:2 (1-Linoleoyl-2-Hydroxy-sn-glycero-3-PC), a lysophospholipid, is a potential biomarker identified from insulin resistance (IR) polycystic ovary
(1S,2R)-Tranylcypromine-d5 (hydrochloride) is the deuterium labeled Tranylcypromine hydrochloride[1]. Tranylcypromine hydrochloride (SKF 385 hydrochloride) is an irreversible inhibitor of lysine-specific demethylase 1 (LSD1/BHC110) and monoamine oxidase (MAO). Tranylcypromine hydrochloride inhibits LSD1, MAO A and MAO B with IC50s of 20.7, 2.3 and 0.95 μM, respectively. Tranylcypromine hydrochloride can be used for the research of depression[2][3][4].
11-Beta-hydroxyandrostenedione-d7 is the deuterium labeled 11-Beta-hydroxyandrostenedione. 11-Beta-hydroxyandrostenedione (4-Androsten-11β-ol-3,17-dione) is a steroid mainly found in the the adrenal origin (11β-hydroxylase is present in adrenal tissue, but absent in ovarian tissue). 11-Beta-hydroxyandrostenedione is a 11β-hydroxysteroid dehydrogenase (11βHSD) isozymes inhibitor [1][2]
Histamine-α,α,β,β-d4 (dihydrochloride) is the deuterium labeled Histamine. Histamine is an organic nitrogenous compound involved in local immune responses as well as regulating physiological function in the gut and acting as a neurotransmitter.
2'-Deoxyadenosine-5'-triphosphate- 13C10 (dATP- 13C10) dilithium is 13C-labeled 2'-Deoxyadenosine-5'-triphosphate (HY-136648). 2'-Deoxyadenosine-5'-triphosphate (dATP) is a nucleotide used in cells for DNA synthesis (or replication), as a substrate of DNA polymerase.
DMT-dA(bz) Phosphoramidite- 15N5 is the 15N labeled DMT-dA(bz) Phosphoramidite[1]. DMT-dA(bz) Phosphoramidite is typically used in the synthesis of DNA[2].
(Rac)-Nebivolol-d2, 15N is 15N and deuterated labeled (Rac)-Nebivolol (HY-B0203B). (Rac)-Nebivolol ((Rac)-R 065824) is a racemic isomer of Nebivolol. Nebivolol is a selective β1-adrenergic receptor antagonist with an IC50 value of 0.8 nM. Nebivolol can prevent up-regulation of Nox2/NADPH oxidase and lipoperoxidation in the early stages of ethanol-induced cardiac toxicity. Vasodilatory activity .
Vigabatrin- 13C,d2 (hydrochloride) is the 13C- and deuterium labeled Vigabatrin (hydrochloride). Vigabatrin hydrochloride (γ-Vinyl-GABA hydrochloride), a inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin hydrochloride is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase[1][2][3].
γ-Aminobutyric acid-4,4-d2 is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
9(S)-HODE- 13C18 ((+)-α-Dimophecolic acid- 13C18) is 13C labeled 9S-HODE. 9S-HODE (Alpha-dimorphecolic acid) is an octadecadienoic acid and the main active derivative of linoleic acid, which can reduce the viability of HL-60 cells and induce apoptosis. 9S-HODE is rich in lipid peroxidation (LPO) products and is almost an ideal marker for LPO .
3-Hydroxybutyric acid- 13C4 (sodium) is the 13C labeled 3-Hydroxybutyric acid sodium (HY-W010452). 3-Hydroxybutyric acid sodium is a metabolite that is elevated in type I diabetes, and can modulate the properties of membrane lipids[1].
3-Hydroxybutyric acid- 13C2 (sodium) is the 13C labeled 3-Hydroxybutyric acid sodium (HY-W010452). 3-Hydroxybutyric acid sodium is a metabolite that is elevated in type I diabetes, and can modulate the properties of membrane lipids[1].
2,4-D- 13C6 is the 13C-labeled 2,4-D. 2,4-D (2,4-Dichlorophenoxyacetic acid) is a selective systemic herbicide for the control of broad-leaved weeds. 2,4-D acts as a plant hormone, causing uncontrolled growth in the meristematic tissues. 2,4-D inhibits DNA and protein synthesis and thereby prevents normal plant growth and development[1].
γ-Aminobutyric acid- 13C4 is the 13C-labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
Acetyl coenzyme A- 13C2 lithium is the 13C-labeled Acetyl coenzyme A (HY-114293). Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Ethyl maltol-d5 is the deuterium labeled Ethyl maltol. Ethyl maltol (2-Ethyl-3-hydroxy-4H-pyran-4-one) is an orally active and important food additive and flavor enhancer. Ethyl maltol is less toxic to rats and dogs. Ethyl maltol can enhance copper-mediated cytotoxicity and induce apoptosis in lung epithelial cells [3].
2-Ketoglutaric acid-13C2 is a deuterated labeled 2-Ketoglutaric acid . 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM) .
dGTP- 13C10 (2'-Deoxyguanosine-5'-triphosphate- 13C10) dilithium is 13C-labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
2'-Deoxyadenosine-5'-triphosphate- 15N5 (dATP- 15N5) dilithium is 15N labeled 2'-Deoxyadenosine-5'-triphosphate (HY-136648). 2'-Deoxyadenosine-5'-triphosphate (dATP) is a nucleotide used in cells for DNA synthesis (or replication), as a substrate of DNA polymerase.
Prostaglandin E2-1-glyceryl ester-d5 (PGE2-1-glyceyl ester-d5) is deuterium labeled Prostaglandin E2-1-glyceryl ester. Prostaglandin E2-1-glyceryl ester, a Prostaglandin Glycerol Ester, is an endocannabinoid ligand for the CB1 receptor. Prostaglandin E2-1-glyceryl ester induces rapid, transient elevation of intracellular free Ca 2+ .
L-Hydroxyproline-d4 is deuterium labeled L-Hydroxyproline. L-Hydroxyproline, one of the hydroxyproline (Hyp) isomers, is a useful chiral building block in the production of many pharmaceuticals .
1,2-Dioctanoyl-3-chloropropanediol-d5 is deuterium labeled 1,2-Dioctanoyl-3-chloropropanediol. 1,2-Dioctanoyl-3-chloropropanediol (3-Chloropropane-1,2-diyl dioctanoate) is an ester product .
11-Beta-hydroxyandrostenedione-d4 is the deuterium labeled 11-Beta-hydroxyandrostenedione. 11-Beta-hydroxyandrostenedione (4-Androsten-11β-ol-3,17-dione) is a steroid mainly found in the the adrenal origin (11β-hydroxylase is present in adrenal tissue, but absent in ovarian tissue). 11-Beta-hydroxyandrostenedione is a 11β-hydroxysteroid dehydrogenase (11βHSD) isozymes inhibitor[1][2].
VD3-d6 (Vitamin D3-26,26,26,27,27,27-d6) is deuterated VD3. Compounds labeled with stable or radioactive isotopes can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
L-Glutathione reduced- 13C2, 15N is the 13C- and 15N-labeled L-Glutathione reduced. L-Glutathione reduced (GSH) is an endogenous antioxidant and is capable of scavenging oxygen-derived free radicals.
1-Stearoyl-2-15(S)-HETE-sn-glycero-3-PE-d11 (15(S)-HETE-SAPE-d11) is deuterium labeled 1-Stearoyl-2-15(S)-HETE-sn-glycero-3-PE. 1-Stearoyl-2-15(S)-HETE-sn-glycero-3-PE is a phospholipid that contains stearic acid (HY-B2219) at the sn-1 position and 15(S)-HETE at the sn-2 position. It is formed in human peripheral monocytes activated by the calcium ionophore A23187 (HY-N6687) by direct oxidation of 1-stearoyl-2-arachidonoyl-sn-glycero-3-PE (SAPE) by 15-LO. Phosphoethanolamine (PE) HETEs (PE-HETEs), including 1-stearoyl-2-15(S)-HETE-sn-glycero-3-PE, are the main source of esterified HETE in ionophore-activated monocytes .
Uridine 5'-monophosphate- 13C9 (5'- Uridylic acid- 13C9) dilithium is 13C-labeled Uridine 5'-monophosphate (HY-101981). Uridine 5'-monophosphate (5'- Uridylic acid), a monophosphate form of UTP, can be acquired either from a de novo pathway or degradation products of nucleotides and nucleic acids in vivo and is a major nucleotide analogue in mammalian milk.
L-Valine-d8 is a deuterated form of L-Valine. L-Valine-d8 can be used in the labelled synthesis of L-valineamide-d8 intermediate[1]. L-Valine is one of 20 proteinogenic amino acids. L-Valine is an essential amino acid[2].
Cefazolin- 13C2, 15N (Cephazolin- 13C2, 15N) is 13C and 15N labeled Cefazolin. Cefazolin (Cephazolin) is a first-generation cephalosporin antibiotic and can be used in varieties of bacterial infections research . Cefazolin has anti-inflammatory effect and can attenuate post-operative cognitive dysfunction (POCD) .
Emtricitabine- 13C, 15N2 (BW1592- 13C, 15N2) is a 13C- and 15N-labeled Emtricitabine (HY-17427). Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with an EC50 of 0.01 μM in PBMC cell. It is an antiviral agent for the treatment of HIV infection.
Uridine 5'-monophosphate- 15N2 (5'-?Uridylic acid- 15N2) dilithium is 15N labeled Uridine 5'-monophosphate (HY-101981). Uridine 5'-monophosphate (5'-?Uridylic acid), a monophosphate form of UTP, can be acquired either from a de novo pathway or degradation products of nucleotides and nucleic acids in vivo and is a major nucleotide analogue in mammalian milk.
rU Phosphoramidite- 13C9 (DMT-2'O-TBDMS-rU phosphoramidite- 13C9) is 13C-labeled rU Phosphoramidite (HY-W048482). rU Phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
Nitrofurazone- 13C, 15N2 (Nitrofural- 13C, 15N2) is the 13C and 15N labled Nitrofurazone (HY-B0226) . Nitrofurazone is a potential antibiotic that can be used topically to treat wounds, burns, ulcers and skin infections to combat various microorganisms and to prepare surfactants . Nitrofurazone may affect the ecosystem function in Marine environment and affect the functional processes of epiphytic fauna [3].
L-Arginine-1,2- 13C2 (hydrochloride) is the 13C-labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
[1,1'-Biphenyl]-3-amine-13C6 hydrochloride (Biphenyl-3-amine-13C6 hydrochloride) is the 13C labeled isotope of [1,1'-Biphenyl]-3-amine hydrochloride (HY-W106014) .
Uridine 5′-diphosphoglucose- 13C6 (disodium) is the 13C labeled Uridine 5′-diphosphoglucose disodium salt[1]. Uridine 5′-diphosphoglucose disodium salt (UDP-D-Glucose disodium salt) is the precursor of glucose-containing oligosaccharides, polysaccharides, glycoproteins, and glycolipids in animal tissues and in some microorganisms. Uridine-5′-diphosphoglucose is an agonist of the P2Y14 receptor, a neuroimmune system GPCR[2].
L-Alanine- 13C,d is the 13C- and deuterium labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
L-Phenylalanine- 13C6 is the 13C-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
L-Phenylalanine- 13C9 is the 13C-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
L-Alanine- 15N,d4 is the deuterium and 15N-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
rU Phosphoramidite- 15N2 (DMT-2'O-TBDMS-rU phosphoramidite- 15N2) is 15N labeled rU Phosphoramidite (HY-W048482). rU Phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
trans-2,cis-6-Nonadienal- 13C2 is 13C labeled 4-Ethylphenol (HY-W012836). 4-Ethylphenol is a volatile phenolic compound associated with off-odour in wine.
MAPI is a polypeptide irreversible 3C cysteine protease (SV3CP) inhibitor. MAPI inhibits SV3CP by covalently binding its C-terminal Michael-acceptor extension to the active site thiol of SV3CP Cys 139. MAPI is promising for research of noroviruses infection .
Riluzole- 13C, 15N2 is the 13C and 15N labeled Riluzole[1]. Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM[2][3].
(E)-3-Methyl-2-hexenoic acid-d5 ((2E)-3-Methyl-2-hexenoic acid-d5) is a deuterium labeled (E)-3-Methyl-2-hexenoic acid. (E)-3-Methyl-2-hexenoic acid is an axillary odor-related compound .
2-Thiouracil- 13C, 15N2 is the 13C, 15N labeled 2-Thiouracil. 2-Thiouracil (Thiouracil) is an antithyroid compound. 2-Thiouracil can function as a highly specific melanoma seeker. 2-Thiouracil is a selective inhibitor of neuronal nitric oxide synthase (nNOS) with a Ki of 20 μM.
Lenalidomide- 13C5, 15N is 15N and 13C labeled Lenalidomide (HY-A0003). Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
Ethyl linoleate-d5 (Linoleic Acid ethyl ester-d5) is deuterium labeled Ethyl linoleate. Ethyl linoleate (Linoleic Acid ethyl ester) inhibit the development of atherosclerotic lesions and the expression of inflammatory mediators . .
Fluconazole-13C2,15N (UK-49858-13C2,15N) is the 13C and 15N labeled isotope of Fluconazole (HY-B0101). Fluconazole (UK-49858) is a triazole antifungal agent with excellent activities against a broad range of fungi, especially against Candida albicans. Fluconazole inhibits C. albicans and Candida kefyr with IC99s range from 0.20 μg/mL to 0.39 μg/mL .
Gemcitabine- 13C, 15N2 (hydrochloride) is the 13C and 15N labeled Gemcitabine hydrochloride[1]. Gemcitabine Hydrochloride (LY 188011 Hydrochloride) is a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent. Gemcitabine Hydrochloride inhibits DNA synthesis and repair, resulting in autophagyand apoptosis[2][3].
Tranexamic acid- 13C2, 15N (Cyclocapron- 13C2, 15N) is the 13C2 and 15N labeled Tranexamic acid. Tranexamic acid is an antifibrinolytic agent that alleviates liver damage and fibrosis in mouse models of chronic bile duct injury .
(3S,5R)-Fluvastatin-d6 is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway[1].
Allolithocholic Acid-d4 (3α-hydoxy-5α-Cholaoic Acid-d4, allo-LCA-d4) is deuterium labeled Allolithocholic acid. Allolithocholic acid is a steroid acid could found in normal serum and feces. Allolithocholic acid facilitates excretion, absorption, and transport of fats and sterols in the intestine and liver .
Pomalidomide- 15N, 13C5 is 15N and 13C labeled Pomalidomide (HY-10984). Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.
(9S,13R)-12-OPDA-d5 is an isotopic label of (9S,13R)-12-oxyphytodienoic acid. (9S,13R)-12-Oxophytodienoic acid is an isomer of 12-oxoPDA (HY-118828). (9S,13R)-12-Oxo phytodienoic Acid is a lipoxygenase metabolite in green plant leaves .
Nonanoic acid-d2 is the deuterium labeled Nonanoic acid[1]. Nonanoic acid is a naturally-occurring saturated fatty acid with nine carbon atoms. Nonanoic acid significantly reduces bacterial translocation, enhances antibacterial activity, and remarkably increases the secretion of porcine β-defensins 1 (pBD-1) and pBD-2[2].
L-Glutamine-1,2- 13C2 is the 13C-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells .
Diethyl succinate- 13C4 is the 13C labeled Diethyl succinate[1]. Diethyl succinate (Diethyl Butanedioate) is used at physiological pH and crosses biological membranes, incorporates into cells in tissue culture and is metabolized by the TCA cycle. Diethyl succinate is known to be non-toxic and used in fragrances and flavoring[2].
L-Ascorbic acid- 13C6-1 (L-Ascorbate-1; Vitamin C- 13C6-1) is a 13C labeled L-Ascorbic acid (HY-B0166) . L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor [3] . L-Ascorbic acid exhibits anti-cancer effects through the generation of reactive oxygen species (ROS) and selective damage to cancer cells .
5-Fluorouracil- 13C, 15N2 is the 13C and 15N labeled 5-Fluorouracil[1]. 5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer[2][3]. 5-Fluorouracil also inhibits HIV[4].
L-Phenylalanine- 15N,d8 is the deuterium and 15N-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca2+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
Taurine- 13C2, 15N is the 13C- and 15N- labeled Taurine. Taurine, a sulphur-containing amino acid and an organic osmolyte involved in cell volume regulation, provides a substrate for the formation of bile salts, and plays a role in the modulation of intracellular free calcium concentration. Taurine has the ability to activate autophagy in adipocytes[1][2][3].
Oxypurinol- 13C, 15N2-1 (Oxipurinol- 13C, 15N2-1) is 15N and 13C labeled Oxypurinol (HY-19657). Oxipurinol, the major active metabolite of Allopurinoll (HY-B0219), is an inhibitor of xanthine oxidase. Oxipurinol can be used to regulate blood urate levels and treat gout .
PSI-6206-d1, 13C, 15N2 is 15N and 13C labeled PSI-6206 (HY-15236). PSI-6206 (RO 2433) is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase. PSI-6206 low potently inhibits HCV replicon with EC90 of >100 μM.
Dienogest-13C,15N,d4 (STS 557-13C,15N,d4) is the 13C, 15N and deuterium labeled isotope of Dienogest (HY-B0084). Dienogest (STS-557) is an orally active and selective progesterone receptor agonist that effectively reduces the gene expression of COX-2, mPGES-1 and aromatase. Dienogest also inhibits the mRNA and protein expression of PGE2 synthase and the activation of NF-κB. Dienogest can be used in studies of endometriosis, menopause and menorrhagia .
Benzyl alcohol-α- 13C-α,α-d2 is the 13C-labeled Benzyl alcohol. Benzyl alcohol is an aromatic alcohol; a colorless liquid with a mild pleasant aromatic odor.
L-Alanine- 13C2, 15N is the 13C- and 15N-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
N-Acetyl-D-glucosamine- 13C6 (N-Acetyl-2-amino-2-deoxy-D-glucose- 13C6) is the 13C labled N-Acetyl-D-glucosamine (HY-A0132) . N-Acetyl-D-Glucosamine (N-Acetyl-2-amino-2-deoxy-D-glucose) is a monosaccharide derivative of glucose.
Dinoprost- 13C5 is 13C labeled Dinoprost (HY-12956). Dinoprost (Prostaglandin F2α) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost plays a key role in the onset and progression of labour .
γ-Glu-(Phe- 13C9, 15N) is the 13C and 15N labeled isotope of γ-Glu-Phe(HY-101399).γ-Glu-Phe or the postenzymatic reaction mixture enhanced the umami intensity of commercial soy sauce and model chicken soup.
13,14-Dihydro-15-keto Prostaglandin F2α-d4 (13,14-Dihydro-15-keto-PGF2α-d4) is a deuterated labeled 13,14-Dihydro-15-keto Prostaglandin F2α (HY-113208). 13,14-Dihydro-15-keto Prostaglandin F2α-d4 is an endogenous metabolite present in Blood that can be used for the research of Pregnancy .
Cyclic GMP- 13C, 15N2 is 13C and 15N labeled Cyclic GMP. Cyclic GMP (cGAMP) is an endogenous second messenger that triggers interferon production in response to cytoplasmic DNA. Cyclic GMP activates the stimulator of interferon genes (STING), activating a signaling cascade that leads to the production of type I interferons and other immune mediators [3].
L-Phenylalanine- 13C9, 15N is the 13C- and 15N-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
8-Hydroxy-2'-deoxyguanosine- 13C, 15N2 is 13C and 15N labeled 8-Hydroxy-2'-deoxyguanosine. 8-Hydroxy-2'-deoxyguanosine is a critical biomarker of oxidative stress and carcinogenesis .
Ile-(Leu-13C6,15N)-OH (TFA) is 13C- and 15N-labeled L-Isoleucyl-L-leucine (HY-W269700). L-Isoleucyl-L-leucine has a role as a metabolite and can be used to inhibit movement-induced muscle damage and muscle defective condition.
MK-6186 is a novel non-nucleoside reverse transcriptase inhibitor with sub-nanomolar activity against wild-type viruses and the two most common NNRTI-resistant RT mutants (K103N and Y181C). MK-6186 exhibits excellent antiviral activity against K103N and Y181C mutant viruses. When MK-6186 targets 12 common NNRTI-associated mutant viruses, only two relatively rare mutants (Y188L and V106I/Y188L) show high resistance, with FC values exceeding 100, while the FC values of the remaining viruses are all below 10. In addition, when MK-6186 faces 96 clinical virus isolates carrying NNRTI-resistant mutations, most (70%) viruses show more than 10-fold resistance to efavirenz (EFV), while only 29% of mutant viruses show more than 10-fold resistance to MK-6186 .
(Leu-13C6,15N)-Ile-OH (L-Leucyl-13C6,15N-L-isoleucine) TFA is the deuterium labeled Leu-Ile-OH. Leu-Ile-OH protects against neuronal death by inducing brain-derived neurotrophic factor (BDNF) and glial cell line-derived neurotrophic factor (GDNF) synthesis .
Eicosapentaenoic acid 1,2,3,4,5- 13C5 (EPA 1,2,3,4,5- 13C, FA 20:5- 13C5) is 13C labeled Eicosapentaenoic Acid. Eicosapentaenoic Acid (EPA) is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid can promote relaxation of vascular smooth muscle cells and vasodilation [3] .
Citrinin- 13C13 (NSC 186- 13C13) is the 13C labeled Citrinin (HY-N6746). Citrinin (NSC 186) is a mycotoxin that causes food contamination and has different toxic effects. Citrinin is an effective oral anticancer agent. Citrinin has various regulatory effects on mouse immune system, including regulating the number of immune cells, inducing apoptosis and autophagy of immune cells, altering toll-like receptor expression and cytokine production. Citrinin can induce oxidative stress and lead to early apoptosis of oocytes. Low doses of Citrinin have neuroprotective effects against glutamate-induced excitotoxicity in rat cortical neurons. In addition, Citrinin also has antibacterial activity [3] .
Astressin 2B TFA is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC50 values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B TFA antagonizes CRF2-mediated inhibition of gastric emptying [3].
Astressin 2B is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC50 values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B antagonizes CRF2-mediated inhibition of gastric emptying [3].
N-Acetyl-D-glucosamine- 13C8, 15N is 13C and 15N labeled N-Acetyl-D-glucosamine (HY-A0132). N-Acetyl-D-glucosamine is a monosaccharide derivative of glucose.
N-Acetyl-D-glucosamine- 13C2, 15N is the 13C and 15N labeled N-Acetyl-D-glucosamine. N-Acetyl-D-Glucosamine (N-Acetyl-2-amino-2-deoxy-D-glucose) is a monosaccharide derivative of gluc[1][2].
Tenuazonic acid-(acetyl- 13C2) (mixture of diastereomers) in methanol (3-(Acetyl- 13C2)-5-((S)-sec-butyl)-4-hydroxy-1,5-dihydro-2H-pyrrol-2-one) is 13C labeled Tenuazonic acid-(acetyl) (mixture of diastereomers) in methanol .
SKF 100398 (d(CH2)5Tyr(Et)VAVP), an arginine vasopressin (AVP) analogue, is a specific antagonist of the antidiuretic effect of exogenous and endogenous AVP .
S9-CMC1 TFA is a covalent peptide lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 value of 2.53 μM. S9-CMC1 TFA specifically recognizes Cys360 in the enzyme-active region. S9-CMC1 TFA inhibits LSD1 activity, increasing H3K4me1 and H3K4me2 levels, leading to G1 cell cycle arrest and apoptosis and inhibiting cell proliferation. S9-CMC1 TFA significantly inhibits tumor growth in A549 xenograft animal models .
(1S,3aR,6aS)-(2S)-2-Cyclohexyl-N-(2-pyrazinylcarbonyl)glycyl-3-methyl-L-valyl-N-[(1R)-1-[2-(cyclopropylamino)-2-oxoacetyl]butyl]octahydrocyclopenta[c]pyrrole-1-carboxamide-d4 is deuterated labeled (1S,3aR,6aS)-(2S)-2-Cyclohexyl-N-(2-pyrazinylcarbonyl)glycyl-3-methyl-L-valyl-N-[(1R)-1-[2-(cyclopropylamino)-2-oxoacetyl]butyl]octahydrocyclopenta[c]pyrrole-1-carboxamide.
Kahalalide A is an anti-mycobacterial compound with antimicrobial activity. Kahalalide A is derived from the marine mollusk Elysia rufescens. Kahalalide A has attracted extensive attention in natural product research due to its potential medicinal value .
Rusfertide is a peptide mimetic of natural hepcidin, which targets and degrades ferroportin, reduces serum iron and transferrin-saturation, and thus regulates the production of red blood cells. Rusfertide ameliorates the polycythemia vera, β-thalassemia and hereditary hemochromatosis .
Noraramtide (BHV-1100) is an antibody recruitment molecule. Noraramtide can specifically bind to CD38 molecules to recruit natural killer (NK) cells. Noraramtide enhances the ability of NK cells to kill tumor cells through antibody-dependent cellular cytotoxicity (ADCC). This mechanism allows NK cells to more effectively recognize and eliminate tumor cells while avoiding mutual killing between NK cells. Noraramtide can be used for the study of autologous cancer immunity .
Colfosceril miristate-d9 (DMPC-d9) is deuterium labeled Colfosceril miristate. Colfosceril miristate a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
1,2-Dimyristoyl-sn-glycero-3-phosphocholine-d67 is deuterium labeled 1,2-Dimyristoyl-sn-glycero-3-phosphocholine. 1,2-Dimyristoyl-sn-glycero-3-phosphocholine (DMPC) is a synthetic phospholipid used in liposomes. 1,2-Dimyristoyl-sn-glycero-3-phosphocholine
Stewart-Grubbs catalyst is an effective catalyst for the cross-metathesis of olefins with a large number of allylic substituents. In addition, ChemBeads are chemically coated glass beads that improve flowability and chemical homogeneity, making them ideal for automated solid dispensing and high-throughput experiments. Notably, the manufacture of ChemBeads does not require additional chemicals or surfactants, allowing for precise dispensing of sub-milligram amounts of catalyst.
Colfosceril miristate-d63 (DMPC-d63) is deuterium labeled Colfosceril miristate. Colfosceril miristate a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
Colfosceril miristate-d13 (DMPC-d13) is deuterium labeled Colfosceril miristate. Colfosceril miristate a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
Colfosceril miristate-d58 (DMPC-d58) is deuterium labeled Colfosceril miristate. Colfosceril miristate a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
Colfosceril miristate-d4 (DMPC-d4) is deuterium labeled Colfosceril miristate. Colfosceril miristate is a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
(Rac)-1,2-Dimyristoyl-sn-glycero-3-phosphocholine-d72 is deuterium labeled (Rac)-1,2-Dimyristoyl-sn-glycero-3-phosphocholine. 1,2-Dimyristoyl-sn-glycero-3-phosphocholine (DMPC) is a synthetic phospholipid used in liposomes. 1,2-Dimyristoyl-sn-glycero-3-ph
Argifin is a sub-nanomolar chitinase inhibitor produced by soil microorganisms, with IC50s of 0.025 μM, 6.4 μM , 1.1 μM and 4.5 μM for SmChiA (Serratia marcescens chitinaese A), SmChiB, Aspergillus fumigatus chitinase B1 and human chitotriosidase, respectively .
Melanotan I is a potent non-selective melanocortin receptor (MCR) agonist. Melanotan I is a synthetic analogue of α-melanocyte stimulating hormone (α-MSH) that stimulates melanogenesis. Melanotan I can induce skin tanning by mimicking the actions of a-MSH on the melanocortin type 1 receptors (MC1R) of melanocytes. Melanotan I can be used for the research of sun-induced skin cancer, melanoma, inflammation and male erectile dysfunction [3] .
Calcitonin- 13C6, 15N4 (salmon) (Salmon calcitonin- 13C6, 15N4) TFA is 13C and 15N-labeled Calcitonin (salmon) (HY-P0090). Calcitonin (salmon) , a calcium regulating hormone, is a dual-action amylin and calcitonin receptor agonist, could stimulate bone formation and inhibit bone resorption .
Astressin 2B TFA is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC50 values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B TFA antagonizes CRF2-mediated inhibition of gastric emptying [3].
Ac-{Cpg}-Thr-Ala-{Ala(CO)}-Asp-{Cpg}-NH2 (compound 40) is a potent Plasmodium subtilisin-like protease 1 (SUB1) inhibitor. SUB1-IN-1 shows IC50 values of 12 nM and 10 nM against P. vivax and P. falciparumSUB1 (Pv- and PfSUB1), respectively .
MAPI is a polypeptide irreversible 3C cysteine protease (SV3CP) inhibitor. MAPI inhibits SV3CP by covalently binding its C-terminal Michael-acceptor extension to the active site thiol of SV3CP Cys 139. MAPI is promising for research of noroviruses infection .
N-(2-Carbamoyl-ethyl)-Val-Leu-anilide is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .
Astressin 2B is a potent and selective corticotropin-releasing factor receptor 2 (CRF2) antagonist, with the IC50 values of 1.3 nM and > 500 nM for CRF2 and CRF1, respectively. Astressin 2B antagonizes CRF2-mediated inhibition of gastric emptying [3].
SKF 100398 (d(CH2)5Tyr(Et)VAVP), an arginine vasopressin (AVP) analogue, is a specific antagonist of the antidiuretic effect of exogenous and endogenous AVP .
S9-CMC1 TFA is a covalent peptide lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 value of 2.53 μM. S9-CMC1 TFA specifically recognizes Cys360 in the enzyme-active region. S9-CMC1 TFA inhibits LSD1 activity, increasing H3K4me1 and H3K4me2 levels, leading to G1 cell cycle arrest and apoptosis and inhibiting cell proliferation. S9-CMC1 TFA significantly inhibits tumor growth in A549 xenograft animal models .
Kahalalide A is an anti-mycobacterial compound with antimicrobial activity. Kahalalide A is derived from the marine mollusk Elysia rufescens. Kahalalide A has attracted extensive attention in natural product research due to its potential medicinal value .
Rusfertide is a peptide mimetic of natural hepcidin, which targets and degrades ferroportin, reduces serum iron and transferrin-saturation, and thus regulates the production of red blood cells. Rusfertide ameliorates the polycythemia vera, β-thalassemia and hereditary hemochromatosis .
Noraramtide (BHV-1100) is an antibody recruitment molecule. Noraramtide can specifically bind to CD38 molecules to recruit natural killer (NK) cells. Noraramtide enhances the ability of NK cells to kill tumor cells through antibody-dependent cellular cytotoxicity (ADCC). This mechanism allows NK cells to more effectively recognize and eliminate tumor cells while avoiding mutual killing between NK cells. Noraramtide can be used for the study of autologous cancer immunity .
Ganitumab (AMG 479) is a recombinant human monoclonal antibody to the human type 1 insulin-like growth factor receptor (IGF1R). Ganitumab recognizes murine IGF1R with sub-nanomolar affinity (KD=0.22 nM) and inhibits the interaction of murine IGF1R with IGF1 and IGF2. Ganitumab can be used in research of cancer .
Alpha-Naphthoflavone is an orally active flavonoid that is a potent, competitive inhibitor of aromatase< b>aromatase. < b > IC < sub > 50 < / sub > < / b > and < b > K < sub > I < / sub > < / b > value were 0.5 and 0.2 microns. Alpha-Naphthoflavone can inhibit cell proliferation and induce apoptosis[3] .
Geranylgeraniol is an orally acitve vitamin K2sub-type, an intermediate of the mevalonate pathway. Geranylgeraniol targets NF-kB signaling pathway and could alleviate LPS-induced microglial inflammation in animal model [3] .
Argifin is a sub-nanomolar chitinase inhibitor produced by soil microorganisms, with IC50s of 0.025 μM, 6.4 μM , 1.1 μM and 4.5 μM for SmChiA (Serratia marcescens chitinaese A), SmChiB, Aspergillus fumigatus chitinase B1 and human chitotriosidase, respectively .
Geranylgeraniol (Standard) is the analytical standard of Geranylgeraniol. This product is intended for research and analytical applications. Geranylgeraniol is an orally acitve vitamin K2 sub-type, an intermediate of the mevalonate pathway. Geranylgeraniol targets NF-kB signaling pathway and could alleviate LPS-induced microglial inflammation in animal model [3][4].
Amentoflavone (Didemethyl-ginkgetin) is a potent and orally active GABA(A) negative modulator. Amentoflavone also shows anti-inflammatory, antioxidative, anti-viral, anti-tumor, anti-radiation, anti-fungal, antibacterial activity. Amentoflavone induces apoptosis and cell cycle arrest at sub-G1 phase [3] .
Pelargonidin chloride is an anthocyanidin and also is a scavenger of nitric oxide radical and has antioxidant activities. Pelargonidin inhibits cell viability and induces cell cycle arrest at sub-G1 phase. Pelargonidin chloride increases the mRNA and protein expression of HO-1, NQO1, Nrf2. Pelargonidin chloride improves Aβ-induced memory and learning impairment [3].
Neochilenin (3-O-Methylquercetin 4 '-O-glucoside) is a glycoside of 3-O-methylquercetin, which can be isolated from the sub-family Cereoideae (Cactaceae). .
Aculene D, a fungal metabolite, shows quorum sensing (QS) inhibitory activity against Chromobacterium violaceum CV026, and could significantly reduce violacein production in N-hexanoyl-l-homoserine lactone (C6-HSL) induced C. violaceum CV026 cultures at sub-inhibitory concentrations .
Amentoflavone (Standard) is the analytical standard of Amentoflavone. This product is intended for research and analytical applications. Amentoflavone (Didemethyl-ginkgetin) is a potent and orally active GABA(A) negative modulator. Amentoflavone also shows anti-inflammatory, antioxidative, anti-viral, anti-tumor, anti-radiation, anti-fungal, antibacterial activity. Amentoflavone induces apoptosis and cell cycle arrest at sub-G1 phase [3] .
The PC4/SUB1 protein acts as a multifunctional coactivator that cooperates with TAF to promote functional interactions between upstream activators and the general transcription machinery. Its role extends to the potential stability of multiprotein transcription complexes. PC4/SUB1 Protein, Human (His) is the recombinant human-derived PC4/SUB1 protein, expressed by E. coli , with N-His labeled tag. The total length of PC4/SUB1 Protein, Human (His) is 127 a.a., with molecular weight of ~19 kDa.
ABCF3 Protein, Human (HEK293, His, Strep, Flag) is the recombinant human-derived ABCF3, expressed by HEK293 , with Strep, His, Flag labeled tag. The total length of ABCF3 Protein, Human (HEK293, His, Strep, Flag) is 708 a.a.,
ABCB5, N-Trx Protein, Human is a plasma membrane-spanning protein that in humans is encoded by the ABCB5 gene. ABCB5 is an ABC transporter and P-glycoprotein family member principally expressed in physiological skin and human malignant melanoma.
ABCA6 Protein, Human (HEK293, His, Strep, Flag) is the recombinant human-derived ABCA6, expressed by HEK293 , with Strep, His, Flag labeled tag. The total length of ABCA6 Protein, Human (HEK293, His, Strep, Flag) is 1616 a.a.,
ABC 29; ABC29; ABCC 1; ABCC; Abcc1; ATP binding cassette sub family C CFTR/MRP; member 1; ATP binding cassette sub-family C member 1; ATP binding cassette subfamily C member 1; ATP binding cassette transporter variant ABCC1delta ex13; ATP binding cassette transporter variant ABCC1delta ex13&14; ATP binding cassette transporter variant ABCC1delta ex25; ATP binding cassette transporter variant ABCC1delta ex25&26; ATP binding cassette, sub-family C CFTR/MRP; , member 1; ATP-binding cassette sub-family C member 1; DKFZp686N04233; DKFZp781G125; GS X; GSX; Leukotriene C4; transporter; LTC4 transporter; MRP 1; MRP; MRP1; MRP1_HUMAN; Multidrug resistance associated protein 1; Multidrug resistance protein; Multidrug resistance-associated protein 1; Multiple drug resistance associated protein; Multiple drug resistance protein 1
ABCC1, Human (His) is a multitasking ATP-binding cassette (ABC) transporter. ABCC1, Human plays a part in inflammatory and other immunological diseases, age-related macular degeneration, cardiovascular disease, and certain neurological disorders as well as tumor progression.
The bABCC1 protein plays a key role in cellular physiology, mediating the ATP-dependent export of a variety of substrates, including drugs and organic anions. Notably, it confers resistance to anticancer drugs, actively reducing their intracellular accumulation. bABCC1 Protein, Bovine (HEK293, GFP, Strep, His) is the recombinant human-derived bABCC1 protein, expressed by HEK293 , with C-10*His, C-GFP, C-Strep labeled tag. The total length of bABCC1 Protein, Bovine (HEK293, GFP, Strep, His) is 1530 a.a., .
Omeprazole-d3 is deuterium labeled Omeprazole. Omeprazole, a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].
Deutenzalutamide (Enzalutamide-d3) is a developed deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells .
Tricaprilin-d15(Trioctanoin-d15 is the deuterium labeled Tricaprilin (HY-B1804). Tricaprilin is an orally active and well tolerated ketogenic agent that safely induces ketosis. Tricaprilin restores brain electrical activity and metabolism to help counteract neuroinflammation in migraine. Tricaprilin is promising for research of migraine prevention and Alzheimer’s disease (AD). Tricaprilin is a pure C8 medium chain triglyceride (MCT) [3].
Tricaprilin-d50(Trioctanoin-d50 is the deuterium labeled Tricaprilin (HY-B1804). Tricaprilin is an orally active and well tolerated ketogenic agent that safely induces ketosis. Tricaprilin restores brain electrical activity and metabolism to help counteract neuroinflammation in migraine. Tricaprilin is promising for research of migraine prevention and Alzheimer’s disease (AD). Tricaprilin is a pure C8 medium chain triglyceride (MCT) [3].
Pretomanid-d5 is deuterated labeled Pretomanid (HY-10844). Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL.
Zidovudine-d3 is the deuterium labeled Zidovudine. Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection.
Clomipramine-d3 is the deuterium labeled Clomipramine. Clomipramine is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively[1][2].
Acetaminophen-d3 is the deuterium labeled Acetaminophen. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent[1][2][3]. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor[4].
Alpha-Estradiol-d3 is the deuterium labeled Alpha-Estradiol. Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia.
Normetanephrine-d3 (hydrochloride) is the deuterium labeled Normetanephrine hydrochloride. Normetanephrine ((±)-Normetanephrine) hydrochloride is the O-methylated metabolite of norepinephrine (NE)[1].
Methoxsalen-d3 is the deuterium labeled Methoxsalen[1]. Methoxsalen (8-Methoxypsoralen) is a potent tricyclic furocoumarin suicide inhibitor of CYP (cytochrome P-450), is an agent used to treat psoriasis, eczema, vitiligo and some cutaneous Lymphomas in conjunction with exposing the skin to sunlight[2].
Liothyronine-d3 is deuterated labeled Liothyronine (HY-A0070A). Liothyronine is an active form of thyroid hormone. Liothyronine is a potent thyroid hormone receptors TRα and TRβ agonist with Kis of 2.33 nM for hTRα and hTRβ, respectively [3].
Butylphthalide-d3 is the deuterium labeled Butylphthalide. Butylphthalide(3-n-Butylphthalide), an anti-cerebral-ischemia agent, is first isolated from the seeds of celery and showes efficacy in animal models of stroke.
Tamoxifen-d3 hydrochloride is deuterated labeled Tamoxifen (Citrate) (HY-13757). Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells [3].Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen Citrate activates autophagy and induces apoptosis .Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse .
Frovatriptan-d3 (hydrochloride) is the deuterium labeled Frovatriptan[1]. Frovatriptan is a potent 5-HT1B//D receptor agonist and has the highest 5-HT1B potency in the triptan class. Frovatriptan is apparently cerebroselective. Frovatriptan is efficacious and even superior in some endpoints also when taken during the headache phase in migraine attacks with aura[2].
5-Aminosalicylic acid-d3 is the deuterium labeled 5-Aminosalicylic Acid. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB[1][2][3][4].
N,N-Dimethylglycine-d3(Dimethylglycine-d3) hydrochloride is the deuterium labeled N,N-Dimethylglycine hydrochloride (HY-W001158). N,N-Dimethylglycine (Dimethylglycine) is a natural N-methylated glycine, is a nutrient supplement and acts as an NMDAR glycine site partial agonist. N,N-Dimethylglycine is a methyl donor, could improve immunity, function as an antioxidant to prevent oxidative stress, and scavenge excess of free radicals. N,N-Dimethylglycine exhibits antidepressant-like and surfactant effects [3].
Fulvestrant-d3 is the deuterium labeled Fulvestrant. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy[1].
Deracoxib-d3 is the deuterium labeled Deracoxib. Deracoxib, a selective cyclooxygenase-2 inhibitor, is a non-narcotic, non-steroidal anti-inflammatory drug (NSAID).
Guaifenesin-d3 is the deuterium labeled Guaifenesin. Guaifenesin (Guaiacol glyceryl ether), a constituent of guaiac resin from the wood of Guajacum officinale Linné, is an expectorant. Guaifenesin can alleviate cough discomfortby increasing sputum volume and decreasing its viscosity, thereby promoting effective cough[1][2].
Tamoxifen-d3 is the deuterium labeled Tamoxifen . Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells [3] . Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen activates autophagy and induces apoptosis . Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse .
Binimetinib-d3(MEK162-d3) is deuterium labeled Binimetinib. Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM .
Gatifloxacin-d3 (hydrochloride) is the deuterium labeled Gatifloxacin (hydrochloride). Gatifloxacin hydrochloride (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin hydrochloride can be used to treat bacterial conjunctivitis in vivo.
5-Aminosalicylic Acid-d3 (hydrochloride) is the deuterium labeled 5-Aminosalicylic Acid. 5-Aminosalicylic acid (Mesalamine) hydrochloride acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
Thiamphenicol-d3 is a deuterium labeled Thiamphenicol. Thiamphenicol, a methyl-sulfonyl derivative of Chloramphenicol, is a broad-spectrum antimicrobial antibiotic. Thiamphenicol acts by binding to the 50S ribosomal subunit, leading to inhibition of protein synthesis and bacteriostatic effect (against Gram-negative, Gram-positive aerobic and anaerobic bacteria)[1][2].
Physcion-d3(Parietin-d3) is the deuterium labeled Physcion (HY-N0108). Physcion acts as an inhibitor of 6-phosphogluconate dehydrogenase, with an IC50 and a Kd of 38.5 μM and 26.0 μM, respectively. Physcion exhibits laxative, hepatoprotective, anti-inflammatory, anti-microbial, anti-proliferative and anti-tumor effects [3].
Antipyrine-d3 is the deuterium labeled Antipyrine. Antipyrine (Phenazone) is an antipyretic and analgesic. Antipyrine can be used as a probe agent for oxidative agent metabolism. Antipyrine has been widely used in assessment of hepatic oxidative capacity[1][2].
Taxifolin-d3 is deuterium labeled Taxifolin. Taxifolin ((+)-Dihydroquercetin) exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM[1]. Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity[2].
Nomifensine-d3((±)-Nomifensine-d3) maleate is the deuterium labeled Nomifensine maleate (HY-B1110A). Nomifensine ((±)-Nomifensine) is a potent norepinephrine (NE) and dopamine (DA) reuptake inhibitor. Nomifensine inhibits uptake of NE, DA and 5-HT in rat brain synaptosomes, with IC50 values of 6.6 nM, 48 nM and 830 nM, and Ki values of 4.7 nM, 26 nM and 4000 nM, respectively. Nomifensine shows low or ineffective binding activity to dopamine D2, α1-adrenergic, 5-HT2, and muscarinic receptors. Nomifensine has antidepressive effects [3].
Roflumilast-d3 is deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells.
Acetylcysteine-d3 is the deuterium labeled Acetylcysteine. Acetylcysteine (N-Acetylcysteine) is a mucolytic agent which reduces the thickness of the mucus. Acetylcysteine is a ROS inhibitor. Acetylcysteine is a cysteine precursor, prevents hemin-induced ferroptosis by neutralizing toxic lipids generated by arachidonate-dependent activity of 5-lipoxygenases. Acetylcysteine induces cell apoptosis. Acetylcysteine also has anti-influenza virus activities. In addition, Acetylcysteine is the most stable form of cysteine during drug delivery and can be used in disulfidptosis studies [3] .
Esomeprazole-d3 potassium is deuterated labeled Esomeprazole (HY-17021). Esomeprazole ((S)-Omeprazole) is a potent and orally active proton pump inhibitor and reduces acid secretion through inhibition of the H +, K +-ATPase in gastric parietal cells. Esomeprazole has the potential for symptomatic gastroesophageal reflux disease research [3].
L-Tryptophan-d3 is the deuterium labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3[1].
Meldonium-d3 is the deuterated form of Meldonium. Meldonium is a cardiovascular protective agent that competitively inhibits BBOX1 and OCTN2. The IC50 value of Mildronate against human recombinant BBOX is 34-62 μM, and the EC50 value against human OCTN2 is 21 μM. Meldonium is a fatty acid oxidation inhibitor [3].
Pizotyline-d3 is deuterated labeled Pizotifen (HY-B0115). Pizotifen (Pizotyline) is a potent 5-HT2 receptor antagonist, with a high affinity for 5-HT1C binding site.
Cefotaxime-d3 is the deuterium labeled Cefotaxime (HY-A0088A). Cefotaxime is the β-lactamase stable cephalosporin and the third-generation cephalosporin antibiotic. Cefotaxime possesses broad-spectrum antibiotic activity against numerous Gram-positive and Gram-negative bacteria [3] .
Rapamycin-d3 is the deuterium labeled Rapamycin. Rapamycin is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant .
Florfenicol-d3 is the deuterium labeled Florfenicol. Florfenicol, a commonly used veterinary antibiotic, is currently indicated for bovine respiratory disease, and also used in aquaculture for the control of enteric septicemia in catfish. Florfenicol can induce early embryonic death in eggs, with an LC50 of 1.07 μg/g.
Pyrazinamide-d3 is deuterium labeled Pyrazinamide. Pyrazinamide (Pyrazinecarboxamide; Pyrazinoic acid amide) is a potent and orally active antitubercular antibiotic. Pyrazinamide is a proagent that is converted to the active form pyrazinoic acid (POA) by PZase/nicotinamidase encoded by the pncA gene in M. tuberculosis[1][2].
Salbutamol-d3 is the deuterium labeled Salbutamol. Salbutamol is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease (COPD).
Tetrahydrouridine-d3 is the deuterium labeled Tetrahydrouridine[1]. Tetrahydrouridine dihydrate is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine[2][3].
Esomeprazole-d3 is deuterium labeled Esomeprazole. Esomeprazole ((S)-Omeprazole) is a potent and orally active proton pump inhibitor and reduces acid secretion through inhibition of the H+, K+-ATPase in gastric parietal cells. Esomeprazole has the potential for symptomatic gastroesophageal reflux disease research[1][2][3].
Doxorubicinone-d3 is the deuterium labeled Doxorubicinone. Doxorubicinone is a metabolite of an anti-cancer chemotherapy agent Doxorubicin[1]. Doxorubicin is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively.
Rifampicin-d3 is the deuterium labeled Rifampicin. Rifampicin is a potent and broad spectrum antibiotic against bacterial pathogens. Rifampicin has anti-influenza virus activities[1][2].
Stearoylethanolamide-d3(Ceamid-d3) is deuterium labeled Stearoylethanolamide. Stearoylethanolamide is an endocannabinoid-like compound with pro-apoptotic activity .
(-)-Ketoconazole-d3 is deuterium labeled (-)-Ketoconazole. (-)-Ketoconazole ((-)-R 41400) is one of the enantiomer of Ketoconazole. Ketoconazole is a racemic mixture of two enantiomers, levoketoconazole ((2S,4R)-(−)-ketoconazole) and dextroketoconazole ((2R,4S)-(+)-ketoconazole).
Sarcosine-d3 is the deuterium labeled Sarcosine. Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia[1][2].
Thymidine-d3 is the deuterium labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[1][2][3].
Cefotaxime-d3 (sodium) is the deuterium labeled Cefotaxime (sodium salt). Cefotaxime sodium salt, a β-lactamase stable cephalosporin and a third-generation cephalosporin antibiotic, possesses broad-spectrum antibiotic activity against numerous Gram-positive and Gram-negative bacteria[1][2][3][4][5].
Exemestane-d3 is the deuterium labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research[1][2].
DL-Mevalonolactone-d3 is the deuterium labeled DL-Mevalonolactone[1]. DL-Mevalonolactone ((±)-Mevalonolactone;Mevalolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone (Mevalonolactone) decreases mitochondrial membrane potential ( Ψm), NAD(P)H content and the capacity to retain Ca2+ in the brain, besides inducing mitochondrial swelling[2][3].
Artemisinin-d3 is the deuterium labeled Artemisinin. Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants[1]. Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects[2].
Esomeprazole-d3 (sodium) is the deuterium labeled Esomeprazole. Esomeprazole ((S)-Omeprazole) is a potent and orally active proton pump inhibitor and reduces acid secretion through inhibition of the H+, K+-ATPase in gastric parietal cells. Esomeprazole has the potential for symptomatic gastroesophageal reflux disease research[1][2][3].
Fmoc-leucine-d3 is the deuterium labeled Fmoc-leucine. Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-induced glucose-intolerant, and in diabetic db/db mice. Fmoc-leucine has a lower adipogenic activity[1].
D-Alanine-d3 is the deuterium labeled D-Alanine. D-Alanine is a weak GlyR (inhibitory glycine receptor) and PMBA agonist, with an EC50 of 9 mM for GlyR.
Oseltamivir acid-d3 is a deuterium labeled Oseltamivir acid. Oseltamivir acid, the active metabolite of Oseltamivir phosphate, is an orally bioavailable, potent and selective inhibitor of influenza virus neuraminidase (IC50=2 nM) with activity against both influenza A and B viruses[1][2].
N-Acetyl-5-hydroxytryptamine-d3 is the deuterium labeled N-Acetyl-5-hydroxytryptamine. N-Acetyl-5-hydroxytryptamine is a Melatonin precursor, and that it can potently activate TrkB receptor[1][2].
Clomipramine-d3 (hydrochloride) is a deuterium labeled Clomipramine hydrochloride. Clomipramine hydrochloride is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively[1][2].
S-Adenosyl-L-methionine-d3 (S-Adenosyl methionine-d3) is the deuterated product of S-Adenosyl-L-methionine (HY-B0617). S-Adenosyl-L-methionine (S-Adenosyl methionine) is an orally active methyl group donor. S-Adenosyl-L-methionine is a dietary supplement with potent antidepressant effects. S-Adenosyl-L-methionine also has anti‑proliferative, pro‑apoptotic and anti‑metastatic roles in cancers. S-Adenosyl-L-methionine has the potential for, cancer, liver disease and osteoarthritis research [3].
(R)-Pyrrolidine-2-carboxylic acid-d3 is the deuterium labeled (R)-pyrrolidine-2-carboxylic acid. (R)-pyrrolidine-2-carboxylic acid is an endogenous metabolite.
Lamotrigine- 13C3,d3 is the 13C-labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al[1][2].
Rosuvastatin- 13C,d3 sodium is 13C and deuterated labeled Rosuvastatin sodium (HY-17504B). Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels [3].
Skatole-d3 is the deuterium labeled Skatole. Skatole is produced by intestinal bacteria, regulates intestinal epithelial cellular functions through activating aryl hydrocarbon receptors and p38[1].
Meglutol-d3 is the deuterium labeled Meglutol[1]. Meglutol is an antilipemic agent which lowers cholesterol, triglycerides, serum beta-lipoproteins and phospholipids, and inhibits the activity of hydroxymethylglutarryl CoA reductases, which is the rate limiting enzyme in the biosynthesis of cholesterol.
Estradiol-d3 is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.
D-Glucose-d-33 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
Methylacetylacetate-d3 (Acetoacetate methylester-d3) is a deuterium labeled Methyl acetylacetate (HY-Y1298). Methyl acetylacetate is an endogenous metabolite .
Vincristine-d3 (sulfate)is the deuterium labeled Vincristine sulfate. Vincristine sulfate is an antitumor vinca alkaloid which inhibits microtubule formation in mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. It binds to microtubule with a Ki of 85 nM[1][2].
Doxifluridine-d3 is deuterated labeled Doxifluridine (HY-B0021). Doxifluridine has anticancer activity. Doxifluidine is a 5-FU prodrug. Doxifluridine is a thymidinesynthase inhibitor. Doxifluridine can enhance tumor inhibition by synergizing with a variety of drugs [3].
Retinoic acid-d3 is the deuterium labeled Retinoic acid (HY-14649). Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha [3].
Vincristine-d3-ester (sulfate) is the deuterium labeled Vincristine sulfate. Vincristine sulfate is an antitumor vinca alkaloid which inhibits microtubule formation in mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. It binds to microtubule with a Ki of 85 nM[1].
Lurbinectedin-d3 is deuterium labeled Lurbinectedin. Lurbinectedin (PM01183) is a DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively[1].
L-Serine-d3 is the deuterium labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
Ondansetron-d3 is the deuterium labeled Ondansetron[1]. Ondansetron(GR 38032;SN 307) is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy[2].
Mifepristone-d3 is the deuterium labeled Mifepristone. Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay[1].
Levosulpiride-d3 is the deuterium labeled Levosulpiride. Levosulpiride (RV-12309) is the (S)-enantiomer of sulpiride, which is a D2 receptor a antagonist, an atypical antipsychotic agent of the benzamide class[1][2].
Etoricoxib-d3 is the deuterium labeled Etoricoxib[1]. Etoricoxib (MK-0663) is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood[2][3][4].
Mirtazapine-d3 is a deuterium labeled Mirtazapine. Mirtazapine is a 5-HT receptor inhibitor. Mirtazapine is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent by blocking 5-HT2 and 5-HT3 receptors[1].
Dioxybenzone-d3 is deuterium labeled Dioxybenzone. Dioxybenzone (Benzophenone-8; UV-24) is an organic compound used to block UVB and short-wave UVA (ultraviolet) radiation. Dioxybenzone has orally activity. Dioxybenzone exhibits estrogenic disrupting effect. Dioxybenzone up-regulates inflammatory cytokines. Dioxybenzone can be used for cancer, reproductive system disease and inflammatory disease study [3] .
Pantoprazole-d3 is deuterium labeled Pantoprazole. Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI)[1]. Pantoprazole, a substituted benzimidazole, is a potent H+/K+-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142)[3][4].
Oltipraz-d3 is the deuterium labeled Oltipraz. Oltipraz has an inhibitory effect on HIF-1α activation in a time-dependent manner, completely abrogating HIF-1α induction at ≥10 μM concentrations, the IC50 of Oltipraz for HIF-1α inhibition is 10 μM. Oltipraz is a potent Nrf2 activator.
Tilmicosin-d3 is the deuterium labeled Tilmicosin. Tilmicosin (LY-177370) is an orally active calcium channel antagonist and macrolide antibiotic with antimicrobial activity. Tilmicosin mainly acts on the 50S subunit of bacterial ribosomes, inhibiting protein synthesis. Tilmicosin is effective in the treatment of respiratory diseases in livestock such as cattle, sheep and pigs. In addition, Tilmicosin has immunomodulatory and anti-inflammatory effects .
Pocapavir-d3(SCH-48973-d3;V-073-d3) is the deuterium labeled Pocapavir (HY-104074) . Pocapavir (SCH-48973) is an orally active capsid inhibitor. Pocapavir prevents virion uncoating upon entry into the cell. Pocapavir has antiviral activity against polioviruses. Pocapavir also inhibits enterovirus infections .
Fexofenadine-d3 is the deuterium labeled Fexofenadine[1]. Fexofenadine (MDL-16455) is an orally active and nonsedative H1 receptor antagonist. Fexofenadine can be used in allergic rhinitis and chronic idiopathic urticarial research[2][3][4].
Medroxyprogesterone acetate-d3 is deuterium labeled Medroxyprogesterone acetate. Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors[1].
Brequinar-d3(DUP785-d3) is deuterium labeled Brequinar. Brequinar (DUP785) is a potent inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 of 5.2 nM for human DHODH. Brequinar has potent activities against a broad spectrum of viruses. Brequinar also has an anti-SARS2 activity .
Verapamil-d3 (hydrochloride) is the deuterium labeled Verapamil hydrochloride. Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research[1][2][3].
Trabectedin D3 (Ecteinascidin 743 D3) is deuterium labeled Trabectedin. Trabectedin is a tetrahydroisoquinoline alkaloid with potent antitumor activity. Trabectedin binds to the minor groove of DNA, blocks transcription of stress-induced proteins, induces DNA backbone cleavage and cancer cells apoptosis, and increases the generation of ROS in MCF-7 and MDA-MB-453 cells. Trabectedin has tje potential for soft tissue sarcoma and ovarian cancer treatment [3].
Oleanolic acid-d3 is the deuterium labeled Oleanolic Acid[1]. Oleanolic acid (Caryophyllin) is a natural compound from plants with anti-tumor activities[2].
Vitamin D3-d3 is the deuterium labeled Vitamin D3. Vitamin D3 (Cholecalciferol; Colecalciferol) is a naturally occuring form of vitamin D. Vitamin D3 induces cell differentiation and prevents proliferation of cancer cells.
Nortriptyline-d3 (hydrochloride) is the deuterium labeled Nortriptyline hydrochloride. Nortriptyline hydrochloride (Desmethylamitriptyline hydrochloride) is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and used to relieve the symptoms of depression[1].
Methylmalonic acid-d3 is the deuterium labeled Methylmalonic acid. Methylmalonic acid (Methylmalonate) is an indicator of Vitamin B-12 deficiency in cancer[1][2].
Benserazide-d3 (hydrochloride) is the deuterium labeled Benserazide hydrochloride. Benserazide hydrochloride (Serazide) is commonly used in Parkinson's disease and is an inhibitor of peripheral aromatic L-amino acid decarboxylase (AADC)[1].
Lamotrigine-d3 is the deuterium labeled Lamotrigine[1]. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al[2][3].
Diazoxide-d3 is deuterium labeled Diazoxide. Diazoxide (Sch-6783) is an ATP-sensitive potassium channel activator, has the potential for hyperinsulinism treatment.
Methionine-d3 is the deuterium labeled Methionine. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
Undecanoic acid-d3 is the deuterium labeled Undecanoic acid. Undecanoic acid (Undecanoate) is a monocarboxylic acid with antimycotic property, which inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum[1].
Dorzolamide-d3 hydrochloride is deuterated labeled Dorzolamide hydrochloride (HY-B0109A). Dorzolamide (L671152) hydrochloride is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity .
Pyridoxine-d3 (hydrochloride) is the deuterium labeled Pyridoxine hydrochloride. Pyridoxine hydrochloride (Pyridoxol; Vitamin B6) is a pyridine derivative. Pyridoxine (Pyridoxol; Vitamin B6) exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
Orlistat-d3 is a deuterated labeled Orlistat . Orlistat (Tetrahydrolipstatin) is a well-known irreversible inhibitor of pancreatic and gastric lipases. Orlistat is also an inhibitor of fatty acid synthase (FASN), is used orally for long-term research of obesity .?Anti-atherosclerotic?effect [3].
Baricitinib-d3 is the deuterium labeled Baricitinib. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
3-O-Methyldopa-d3(3-Methoxy-L-tyrosine-d3) is deuterium labeled 3-O-Methyldopa (HY-113468A). 3-O-Methyldopa is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of l-DOPA and dopamine .
3,4,5-Trimethoxybenzoic acid-d3 is the deuterium labeled 3,4,5-Trimethoxybenzoic acid[1]. 3,4,5-Trimethoxybenzoic acid (Eudesmic acid;Trimethylgallic Acid) is a benzoic acid derivative. A building block in medicine and organic synthesis.
Daunorubicin- 13C,d3 is 13C and deuterium labeled Daunorubicin. Daunorubicin (Daunomycin) is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin inhibits DNA and RNA synthesis. Daunorubicin is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin is also an anthracycline antibiotic. Daunorubicin can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor .
Frovatriptan-d3 (succinate) is deuterium labeled Frovatriptan (succinate). Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research[1][2].
5-Aminosalicylic acid-d3 disodium is deuterated labeled 5-Aminosalicylic Acid (HY-15027). 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).
Hexacosanoic acid methylester-d3 (C26:0 methylester-d3) is deuterium labeled Methyl hexacosanoate. Methyl hexacosanoate is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Dabigatran-d3 is the deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
Malic acid-d3 is the deuterium labeled Malic acid. Malic acid (Hydroxybutanedioic acid) is a dicarboxylic acid that is naturally found in fruits such as apples and pears. It plays a role in many sour or tart foods[1][2].
Infigratinib-d3 is a deuterated analog of infigratinib. Infigratinib is an effective inhibitor of the FGFR family, with IC50 values of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively .
Vinorelbine-d3 (ditartrate) is the deuterium labeled Vinorelbine ditartrate. Vinorelbine (ditartrate) is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC50 of 1.25 nM.
Rivastigmine-d3 hydrochloride is deuterated labeled Rivastigmine (HY-17368). Rivastigmine (ENA 713 free base) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease .
Thiamine-d3 (hydrochloride) is the deuterium labeled Thiamine hydrochloride. Thiamine hydrochloride (Thiamine chloride hydrochloride) is an essential micronutrient needed as a cofactor for many central metabolic enzymes.
Theophylline-d3 is deuterated labeled Theophylline (HY-B0809). Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research [3] .
4-Hydroxyantipyrine-d3 is the deuterium labeled 4-Hydroxyantipyrine. 4-Hydroxyantipyrine is the major metabolite of Antipyrine, can be as a biodistribution promoter. 4-Hydroxyantipyrine can increase distribution of concentration ratio of Antipyrine in the brain[1][2][3].
Cabotegravir-d3 (sodium) is the deuterium labeled Cabotegravir sodium. Cabotegravir sodium is a highly potent HIV integrase inhibitor with an IC50 value of 2.5 nM for HIVADA. Cabotegravir sodium is primarily metabolized by uridine diphosphate glucuronosyltr
Methyldopa-d3 (hydrochloride) is deuterium labeled Methyldopa (hydrochloride). Methyldopa hydrochloride (L-(-)-α-Methyldopa hydrochloride) hydrochloride, a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa hydrochloride is a proagent and is metabolized (α-Methylepinephrine) in the central nervous system[1][2].
Omeprazole metabolite Omeprazole sulfone-d3 is the deuterium labeled Omeprazole metabolite Omeprazole sulfone. Omeprazole sulfone is a metabolite of Omeprazole, which is a proton pump inhibitor.
Etoposide-d3 (VP-16-d3) is the deuterium labeled Etoposide (HY-13629). Etoposide (VP-16) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy .
Licarbazepine-d3 is the deuterium labeled Licarbazepine (HY-108506). Licarbazepine is a voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects[1][2].
Vildagliptin-d3 is the deuterium labeled Vildagliptin. Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity[1][2].
Ulipristal-d3(CDB-3236-d3) is deuterium labeled Ulipristal. Ulipristal (CDB 3236) is a selective progesterone receptor modulator (SPRM). Ulipristal binds to the progesteron receptor, thereby inhibiting PR-mediated gene expression, and interfering with progesterone activity in the reproductive system .
Imatinib-d3 (hydrochloride) is the deuterium labeled Imatinib. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
Riboflavin-d3 is the deuterium labeled Riboflavin. Riboflavin is an easily absorbed micronutrient with a key role in maintaining health in humans and other animals.
N-Desmethyl Clomipramine-d3 (hydrochloride) is the deuterium labeled N-Desmethyl Clomipramine. N-Desmethyl Clomipramine hydrochloride (Desmethylclomipramine hydrochloride) is a primary plasma N-desmethyl metabolite of Clomipramine[1]
Thiamphenicol-d3-1(Thiophenicol-d3-1;Dextrosulphenidol-d3-1) is the deuterium-labeled Thiamphenicol (HY-B0479) . Thiamphenicol (Thiophenicol)，a methyl-sulfonyl derivative of Chloramphenicol，is a broad-spectrum antimicrobial antibiotic. Thiamphenicol acts by binding to the 50S ribosomal subunit，leading to inhibition of protein synthesis and bacteriostatic effect (against Gram-negative，Gram-positive aerobic and anaerobic bacteria) [3].
(S)-Malic acid-d3 is the deuterium labeled (S)-Malic acid. (S)-Malic acid ((S)-2-Hydroxysuccinic acid) is a dicarboxylic acid in naturally occurring form, contributes to the pleasantly sour taste of fruits and is used as a food additive[1][2].
Duloxetine-d3 (hydrochloride) is a deuterium labeled Duloxetine hydrochloride. Duloxetine hydrochloride is a serotonin-norepinephrine reuptake inhibitor (SNRI) with a Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD)[1][2].
N6-Methyladenosine-d3(6-Methyladenosine-d3;N-Methyladenosine-d3) is a deuterium labeled N6-Methyladenosine (HY-N0086). N6-Methyladenosine is the most prevalent internal (non-cap) modification present in the messenger RNA (mRNA) of all higher eukaryotes. N6-Methyladenosine can modifies viral RNAs and has antiviral activities.
Dexamethasone-d3-1(Hexadecadrol-d3-1; Prednisolone F-d3-1) is a deuterium labeled Dexamethasone (HY-14648). Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
Levocarnitine propionate-d3 (hydrochloride) is the deuterium labeled Levocarnitine propionate hydrochloride. Levocarnitine propionate hydrochloride (L-Propionylcarnitine chloride; ST-261) is used to treat the deterioration of renal function, congestive heart failure, intermittent claudication, and other diseases.
N-Methylpyrrolidone-d3 is the deuterium labeled N-Methylpyrrolidone [1]. N-Methylpyrrolidone (1-Methyl-2-pyrrolidinone), a five-membered cyclic amide, is an organic polar solvent. N-Methylpyrrolidone is extensively used in the manufacture of adhesives, paints, fuels, and pharmaceuticals[2][3].
Phenylephrine-d3 (hydrochloride) is the deuterium labeled Phenylephrine hydrochloride. (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
Tofacitinib-d3 (citrate) is deuterium labeled Tofacitinib (citrate). Tofacitinib citrate is an orally available JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.
13-cis Acitretin-d3 is a deuterium labeled 13-cis Acitretin. 13-cis Acitretin is the metabolite of Acitretin after chronic administration. Acitretin(Ro 10-1670) is a second-generation, systemic retinoid that has been used in the treatment of psoriasis[1][2].
L-5-Hydroxytryptophan-d3 is the deuterium labeled L-5-Hydroxytryptophan. L-5-Hydroxytryptophan (L-5-HTP), a naturally occurring amino acid and a dietary supplement for use as an antidepressant, appetite suppressant, and sleep aid, is the immediate precursor of the neurotransmitter serotonin and a reserpine antagonist[1]. L-5-Hydroxytryptophan (L-5-HTP) is used to treat fibromyalgia, myoclonus, migraine, and cerebellar ataxia[2][3][4][5].
Citalopram-d3((±)-Citalopram-d3) hydrobromide is deuterium labeled Citalopram (hydrobromide). Citalopram hydrobromide is a selective serotonin reuptake inhibitor (SSRI). Citalopram hydrobromide inhibits 5-HT uptake into synaptosomes with an IC50 of 1.8 nM. Citalopram hydrobromideinhibits the 5-HT uptake in rabbit blood platelets with an IC50 of 14 nM. Antidepressant effect .
Hydroxytyrosol-d5 is the deuterium labeled Hydroxytyrosol. Hydroxytyrosol (DOPET) is a phenolic compound drawn from the olive tree and its leaves with anti-oxidant, anti-atherogenic, anti-thrombotic, antimicrobial, anti-inflammatory and anti-tumour effects[1][2].
Hydroxytyrosol-d4 is the deuterium labeled Hydroxytyrosol. Hydroxytyrosol (DOPET) is a phenolic compound drawn from the olive tree and its leaves with anti-oxidant, anti-atherogenic, anti-thrombotic, antimicrobial, anti-inflammatory and anti-tumour effects[1][2].
Retinoic acid-d3-1 is the deuterium labeled Retinoic acid (HY-14649). Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha [3].
Perindopril-d3 (erbumine) is deuterated labeled Perindopril (erbumine) (HY-B0130A). Perindopril erbumine is an angiotensin-converting enzyme inhibitor. Perindopril erbumine modulates NF-κB and STAT3 signaling and inhibits glial activation and neuroinflammation. Perindopril erbumine can be used for the research of Chronic Kidney Disease and high blood pressure [3] .
(R)-Mirtazapine-d3 is a deuterium labeled (R)-Mirtazapine. (R)-Mirtazapine is a R(−)-enantiomer of Mirtazapine with antinociceptive properties in an animal model of acute thermal nociception. (R)-Mirtazapine is a 5-HT3 receptor antagonist. (R)-Mirtazapine is mainly metabolized by CYP3A4[1].
(S)-Mirtazapine-d3 is a deuterium labeled (S)-Mirtazapine. (S)-Mirtazapine is a S(+)-enantiomer of Mirtazapine with pronociceptive properties in an animal model of acute thermal nociception.(S)-Mirtazapine is a stereoselective 5-HT2 receptor antagonist. (S)-Mirtazapine is metabolized by CYP2D6 and CYP1A2[1].
Fexofenadine-d3-1 fumarate is deuterated labeled Fexofenadine (HY-B0801). Fexofenadine (MDL-16455) is an orally active and nonsedative H1 receptor antagonist. Fexofenadine can be used in allergic rhinitis and chronic idiopathic urticarial research [3].
5'-Methylthioadenosine-d3 is the deuterium labeled 5'-Methylthioadenosine[1]. 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis. 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis[2][3][4].
3-Indoleacetic acid-d7 is the deuterium labeled 3-Indoleacetic acid (HY-18569). 3-Indoleacetic acid (Indole-3-acetic acid) is the most common natural plant growth hormone of the auxin class. It can be added to cell culture medium to induce plant cell elongation and division .
Medroxyprogesterone-d3 is the deuterium labeled Medroxyprogesterone. Medroxyprogesterone is a progestin, a synthetic variant of the human hormone progesterone and a potent progesterone receptor agonist.
N1-Methylpseudouridine-d3 is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc .
3-Indoleacetic acid-d4 (Indole-3-acetic acid-d4; 3-IAA-d4) is the deuterium labeled 3-Indoleacetic acid (HY-18569) . 3-Indoleacetic acid (Indole-3-acetic acid) is the most common natural plant growth hormone of the auxin class. It can be added to cell culture medium to induce plant cell elongation and division .
3-Indoleacetic acid-d5 is the deuterium labeled 3-Indoleacetic acid (HY-18569). 3-Indoleacetic acid-d5 can be used as internal standard for assay of IAA releases by alkaline hydrolysis of ester and amide conjugates .
Retinyl acetate-d3 (ALK-001) is a deuterated Vitamin A. Retinyl acetate-d3 can be used for research of geographic atrophy (GA) secondary to age-related macular degeneration (AMD) .
(S)-Indoximod-d3 is the deuterium labeled (S)-Indoximod. (S)-Indoximod (1-Methyl-L-tryptophan) is an inhibitor of indoleamine 2,3-dioxygenase (IDO). (S)-Indoximod can be used for the research of cancer[1][2][3].
L-Serine- 13C3, 15N,d3 is the deuterium, 13C-, and 15-labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
3-Methoxybenzeneboronic acid-d3 is the deuterium labeled 3-Methoxybenzeneboronic acid (HY-W000854). 3-Methoxybenzeneboronic acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
2'-Deoxycytidine- 15N3 is the 15N labeled 2'-Deoxycytidine[1]. 2'-Deoxycytidine, a deoxyribonucleoside, could inhibit biological effects of Bromodeoxyuridine (Brdu)[2].
Physostigmine-d3 is the deuterium labeled Physostigmine. Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning[1][2][3][4].
Ibuprofen-d3((±)-Ibuprofen-d3) sodium is the deuterium labeled Ibuprofen sodium (HY-78131C). Ibuprofen sodium is an orally active, selective COX-1 inhibitor with an IC50 value of 13 μM. Ibuprofen sodium inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen sodium is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen sodium can be used in the research of pain, swelling, inflammation, infection, immunology, cancers [3] .
Betulin-d3(Trochol-d3) is deuterium labeled Betulin. Betulin (Trochol), is a sterol regulatory element-binding protein (SREBP) inhibitor with an IC50 of 14.5 μM in K562 cell line .
Sulfadoxine-d3 is a deuterium labeled Sulfadoxine (HY-B0439). Sulfadoxine is a sulfonamide that is used, usually in combination with Pyrimethamine (HY-18062), for multidrug-resistant Plasmodium falciparum and P. vivax inhibition. Unlike PYR, Sulfadoxine has no impact on HIV replication or MT-2 cell cycle progression. But also Sulfadoxine exhibits suppression on respiratory, and urinary tract infections[1][2][3][4].
Nefopam-d3 (hydrochloride) is the deuterium labeled Nefopam hydrochloride. Nefopam hydrochloride (Fenazoxine hydrochloride) is a centrally-acting but non-opioid analgesic drug, for the relief of moderate to severe pain. Nefopam hydrochloride targets β-catenin protein level in mesenchymal cells in-vitro and in-vivo[1][2].
Levofloxacin-d3((-)-Ofloxacin-d3) hydrochlorideis deuterium labeled Levofloxacin (hydrochloride). Levofloxacin ((-)-Ofloxacin) hydrochloride is an orally active antibiotic and is active against both Gram-positive and Gram-negative bacteria. Levofloxacin hydrochloride inhibits the DNA gyrase and topoisomerase IV. Levofloxacin hydrochloride can be used for chronic periodontitis, airway inflammation and BK Viremia research. Levofloxacin hydrochloride shows anti-orthopoxvirus activity [3] .
Pyridoxine-d3 is a deuterium labeled Pyridoxine. Pyridoxine (Pyridoxol) is a pyridine derivative. Pyridoxine exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway .
Hydrocortisone-d3 is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex[1].
Eplerenone-d3 is the deuterium labeled Eplerenone. Eplerenone (Epoxymexrenone) is a selective, competitive and oreally active aldosterone antagonist with an IC50 of 138 nM. Eplerenone has low affinity for progesterone, androgen, estrogen and glucocorticoid receptors. Eplerenone can be used for hypertension and heart failure after myocardial infarction reserch[1][2].
Trigonelline-d3 (chloride) is the deuterium labeled Trigonelline chloride. Trigonelline chloride, an alkaloid with potential antidiabetic activity, is present in considerable amounts in coffee. Trigonelline chloride has anti-HSV-1 , antibacterial, and antifungal activities.
Glyburide-d3 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity[1]. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability[4]. Glibenclamide can induce autophagy[5].
Pefloxacin-d3 is the deuterium labeled Pefloxacin. Pefloxacin is a an antibacterial agent and prevents bacterial DNA replication by inhibiting DNA gyrase (topoisomerse).
Metamizole-d3 sodium is the deuterium labeled Metamizole sodium. Metamizole sodium is a non-opioid compound with excellent analgesic and antipyretic effects. Metamizole sodium is a cyclooxygenase-3(COX-3) inhibitor .
Mianserin-d3 is the deuterium labeled Mianserin (HY-B0188). Mianserin? is a Histamine 1 receptor inverse agonist and is a psychoactive agent of the tetracyclic antidepressant .
Nefopam-d3 is a deuterium labeled Nefopam (Fenazoxine). Nefopam is a centrally-acting but non-opioid analgesic drug, and Nefopam targets β-catenin protein level in mesenchymal cells[1][2].
Imidaprilat-d3(6366A-d3) is deuterium labeled Imidaprilate. Imidaprilate is an active metabolite of TA-6366, acts as a potent angiotensin converting enzyme (ACE) inhibitor, with an IC50 of 2.6 nM, and is used in the research of hypertensive disease .
DTAC-d3(Dodecyltrimethylammonium-d3 chloride) is the deuterium labeled DTAC (HY-W096983). DTAC is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
11-Ketodihydrotestosterone-d3 is the deuterium labeled 11-Ketodihydrotestosterone. 11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells[1][2].
Sapropterin-d3((6R)-BH4-d3) is deuterium labeled Sapropterin. Sapropterin ((6R)-BH4) is an orally active phenylalanine hydroxylase (PAH) cofactor, which is effective in reducing blood phenylalanine concentrations. Sapropterin can be used in study of phenylketonuria (PKU) .
L-5-Hydroxytryptophan-d3-1 is the deuterium labeled L-5-Hydroxytryptophan[1]. L-5-Hydroxytryptophan (L-5-HTP), a naturally occurring amino acid and a dietary supplement for use as an antidepressant, appetite suppressant, and sleep aid, is the immediate precursor of the neurotransmitter serotonin and a reserpine antagonist[2]. L-5-Hydroxytryptophan (L-5-HTP) is used to treat fibromyalgia, myoclonus, migraine, and cerebellar ataxia[3][4][5][6].
Clopidogrel-d3 (hydrogen sulfate) is the deuterium labeled Clopidogrel hydrogen sulfate[1]. Clopidogrel hydrogen sulfate is an antiplatelet agent to prevent blood clots. Clopidogrel hydrogen sulfate inhibits CYP2B6 and CYP2C19 with IC50s of 18.2 nM and 524 nM, respectively. Clopidogrel hydrogen sulfate is a potent antithrombotic agent that inhibits ADP-induced platelet aggregation．Clopidogrel hydrogen sulfate also is an orally active P2Y(12) inhibitor[2][3][4][5][6].
Zidovudine- 13C,d3 is the 13C- and deuterium labeled Zidovudine. Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection.
3-Epiglycyrrhetinic acid-d3 (3α-Glycyrrhetic acid-d3) is the deuterium-labeled 3-Epiglycyrrhetinic acid. 3-Epiglycyrrhetinic acid is a derivative of glycyrrhetic acid. Glycyrrhetic acid and its derivative are considered to have anti-inflammatory, anti-ulcer, and antiviral activities .
Hydrocinnamic acid-d5 is the deuterium labeled Hydrocinnamic acid[1]. Hydrocinnamic acid is the major rhizospheric compound with known growth regulatory activities[2].
Hydrocinnamic acid-d9 is the deuterium labeled Hydrocinnamic acid[1]. Hydrocinnamic acid is the major rhizospheric compound with known growth regulatory activitie[2]s.
Tricaprilin- 13C3 (Trioctanoin- 13C3) is a 13C-labeled Tricaprilin (HY-B1804) . Tricaprilin is an orally active and well tolerated ketogenic agent that safely induces ketosis. Tricaprilin restores brain electrical activity and metabolism to help counteract neuroinflammation in migraine. Tricaprilin is promising for research of migraine prevention and Alzheimer’s disease (AD). Tricaprilin is a pure C8 medium chain triglyceride (MCT) [3].
Estrone- 13C3 is the 13C-labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells[1][2].
Ritonavir- 13C3 is 13C labeled Ritonavir. Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.61 μM .
Omeprazole metabolite Omeprazole sulfone (methoxy-d3) is the deuterium labeled Omeprazole metabolite Omeprazole sulfone. Omeprazole sulfone is a metabolite of Omeprazole, which is a proton pump inhibitor.
Pyrroloquinoline quinone-13C3 (sodium) is an isotope of Pyrroloquinoline quinone. Pyrroloquinoline quinone (PQQ), a redox co-factor, is an anionic, redox-cycling orthoquinone. Pyrroloquinoline quinone is isolated from cultures of methylotropic bacteria and tissues of mammals. Pyrroloquinoline quinone is an essential nutrient for mammals and is important for immune function .
Cyromazine- 13C3 is the 13C3 labeled Cyromazine. Cyromazine is a triazine insect growth regulator used as an insecticide and an acaricide. It is a cyclopropyl derivative of melamine. Cyromazine works by affecting the nervous system of the immature larval stages of certain insects.
D-Glucose- 13C3-2 is the 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
Clomipramine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled Clomipramine (hydrochloride). Clomipramine (Chlorimipramine) hydrochloride is a potent 5-HT reuptake blocker with the IC50 value of 1.5 nM. Clomipramine hydrochloride is a tricyclic antidepressant that can be used for the research of depression and obsessive compulsive disorder (OCD)[1].
D-Glucose- 13C3-1 is the 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
Tedizolid- 13C,d3 is the 13C- and deuterium labeled Tedizolid. Tedizolid (TR 700; Torezolid; DA-7157) is a novel oxazolidinone, acting through inhibition of bacterial protein synthesis by binding to 23S ribosomal RNA (rRNA) of the 50S subunit of the ribosome.
Omeprazole sulfide-d3 is the deuterium labeled Omeprazole sulfide. Omeprazole metabolite Omeprazole sulfide (Ufiprazole) is a metabolite of Omeprazole, which is a proton pump inhibitor.
Methotrexate metabolite-d3 is the deuterium labeled Methotrexate metabolite. Methotrexate metabolite (DAMPA), the active metabolite of Methotrexate. Methotrexate is a folic acid antagonist that is widely used as an immunosuppressant and chemotherapeutic agent[1].
Trilostane-d3 is the deuterium-labeled Trilostane (HY-14281). Trilostane-d3 (Win 24540) is a competitive and orally active 3-β-hydroxysteroiddehydrogenase (3β-HSD) inhibitor. Trilostane-d3 is a synthetic nonhormonal steroid. Trilostane-d3 can be used for the research of breast cancer and prostate cancer .
Dinotefuran-d3 is the deuterium labeled Dinotefuran[1]. Dinotefuran is an insecticide of the neonicotinoid class, its mechanism of action involves disruption of the insect's nervous system by inhibiting nicotinic acetylcholine receptors[2].
Mexiletine-d3 (hydrochloride) is deuterium labeled Mexiletine (hydrochloride). Mexiletine hydrochloride (KOE-1173 hydrochloride), a Class IB antianhythmic, is a non-selective voltage-gated sodium channel blocker[1][2].
Flunixin-d3 is the deuterium labeled Flunixin. Flunixin Meglumine is a potent inhibitor of COX used as analgesic agent with anti-inflammatory and antipyretic activity[1][2].
Flumatinib-d3 is deuterium labeled Flumatinib. Flumatinib (HHGV678) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib inhibits c-Abl, PDGFRβ and c-Kit with IC50s of 1.2 nM, 307.6 nM and 665.5 nM, respectively[1].
Parbendazole-d3 is the deuterium labeled Parbendazole. Parbendazole is a potent inhibitor of microtubule assembly, destabilizes tubulin, with an EC50 of 530 nM, and exhibits a broad-spectrum anthelmintic activity.
Acalabrutinib-d3(ACP-196-d3) is the deuterated form of Acalabrutinib (HY-17600). Acalabrutinib (ACP-196) is an orally active, irreversible, highly selective second-generation BTK inhibitor. Acalabrutinib covalently binds to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib shows strong targeting and efficacy in mouse models of chronic lymphocytic leukemia (CLL).
Ritodrine-d3 (hydrochloride) is the deuterium labeled Ritodrine (hydrochloride). Ritodrine hydrochloride (DU21220 hydrochloride) is a β-2 adrenergic receptor agonist.
Elimusertib-d3 (BAY 1895344-d3) is the deuterium labeled Elimusertib (BAY 1895344). Elimusertib is a potent, orally active and selective ATR inhibitor and has anti-tumor activity .
Ozenoxacin-d3 is the deuterium-labeled Ozenoxacin (HY-14957). Ozenoxacin-d3 is a nonfluorinated quinolone antibacterial, which shows potent activities against the main microorganisms isolated from skin and soft tissue infections.
Cinacalcet-d3 is the deuterium labeled Cinacalcet. Cinacalcet (AMG 073) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.
Sulindac-d3 is deuterium labeled Sulindac. Sulindac (MK-231) is a non-steroidal antiinflammatory agent, acts as a COX-2 inhibitor, and inhibits overexpression of COX-2.
Nordoxepin-d3 (hydrochloride) is the deuterium labeled Nordoxepin hydrochloride. Nordoxepin hydrochloride is an active metabolite of Doxepin hydrochloride (HY-B0725), which is an orally active tricyclic antidepressant[1].
Pazopanib-d3(GW786034-d3) is deuterium labeled Pazopanib. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively .
Fluorofenidone-d3 is deuterium labeled Fluorofenidone. Fluorofenidone (AKF-PD), an analogue of AMR69, shows equivalent antifibrotic activity, lower toxicity and longer half-life. Fluorofenidone (AKF-PD) attenuates the progression of renal interstitial fibrosis partly by suppressing NADPH oxidase and extracellular matrix (ECM) deposition via the PI3K/Akt signalling pathway[1][2].
Methoxyamine-d3 (O-Methylhydroxylamine-d3) hydrochloride is the deuterium labeled Methoxyamine hydrochloride. Methoxyamine hydrochloride is an orally active and potent base excision repair (BER) inhibitor .
Amitraz-d3 is the deuterium labeled Amitraz. Amitraz is a non-systemic acaricide and insecticide, with alpha-adrenergic agonist activity, interaction with octopamine receptors of the central nervous system and inhibition of monoamine oxidases and prostaglandin synthesis.
Albendazole-d3 is the deuterium labeled Albendazole, which is a member of the benzimidazole compounds used as a agent indicated for the treatment of a variety of worm infestations[1].
Capsaicin-d3 is the deuterium labeled Capsaicin. Capsaicin ((E)-Capsaicin), an active component of chili peppers, is a TRPV1 agonist. Capsaicin has pain relief, antioxidant, anti-inflammatory, neuroprotection and anti-cancer effects[1][2].
Apalutamide-d3 is the deuterium labeled Apalutamide[1]. Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM[2].
Celecoxib-d3 is the deuterium labeled Celecoxib. Celecoxib,a selective non-steroidal anti-inflammatory drug (NSAID), is a selective COX-2 inhibitor with an IC50 of 40 nM[1][2].
Tadalafil-d3 is the deuterium labeled Nortadalafil. Nortadalafil is demethyl Tadalafil, which is a PDE5 inhibitor, currently marketed in pill form for treating erectile dysfunction (ED) under the name Cialis; and under the name Adcirca for the treatment of pulmonary arterial hypertension.
Glycyrrhizic acid-d3(Glycyrrhizin-d3) is deuterium labeled Glycyrrhizic acid. Glycyrrhizic acid is a triterpenoid saponinl, acting as a direct HMGB1 antagonist, with anti-tumor, anti-diabetic activities .
Parecoxib-d3 is the deuterium labeled Parecoxib. Parecoxib (SC 69124) is a highly selective and orally active COX-2 inhibitor, the proagent of Valdecoxib (HY-15762). Parecoxib Sodium is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits prostaglandin (PG) synthesis. Parecoxib can be used for the relief of acute postoperative pain and symptoms of chronic inflammatory conditions such as osteoarthritis and rheumatoid arthritis in vivo.
Eprinomectin-d3(MK-397-d3) is the deuterium-labeled Eprinomectin (HY-12643). Eprinomectin is a type of avermectin. Eprinomectin，as a broad-spectrum fungicide，has insecticidal，insecticidal and acaricidal activities. Eprinomectin induces apoptosis and autophagy in prostate cancer cells and has antitumor activity .
Flurbiprofen-d3 is the deuterium labeled Flurbiprofen. Flurbiprofen (dl-Flurbiprofen) is a potent, orally active nonsteroidal anti-inflammatory agent (NSAIA/NSAID), with antipyretic and analgesic activities. Flurbiprofen is commonly used for the research of inflammatory diseases, including osteoarthritis and rheumatoid arthritis. Flurbiprofen is a non-selective cyclooxygenase (COX) inhibitor that can be used for the research of colorectal cancer[1][2][3].
Puromycin-d3 (dihydrochloride) is the deuterium labeled Puromycin dihydrochloride. Puromycin dihydrochloride (CL13900 dihydrochloride), an aminonucleoside antibiotic, inhibits protein synthesis[1].
Aspartame-d3 is the deuterium labeled Aspartame. Aspartame (SC-18862) is a methyl ester of a dipeptide. Aspartame can be used as a synthetic nonnutritive sweetener. Aspartame is composed of phenylalanine (50%), aspartic acid (40%) and methanol (10%)[1][2].
Cimetidine-d3 is the deuterium labeled Cimetidine. Cimetidine (SKF-92334) is an orally active and inverse histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine is an inverse agonist. Cimetidine has anti-cancer and anti-inflammatory activity[1][2][5].
Spironolactone-d3 is the deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC50 of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes[1][2][3].
Captopril-d3 is deuterium labeled Captopril. Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor with an IC50 of 7.9 μM[1][2][3].
Valsartan-d3 is the deuterium labeled Valsartan[1]. Valsartan (CGP 48933) is an angiotensin II receptor antagonist and has the potential for high blood pressure and heart failure research[2].
Guaiacol-d3 is the deuterium labeled Guaiacol. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Guaiacol has an anti-inflammatory activity[1].
Nintedanib-d3 is the deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
Bergapten-d3 is deuterium labeled Bergapten. Bergapten is a natural anti-inflammatory and anti-tumor agent. Bergapten is inhibitory towards mouse and human CYP isoforms.
Olanzapine-d3 is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic[1][2].
Oseltamivir-d3 (phosphate)eis the deuterium labeled Oseltamivir phosphate. Oseltamivir phosphate (GS 4104) is a neuraminidase inhibitor recommended for the treatment and prophylaxis of influenza A and B.
Nemonoxacin-d3 is the deuterium labeled Nemonoxacin. Nemonoxacin (TG-873870) is an orally active and potent broad-spectrum antibiotic. Nemonoxacin shows good inhibitory activity against different species of staphylococci, streptococci, and enterococci, Neisseria gonorrhoeae, and Haemophilus influenza. Nemonoxacin can be used in the study of bacterial infections and community-acquired pneumonia[1][2][3].
Ampyrone-d3 is the deuterium labeled Ampyrone. Ampyrone is a metabolite of Metamizole sodium (HY-B1279A). Ampyrone is a PGE2-dependent blocker and inhibitor of COX .
Piroxicam-d3 is deuterium labeled Piroxicam. Piroxicam is a non-steroidal anti-inflammatory drugs, acts as a COX inhibitor, with IC50s of 47, 25 μM for human monocyte COX-1 and COX-2, respectively [1].
L-Hyoscyamine-d3 is the deuterium labeled L-Hyoscyamine. L-Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine is a levo-isomer to Atropine (HY-B1205)[1][2].
Prasugrel-d3 is the deuterium labeled Prasugrel. Prasugrel (PCR 4099), a thienopyridine and proagent, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation[1].
Saracatinib-d3 (AZD0530-d3) (ZG5129) is the deuterium-labeled analog of Saracatinib (HY-10234). Saracatinib-d3 is an inhibitor of the Src kinase, which can inhibit severe sepsis caused by bacterial or various microbial infections .
Sarpogrelate-d3 (hydrochloride) is the deuterium labeled Sarpogrelate hydrochloride. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis[1][2][3].
Agomelatine-d3 is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively[1]. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively[2].
Naproxen-d3 is the deuterium labeled Naproxen. Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Ergothioneine-d3 is the deuterium labeled Ergothioneine. Ergothioneine, an imidazole-2-thione derivative of histidine betaine, is synthesized by certain bacteria and fungi. Ergothioneine is generally considered an antioxidant[1].
Diflunisal-d3 is the deuterium labeled Diflunisal. Diflunisal (MK-647) is a salicylate derivative with nonsteroidal anti-inflammatory and uricosuric properties, which is used alone as an analgesic and in rheumatoid arthritis patients. The mechanism of action of diflunisal is as a Cyclooxygenase (COX) Inhibitor.
Methylprednisolone-d3 is the deuterium labeled Methylprednisolone. Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels[3].
Linezolid-d3 is a deuterium labeled Linezolid (PNU-100766). Linezolid is a synthetic antibiotic that acts by inhibiting the initiation of bacterial protein synthesis[1].
Valdecoxib-d3 is the deuterium labeled Valdecoxib. Valdecoxib is a highly potent and selective inhibitor of COX-2, with IC50s of 5 nM and 140 μM for COX-2 and COX-1, respeceively. Valdecoxib can be used in the research of arthritis and pain[1][2].
(±)-Duloxetine-d3 (hydrochloride) is deuterium labeled (±)-Duloxetine (hydrochloride). (±)-Duloxetine ((Rac)-Duloxetine) hydrochloride is the racemate of Duloxetine hydrochloride. Duloxetine hydrochloride, a serotonin-norepinephrine reuptake inhibitor, can be used for diabetic neuropathic pain and fibromyalgia as well as major depressive disorder research[1].
Tasquinimod-d3 (ABR-215050-d3) is the deuterium labeled Tasquinimod (HY-10528). Tasquinimod is an oral antiangiogenic agent, which plays an important role in castration-resistant prostate cancer. Tasquinimod binds to the regulatory Zn 2+ binding domain of HDAC4 with Kd of 10-30 nM. Tasquinimod also is a S100A9 inhibitor [3].
Ozenoxacin-d3 (hydrochloride) is the deuterium labeled Ozenoxacin hydrochloride. Ozenoxacin hydrochloride is a nonfluorinated quinolone antibacterial, which shows potent activities against the main microorganisms isolated from skin and soft tissue infections[1][2][3].
Penicillamine-d3 is the deuterium labeled Penicillamine. Penicillamine (D-(-)-Penicillamine) is the most characteristic degradation product of the penicillin antibiotics. It is used as an antirheumatic and as a chelating agent in Wilson's disease.
Pomalidomide-d3 is the deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors[1][2].
Isoeugenol-d3 is deuterated labeled Sterigmatocystine (HY-N6725). Sterigmatocystine is a precursor of aflatoxins and a mycotoxin produced by common mold strains from Aspergillus versicolor . Sterigmatocystine, a inhibitor of G1 Phase and DNA synthesis, is used to inhibit p21 activity. Sterigmatocystine has teratogenic, and carcinogenic effects in animals [3].
Eugenol acetate-d3 is deuterated labeled Decyl aldehyde (HY-W012570). Decyl aldehyde is a simple ten-carbon aldehyde. Decyl aldehyde is a bacterial luciferase substrate.
Axitinib-d3 (AG-013736-d3) is deuterium labeled Axitinib. Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively[1].
Ropinirole-d3 (hydrochloride) is the deuterium labeled Ropinirole hydrochloride[1]. Ropinirole (SKF 101468) hydrochloride is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease[2][3].
Nabumetone-d3 is the deuterium labeled Nabumetone. Nabumetone is an orally active non-acidic anti-inflammatory agent, acts as a potent and selective COX-2 inhibitor, and is the proagent of the active metabolite 6MNA.
Eletriptan-d3 is the deuterium labeled Eletriptan hydrobromide. Eletriptan hydrobromide is a selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively[1][2].
Vericiguat-d3 (BAY1021189-d3) hydrochloride is a deuterated Vericiguat with tracer functionality. Vericiguat is an orally available stimulator of guanylate cyclase .
Voriconazole-d3 is the deuterium labeled Voriconazole. Voriconazole (UK-109496) is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes[1][2].
Triptolide-d3 is the deuterium labeled Triptolide. Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory, antiproliferative and antitumour effects. Triptolide is a NF-κB activation inhibitor[1][2][3][4][5][6].
Tenidap-d3 is the deuterium labeled Tenidap. Tenidap, a non-steroidal anti-inflammatory drug, is a selective COX-1 inhibitor, with IC50 values of 0.03 μM and 1.2 μM for COX-1 and COX-2, respectively. Tenidap has anti-inflammatory and antirheumatic properties[1][2]. Tenidap is also a specific SLC26A3inhibitor[3].
Etiracetam-d3 is the deuterium labeled Etiracetam. Etiracetam (UCB 6474) is an acetylcholine agonist and a nootropic drug of the racetam family. Less active than its S-enantiomer Levetiracetam (UCB L059)[1].
Medetomidine-d3 (hydrochloride) is the deuterium labeled Medetomidine hydrochloride. Medetomidine hydrochloride is an agonist of adrenergic alpha-2 receptor[1][2].
Nicardipine-d3 (hydrochloride) (YC-93 D3) is the deuterium labeled Nicardipine hydrochloride. Nicardipine hydrochloride is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine hydrochloride acts as an agent for chronic stable angina and for controlling blood pressure[1].
Raltegravir-d3 (potassium) is the deuterium labeled Raltegravir potassium. Raltegravir (MK 0518) potassium is a potent integrase (IN) inhibitor, used to treat HIV infection[1][2].
Sodium 2-oxopropanoate-d3 is the deuterium labeled Sodium 2-oxopropanoate[1]. Sodium 2-oxopropanoate (Sodium pyruvate), a three-carbon metabolite of Glucose, is a compound produced in the glycolytic pathway. Sodium 2-oxopropanoate is a free radical scavenger that can scavenge ROS[2][3].
Terbinafine-d3 (hydrochloride) is the deuterium labeled Terbinafine hydrochloride. Terbinafine hydrochloride (TDT 067 hydrochloride) is an antifungal medication used to treat fungal infections. It is a potent non-competitive inhibitor of squalene epoxidase from Candida with a Ki of 30 nM[1][2]. Terbinafine hydrochloride also antibacterial activity against certain Gram-positive and Gram-negative bacteria[3].
Acetohydrazide-d3 (Ethanehydrazonic acid-d3) is deuterium labeled Acetohydrazide. Acethydrazide is an organic building that undergo catalytic hydrogenation to produce N′-methyl acethydrazide (MAH) .
Omeprazole-d3 sodium is deuterated labeled Omeprazole (HY-B0113). Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) [3].
Acetylpyrazine-d3 is deuterated labeled Linalyl acetate (HY-N6948). Linalyl acetate is the principal components of many plant essential oils with potentially anti-inflammatory activity .
HMMNI-d3 is deuterium labeled HMMNI. HMMNI (Hydroxy dimetridazole) is a hydroxy metabolite of Dimetridazole. Dimetridazole is a nitroimidazole class agent that combats protozoan infections[1].
Clozapine-d3 (HF 1854-d3) is deuterium labeled Clozapine. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively [3]. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) [3] .
Moxidectin-d3(CL-301423-d3) is deuterium labeled Moxidectin. Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk [3] .
Ketoprofen-d3 is the deuterium labeled Ketoprofen. Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC50s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively[1].
Apremilast-d3(CC-10004-d3) is deuterium labeled Apremilast. Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM .
Regadenoson-d3 is the deuterium labeled Regadenoson. Regadenoson (CVT-3146) is a potent and selective A2A adenosine receptor agonist, with Kis of 290 and 1120 nM for rat and pig adenosine A2A receptor, respectively. Regadenoson is selective for the adenosine A2A receptor over adenosine A1 and A2B receptors, and shows 13-fold selectivity over the human adenosine A1 receptor. Regadenoson is a vasodilator stress agent has shifted the landscape of vasodilator myocardial perfusion imaging. Regadenoson increases blood-brain barrier (BBB) permeability in rodents[1][2][3].
Puromycin-d3 is the deuterium labeled Puromycin. Puromycin dihydrochloride is the dihydrochloride salt of puromycin. Puromycin is an aminoglycoside antibiotic that inhibits protein synthesis.
Rabeprazole-d3 (sodium)mis the deuterium labeled Rabeprazole sodium. Rabeprazole sodium (LY307640 sodium) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H+/K+-ATPase. Rabeprazole sodium induces apoptosis. Rabeprazole sodium acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole sodium can be used for the research of gastric ulcerations and gastroesophageal reflux[1][2][3].
Cinacalcet-d3 (hydrochloride) is the deuterium labeled Cinacalcet (hydrochloride). Cinacalcet hydrochloride (AMG-073 hydrochloride) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.
Estradiol benzoate-d3 is the deuterium labeled Estradiol benzoate. Estradiol Benzoate (β-Estradiol 3-benzoate), a proagent of estradiol, acts as a steroid sex hormone. It exhibits mild anabolic and metabolic properties, and increases blood coagulability[1][2][3][4].
L-Serine- 13C3 is the 13C-labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
Lamotrigine- 13C3 is the 13C-labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al[1][2].
3-O-Methyldopa-d3 (hydrate) is the deuterium labeled 3-O-Methyldopa. 3-O-Methyldopa (3-Methoxy-L-tyrosine) is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of l-DOPA and dopamine[1].
Thiamine- 13C3 (hydrochloride) is the 13C-labeled Thiamine (hydrochloride). Thiamine hydrochloride (Thiamine chloride hydrochloride) is an essential micronutrient needed as a cofactor for many central metabolic enzymes.
AalphaC- 15N3 (2-Amino-α-carboline- 15N3) is 15N labeled AalphaC. AalphaC (AαC) is a potential carcinogen with carcinogenic activity. AalphaC is an important biomarker in tobacco smoke and is associated with tobacco smoke exposure. Urinary concentrations of AalphaC are significantly higher in dedicated smokers than in non-smokers, indicating its importance in monitoring tobacco exposure. AalphaC levels increase significantly with increasing serum nicotine levels, indicating its close relationship with tobacco use. In addition, consuming high-temperature cooked beef significantly increases the amount of AalphaC in urine, while consuming vegetables is associated with a decrease in AalphaC concentrations. Smoking half a pack of cigarettes is associated with a significant increase in the amount of AalphaC, which further confirms the biological activity of AalphaC and its association with dietary habits .
Rasagiline- 13C3 ((R)-AGN1135- 13C3; TVP1012- 13C3) mesylate is the deuterium labeled Rasagiline (mesylate) (HY-14605) . Rasagiline (R-AGN1135) mesylate is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively .
Sildenafil-d3-1 (UK-92480-d3-1) is deuterium labeled Sildenafil-d3. Sildenafil (UK-92480) is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM.
L-DOPA-d6 is the deuterium labeled L-DOPA. L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease[1][2][3].
Butylphthalide-d9(3-n-Butylphthalide-d9) is deuterium labeled Butylphthalide. Butylphthalide (3-n-Butylphthalide) is an active molecule against cerebral ischemia. It was originally isolated from celery species and has been shown to be effective in stroke animal models .
Etonogestrel-d6 is deuterium labeled Etonogestrel. Etonogestrel (3-Oxodesogestrel), a biologically active metabolite of progestin Desogestrel, binds with high affinity to progesterone receptors and estrogen receptors in the target organs[1]. Etonogestrel induce FKBP51 mRNA and protein expression in cultured human endometrial stromal cells (HESCs)[2].
(±)-1,2-Propanediol- 13C3 is 13C labeled (±)-1,2-Propanediol (HY-Y0921). (±)-1, 2-propanediol (1,2-(RS)-Propanediol) is an aliphatic alcohol that is often used as an excipient in many active molecular preparations to increase the solubility and stability of the active molecule. (±)-1, 2-propanediol can affect the neurobehavior of zebrafish .
Oseltamivir acid-13C,d3 (GS 4071-13C,d3; Ro 64-0802-13C,d3) is a 13C- and deuterium-labeled Oseltamivir acid (HY-13318). Oseltamivir acid is the active metabolite of Oseltamivir phosphate and inhibits influenza virus neuraminidase (IC50=2 nM). Oseltamivir acid is orally active and can be used to study influenza A/B infections [3] .
Docosanoic acid-d3 (Behenic acid-d3) is the deuterium labeled Docosanoic acid (HY-W013049). Docosanoic acid (Behenic acid) is a long-chain saturated fatty acid. Docosanoic acid inhibits the double-stranded DNA (dsDNA) binding activity of p53 DNA binding domain, with a Kd of 12 nM. Docosanoic acid has low bioavailability and can increase cholesterol in humans [3].
(Rac)-Levomepromazine-d3 (hydrochloride) is a labelled racemic Methotrimeprazine, which is a phenothiazine which has antagonist actions at multiple neurotransmitter receptor sites, including dopaminergic, cholinergic, serotonin and histamine receptors[1][2].
Lignoceric acid-d3 is the deuterium labeled Lignoceric acid[1]. Lignoceric acid (Tetracosanoic acid) is a 24-carbon saturated (24:0) fatty acid, which is synthesized in the developing brain. Lignoceric acid is also a by-product of lignin production. Lignoceric acid can be used for Zellweger cerebro‐hepato‐renal syndrome and adrenoleukodystrophy research[2][3].
Ipratropium-d3 (bromide) is the deuterium labeled Ipratropium bromide. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with binding IC50 values of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma[1][2][3].
Galanthamine-d3 (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD)[1][2][3].
Nonanoic acid-d3 is the deuterium labeled Nonanoic acid. Nonanoic acid is a naturally-occurring saturated fatty acid with nine carbon atoms. Nonanoic acid significantly reduces bacterial translocation, enhances antibacterial activity, and remarkably increases the secretion of porcine β-defensins 1 (pBD-1) and pBD-2[1].
(Rac)-Rotigotine-d3 hydrochloride is a deuterium labeled (Rac)-Rotigotine (hydrochloride) (HY-15394). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
Triclabendazole sulfoxide-d3 is the deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP[1][2].
(R)-(-)-Ibuprofen-d3 is the deuterium labeled (R)-(-)-Ibuprofen. (R)-(-)-Ibuprofen is the R enantiomer of Ibuprofen, inactive on COX, inhibits NF-κB activation; (R)-(-)-Ibuprofen exhibits anti-inflammatory and antinociceptive effects.
Apixaban-d3(BMS-562247-01-d3) is the deuterium labeled Apixaban (HY-50667) . Apixaban (BMS-562247-01) is a highly selective, reversible and orally active inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively . Apixaban is in development for the prevention and treatment of various thromboembolic diseases [3].
Tetrahydrodeoxycorticosterone-d3 is the deuterium labeled Tetrahydrodeoxycorticosterone. Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties[1][2][3].
(S)-(+)-Ibuprofen-d3 is a deuterium labeled (S)-(+)-Ibuprofen. (S)-(+)-Ibuprofen is the S(+)-enantiomer of Ibuprofen that inhibits COX-1 and COX-2 activity with IC50s of 2.1 μM and 1.6 μM. (S)-(+)-Ibuprofen has analgesic, antiinflammatory and antipyretic effects[1][2].
Decanoyl-L-carnitine-d3((-)-Decanoylcarnitine-d3) is deuterium labeled Decanoyl-L-carnitine. Decanoyl-L-carnitine has stimulatory effect on the formation of desaturated fatty acid metabolites from both [1- 14C]-22:4 (n-6) and [1- 14C]-22:5 (n-3) [3].
Homovanillic acid-d3 is the deuterium labeled Homovanillic acid. Homovanillic acid is a dopamine metabolite found to be associated with aromatic L-amino acid decarboxylase deficiency, celiac disease, growth hormone deficiency, and sepiapterin reductase deficiency.
4-Hydroxynonenal-d3 is the deuterium labeled 4-Hydroxynonenal. 4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal and an oxidative/nitrosative stress biomarker. 4-Hydroxynonenal is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2). 4-Hydroxynonenal can modulate a number of signaling processes mainly through forming covalent adducts with nucleophilic functional groups in proteins, nucleic acids, and membrane lipids. 4-Hydroxynonenal plays an important role in cancer through mitochondria[1][2][3].
Octanoic acid-d3 is the deuterium labeled Octanoic acid. Octanoic acid (Caprylic acid) is an oily liquid with a slightly unpleasant rancid taste and used commercially in the production of esters used in perfumery and also in the manufacture of dyes.
Triciribine phosphate-d3 (TCN-P-d3) is a deuterated compound of Triciribine phosphate (TCN-P). TCN-P inhibits adenosine monophosphate (AMP)-activated protein kinase through an allosteric mechanism, affecting the first key step in de novo purine biosynthesis. Triciribine phosphate also inhibits inosine monophosphate dehydrogenase, which is the first key step in guanosine nucleotide synthesis. Triciribine phosphate does not affect ligase activity .
Mometasone furoate-d3 is a deuterium labeled Mometasone furoate. Mometasone furoate (Sch32088) is a glucocorticoid receptor agonist with anti-inflammatory and anti-allergic activity[1].
Cyclobenzaprine-d3 (hydrochloride) is the deuterium labeled Cyclobenzaprine hydrochloride. Cyclobenzaprine hydrochloride (MK130 hydrochloride) is a skeletal muscle relaxant and a central nervous system (CNS) depressant.
Prednisone acetate-d3 is the deuterium labeled Prednisone acetate. Prednisone acetate (Prednisone 21-acetate), the acetate salt form of prednisolone, is a glucocorticoid receptor agonist with anti-inflammatory and immunomodulating properties[1].
Exatecan-d3(DX8951f-d3) mesylate is deuterium-labeled Exatecan mesylate (HY-13631A). Exatecan mesylate is a DNA topoisomerase I inhibitor, with an IC50 of 0.975 μg/mL .
Ulipristal acetate-d3(CDB-2914-d3) is deuterium labeled Ulipristal acetate. Ulipristal acetate (CDB-2914) is an orally active, selective progesterone receptor modulator (SPRM). Ulipristal acetate stimulates the autophagic response selectively in leiomyoma cells. Ulipristal acetate has the potential for benign gynecological conditions treatment, such as uterine myoma [3].
Carbidopa-d3-1 is the deuterium labeled Carbidopa (HY-B0311). Carbidopa, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa inhibits pancreatic cancer cell and tumor growth .
N,N-Dimethylacetamide-d3 is the deuterium labeled N,N-Dimethylacetamide[1]. N,N-Dimethylacetamide (DMAc) is an inexpensive, common aprotic organic solvent[2].
ar-Turmerone-d3 is the deuterium labeled ar-Turmerone. ar-Turmerone ((+)-ar-Turmerone) is a major bioactive compound of the herb Curcuma longa with anti-tumorigenesis and anti-inflammatory activities. ar-Turmerone induces apoptosis in U937 cells. ar-Turmerone exerts positive modulation on murine DCs. ar-Turmerone induces NSC proliferation in vitro and in vivo, and can be used for various neurologic disorders study [3] .
Arachidic acid-d3) is the deuterium labeled Arachidic acid. Arachidonic acid (Icosanoic acid), a long-chain fatty acid, is present in all mammalian cells, typically esterified to membrane phospholipids, and is one of the most abundant polyunsaturated fatty acids present in human tissue[1][2].
D-Serine-d3((R)-Serine-d3) is a deuterium labeled D-Serine (HY-100808). D-Serine ((R)-Serine), an endogenous amino acid involved in glia-synapse interactions that has unique neurotransmitter characteristics, is a potent co-agonist at the NMDA glutamate receptor. D-Serinee has a cardinal modulatory role in major NMDAR-dependent processes including NMDAR-mediated neurotransmission, neurotoxicity, synaptic plasticity, and cell migration [3].
Velpatasvir-d3(GS-5816-d3) is deuterium labeled Velpatasvir. Velpatasvir (VEL, GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons. Velpatasvir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 2.16 μM [3].
Glycopyrrolate-d3 (bromide) is deuterium labeled Glycopyrrolate. Glycopyrrolate (Glycopyrronium bromide), a quaternary ammonium derivative, is a muscarinic receptor antagonist. Glycopyrrolate has bronchoprotective effect and produces a beneficial effect on blood pressure. Glycopyrrolate can be used for the research of bronchial diseases [3] .
Alfuzosin-d3 hydrochloride is the deuterium labeled Alfuzosin hydrochloride. Alfuzosin hydrochloride is an α1 adrenergic receptor antagonist used to treat benign prostatic hyperplasia (BPH).
Abiraterone acetate-d3(CB7630-d3) is deuterium labeled Abiraterone acetate. Abiraterone acetate (CB7630) is an oral, potent, selective, and irreversible inhibitor of CYP17A1 with antiandrogen activity. Abiraterone acetate is a proagent form of Abiraterone (CB7598) .
SN-38-d3 is the deuterium labeled SN-38. SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively[1][2][3][4].
Tropicamide-d3 is the deuterium labeled Tropicamide[1]. Tropicamide (Ro 1-7683) is a selective M4 muscarinic acetylcholine receptor antagonist. Tropicamide produces short acting mydriasis (dilation of the pupil) and cycloplegia when applied as eye drops[2][3].
Trans-Anethole-d3 is deuterated labeled α-Terpineol (HY-N5142). α-Terpineol is isolated from Eucalyptus globulus Labill, exhibits strong antimicrobial activity against periodontopathic and cariogenic bacteria .
α-Terpineol possesses antifungal activity against T. mentagrophytes, and the activity might lead to irreversible cellular disruption .
2-Methoxybenzaldehyde-d3 is the deuterium labeled 2-Methoxybenzaldehyde[1]. 2-Methoxybenzaldehyde (o-Anisaldehyde), isolated from cinnamon essential oil (CEO), exists antibacterial and antifungal activity[2].
Finerenone-d3 is the deuterium labeled finerenone (HY-111372). Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
TRIA-662-d3 is the deuterium labeled TRIA-662[1]. TRIA-662 (1-Methylnicotinamide chloride) is an endogenous metabolite. TRIA-662 shows antithrombotic and anti-inflammatory activities[2].
Nisoldipine-d3 is deuterated labeled Nisoldipine (HY-17402). Nisoldipine (BAY-k 5552; Sular) is a highly efficient and specific L-type Cav1.2 channel blocker with an IC50 of 10 nM.
Carbidopa-d3 (monohydrate) is the deuterium labeled Carbidopa monohydrate. Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa monohydrate is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa monohydrate inhibits pancreatic cancer cell and tumor growth[1][2].
Dolutegravir-d3 is the deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2].
4-Methylanisole-d3 is the deuterium labeled 4-Methylanisole[1]. 4-Methylanisole (4-Methoxytoluene) is food flavoring agent and can be naturally found in Ylang Ylang fragrance oil[2].
Mianserin-d3 (hydrochloride) is the deuterium labeled Mianserin hydrochloride. Mianserin hydrochloride (Org GB 94) is a H1 receptor inverse agonist and is a psychoactive agent of the tetracyclic antidepressant.
Theobromine-d3 is the deuterium labeled Theobromine. Theobromine is a methylxanthine found in cacao beans which can inhibit adenosine receptor A1 (AR1) signaling.
Moxifloxacin-d3 (hydrochloride) is the deuterium labeled Moxifloxacin hydrochloride. Moxifloxacin hydrochloride is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia[1][2][3].
N6-Methyladenosine- 13C3 (6-Methyladenosine- 13C3) is 13C-labeled N6-Methyladenosine (HY-N0086). N6-Methyladenosine is the most prevalent internal (non-cap) modification present in the messenger RNA (mRNA) of all higher eukaryotes. N6-Methyladenosine can modifies viral RNAs and has antiviral activities [3].
Imazamox- 13C,d3 is the 13C- and deuterium labeled Imazamox. Imazamox (CL29926) is a systemic herbicide that inhibits the production of acetolactate synthase (ALS) in plants with high selectivity, high activity, safety and broadspectrum activity, which would then inhibit plant growth and ultimately lead to plant death[1][2].
Rapamycin- 13C,d3 (Sirolimus- 13C,d3; AY-22989- 13C,d3) is the 13C and deuterium labeled Rapamycin (HY-10219) .Rapamycin is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant .
Ritonavir- 13C,d3 is the 13C- and deuterium labeled Ritonavir. Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.61 μM.
Rasagiline- 13C3 (mesylate racemic) is a 13C-labeled Rasagiline mesylate racemic. Rasagiline mesylate racemic is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor[1]. Rasagiline-13C3 (mesylate racemic) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
17α-Hydroxyprogesterone- 13C3 is the 13C-labeled 17α-Hydroxyprogesterone. 17α-Hydroxyprogesterone (17-Hydroxyprogesterone) is an endogenous progestogen as well as chemical intermediate in the biosynthesis of other steroid hormones, including the corticosteroids and the androgens and the estrogens.
Dexmedetomidine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled Dexmedetomidine (hydrochloride). Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine hydrochloride shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine hydrochloride exhibits anxiolysis, sedation, and modest analgesia effects[1][2][3].
Osimertinib- 13C,d3 is the deuterium and 13C labeled Osimertinib. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively.
Cytidine-5'-triphosphate- 15N3,d14 (Cytidine triphosphate- 15N3,d14 dilithium; 5'-CTP- 15N3,d14) dilithium is deuterium and 15N labeled Cytidine-5'-triphosphate (HY-125818). Cytidine 5′-triphosphate (Cytidine triphosphate; 5'-CTP) is a nucleoside triphosphate and serves as a building block for nucleotides and nucleic acids, lipid biosynthesis. Cytidine triphosphate synthase can catalyze the formation of cytidine 5′-triphosphate from uridine 5′-triphosphate (UTP). Cytidine 5′-triphosphate is an essential biomolecule?in the de novo?pyrimidine biosynthetic pathway in?T. gondii.
Deoxycytidine triphosphate- 15N3,d14 (dCTP- 15N3,d14 dilithium; 2′-Deoxycytidine-5′-triphosphate- 15N3,d14) dilithium is deuterium and 15N labeled Deoxycytidine triphosphate (HY-101400). Deoxycytidine triphosphate (dCTP) is a nucleoside triphosphate that can be used for DNA synthesis. Deoxycytidine triphosphate has many applications, such as real-time PCR, cDNA synthesis, and DNA sequencing.
Tramiprosate-d6 is the deuterium labeled Tramiprosate. Tramiprosate (Homotaurine), an orally active and brain-penetrant natural amino acid found in various species of red marine algae. Tramiprosate binds to soluble Aβ and maintains Aβ in a non-fibrillar form. Tramiprosate is also a GABA analog and possess neuroprotection, anticonvulsion and antihypertension effects[1][2][3].
Cytidine 5′-monophosphate- 15N3,d12 (5'-Cytidylic acid- 15N3,d12 dilithium; 5'-CMP- 15N3,d12) dilithium is deuterium and 15N labeled Cytidine 5'-monophosphate (HY-W009162). Cytidine 5'-monophosphate (5'-Cytidylic acid) is a nucleotide which is used as a monomer in RNA. Cytidine 5'-monophosphate consists of the nucleobase cytosine, the pentose sugar ribose, and the phosphate group.
Vanillin- 13C,d3 is the 13C and deuterium labeled Vanillin[1]. Vanillin (p-Vanillin) is a single molecule extracted from vanilla beans and also a popular odor used widely in perfume, food and medicine[2][3].
PSI-6206- 13C,d3 is the deuterium labeled PSI-6206. PSI-6206 is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase. PSI-6206 low potently inhibits HCV replicon with EC90 of >100 μM.
Mifepristone- 13C,d3 is the 13C- and deuterium labeled Mifepristone. Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay[1]. Mifepristone-13C,d3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Etoricoxib- 13C,d3 is the 13C- and deuterium labeled Etoricoxib. Etoricoxib (MK-0663) is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.
Simeprevir- 13C,d3 is the 13C- and deuterium labeled Simeprevir. Simeprevir is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki of 0.36 nM. Simeprevir inhibits HCV replication with an EC50 of 7.8 nM. Simeprevir also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir inhibits the main protease (Mpro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses[1][2][5].
L-Serine- 15N,d3 is the deuterium and 15N-labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
3-Indoleacetic acid-2,2-d2 is the deuterium labeled 3-Indoleacetic acid (HY-18569). 3-Indoleacetic acid (Indole-3-acetic acid) is the most common natural plant growth hormone of the auxin class. It can be added to cell culture medium to induce plant cell elongation and division .
cis-Urocanic acid- 13C3 is the 13C-labeled cis-Urocanic acid. cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor[1].
Trametinib- 13C,d3 is the 13C- and deuterium labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis[1][2].
Lamotrigine- 13C,d3 is the 13C- and deuterium labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al[1][2].
Clindamycin-d3 (hydrochloride) is the deuterium labeled Clindamycin. Clindamycin is an orally active and broad-spectrum bacteriostatic lincosamide antibiotic. Clindamycin can inhibit bacterial protein synthesis, possessing the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla). Clindamycin also can be used for researching malaria[1][2].
3α,21-Dihydroxy-5α-pregnan-20-one-d3 is the deuterium labeled 3α,21-Dihydroxy-5α-pregnan-20-one. 3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.
3-Amino-2-oxazolidinone-d4 is a deuterium labeled 3-Amino-2-oxazolidinone. 3-Amino-2-oxazolidinone (AOZ) is the metabolite of Furazolidone (HY-B1336). 3-Amino-2-oxazolidinone is always be detected as an indicator of furazolidone residues[1][2].
1-Methylguanosine-d3 is deuterium labeled 1-Methylguanosine (HY-113136). 1-Methylguanosine is a methylated nucleoside originating from RNA degradation. 1-Methylguanosine is a tumour marker.
Idasanutlin-d3-1(RG7388-d3-1) is the deuterium labeled Idasanutlin. Idasanutlin is a potent antagonist of MDM2/p53. Idasanutlin inhibits relapsed or refractory acute myeloid leukemia .
2,5-Dimethylpyrazine-d3 is deuterated labeled γ-Terpinene (HY-W020183). γ-Terpinene, a monoterpene, is an orally active antioxidant compound which can scavenge radicals directly. γ-Terpinene has potent antinociception activity .
Oxaceprol-d3(N-Acetyl-L-hydroxyproline-d3) is deuterium labeled Oxaceprol. Oxaceprol (N-Acetyl-L-hydroxyproline), an orally active derivative of L-proline, possesses distinct anti-inflammatory activity. Oxaceprol is usually used for the research of osteoarthritis and rheumatoid arthritis [3].
Rosuvastatin-d3 is a deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM[1]. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals[2].
Ceramide 3-d3 (N-Stearoyl phytosphingosine-d3) is deuterium labeled Ceramide 3. C18 Phytoceramide (t18:0/18:0) (Cer(t18:0/18:0)) is a bioactive sphingolipid found in the stratum corneum of Saccharomyces cerevisiae, wheat grain, and mammalian epidermis. Cer(t18:0/18:0) consists of a phytosphingosine backbone amine linked to a C18 fatty acid chain. Cer(t18:0/18:0) has the function of regulating apoptosis, cell differentiation, proliferation of smooth muscle cells and inhibition of mitochondrial respiratory chain. It also suppresses the expression of allergic cytokines IL-4, TNF-α, and transcription factors c-Jun and NF-κB in histone-stimulated mouse skin tissue. Formulations containing cer(t18:0/18:0) have been used as skin protectants in cosmetics as they reduce water loss and prevent epidermal dehydration and irritation .
Sorafenib-d3 (Donafenib) tosylate is the 13C- and deuterium labeled Sorafenib. Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator .
Tiotropium-d3 (bromide) is the deuterium labeled Tiotropium (Bromide). Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
1-Methylinosine-d3 is the deuterium labeled 1-Methylinosine. 1-Methylinosine is a modified nucleotide found at position 37 in tRNA 3' to the anticodon of eukaryotic tRNA[1].
Isovanillin-d3 is the deuterium labeled Isovanillin[1]. Isovanillin is an aldehyde oxidase inhibitor[2]. Antispasmodic activities[3]. Antidiarrheal activities[4].
2-Methylcitric acid-d3 is the deuterium labeled 2-Methylcitric acid. 2-Methylcitric acid (Methylcitric acid) is an endogenous metabolite in the 2-methylcitric acid cycle. 2-Methylcitric acid accumulates in methylmalonic and propionic acidemias and acts as a marker metabolite. 2-Methylcitric acid markedly inhibits ADP-stimulated and uncoupled respiration in mitochondria supported by glutamate[1].
Omeprazole-d3-1 is the deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
Spironolactone-d3-1 is deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC50 of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes[1][2][3].
Sorafenib-d3 (Donafenib), a deuterated compound of Sorafenib, is the first deuterium-generation tumor suppressor small molecule. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively .
16α-Hydroxyprednisolone-d3 is the deuterium labeled 16α-Hydroxyprednisolone. 16α-Hydroxyprednisolone is a stereoselective metabolite of the 22(R) epimer of the glucocorticoid budesonide via cytochrome P450 3A (CYP3A) enzymes[1][2].
Cyclobenzaprine-d3-1 hydrochloride (MK130-d3-1 hydrochloride) is the deuterium labeled Cyclobenzaprine hydrochloride (HY-B0740). Cyclobenzaprine (MK130) hydrochloride is an orally active 5-HT2 receptor antagonist. Cyclobenzaprine hydrochloride acts centrally, providing skeletal muscle relaxation, alleviating muscle spasms, and reducing pain. Additionally, Cyclobenzaprine hydrochloride has antiprotozoal activity. Additionally, Cyclobenzaprine hydrochloride also possesses antiparasitic activity. Cyclobenzaprine hydrochloride holds promise for research in the fields of acute, painful skeletal muscle disorders and infectious diseases [3]
2-Hydroxymethyl olanzapine-d3 (LY-290411-d3) is a deuterium labeled 2-Hydroxymethyl olanzapine. 2-Hydroxymethyl olanzapine is a metabolite of Olanzapine. .
3-Hydroxy Midostaurin-d5 is a deuterium labeled 3-Hydroxy Midostaurin. 3-Hydroxy Midostaurin is a metabolite of PKC412, which effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively[1].
Sulindac sulfide-d3 is deuterium labeled Sulindac sulfide. Sulindac sulfide is a noncompetitive γ-secretase inhibitor, with an IC50 of 20.2 μM for γ42-secretase activity.
Nemonoxacin-d3-1 is the deuterium labeled Nemonoxacin. Nemonoxacin (TG-873870) is an orally active and potent broad-spectrum antibiotic. Nemonoxacin shows good inhibitory activity against different species of staphylococci, streptococci, and enterococci, Neisseria gonorrhoeae, and Haemophilus influenza. Nemonoxacin can be used in the study of bacterial infections and community-acquired pneumonia[1][2][3].
Perindoprilat-d3 disodium is deuterated labeled Perindoprilat (HY-B1433). Perindoprilat (S 9780) is an angiotensin-converting enzyme (ACE) inhibitor with the IC50 value ranging from 1.5 to 3.2 nM. Perindoprilat can be used in hypertension research .
Voriconazole N-oxide-d3 (Voriconazole oxynitride-d3) is deuterium labeled Voriconazole N-oxide. Voriconazole N-oxide (Voriconazole oxynitride) is a potent antifungal agent. Voriconazole N-oxide has phototoxicity and photocarcinogenicity. Voriconazole N-oxide does not sensitize keratinocytes to ultraviolet B (UVB) .
Linagliptin-d3-1 (BI 1356-d3-1) is the deuterium labeled Linagliptin (HY-10284). Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM .
rac-Vofopitant-d3 (rac-GR 205171-d3) is the deuterium labeled Vofopitant (HY-12142) . Vofopitant is potent tachykinin NK1 receptor antagonist, with pKis of 10.6, 9.5, and 9.8 for human, rat and ferret NK1 receptor, respectively .
Alogliptin-d3 is the deuterium labeled Alogliptin. Alogliptin (SYR-322 free base) is a potent, selective and orally active inhibitor of DPP-4 with an IC50 of <10 nM, and exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9. Alogliptin can be used for the research of type 2 diabetes[1][2][3].
Melatonin-d3 is the deuterium labeled Melatonin. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties [3]. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation . Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress .
Skatole-d8 is the deuterium labeled Skatole. Skatole is produced by intestinal bacteria, regulates intestinal epithelial cellular functions through activating aryl hydrocarbon receptors and p38[1].
β-Alanine-d4 is the deuterium labeled β-Alanine. β-Alanine is a non-essential amino acid that is shown to be metabolized into carnosine, which functions as an intracellular buffer.
Tegaserod- 13C,d3 (maleate) is the 13C- and deuterium labeled Tegaserod (maleate). Tegaserod maleate is a selective 5-HT4 receptor partial agonist and a 5-HT2B receptor antagonist. Tegaserod maleate exhibits a promotile effect throughout the gastrointestinal (GI) tract[1][2][5].
Erythromycin ethylsuccinate- 13C,d3 is the 13C- and deuterium labeled Erythromycin Ethylsuccinate. Erythromycin Ethylsuccinate is an antibiotic useful for the treatment of a number of bacterial infections, has an antimicrobial spectrum similar to or slightly wider than that of penicillin. Erythromycin Ethylsuccinate has antiviral activity against HIV-1.
Phenylephrine-2,4,6-d3 (hydrochloride) is the deuterium labeled Phenylephrine hydrochloride. (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
Etoposide- 13C,d3 is the 13C- and deuterium labeled Etoposide. Etoposide (VP-16; VP-16-213) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy[1].
Cinnamic acid- 13C3 (3-Phenylacrylic acid- 13C3) is the 13C labeled Cinnamic acid (HY-N0610A). Cinnamic acid has potential use in cancer intervention, with IC50s of 1-4.5 mM in glioblastoma, melanoma, prostate and lung carcinoma cells .
3-Indoleacetic acid- 13C6 is the 13C labeled 3-Indoleacetic acid (HY-18569). 3-Indoleacetic acid (Indole-3-acetic acid) is the most common natural plant growth hormone of the auxin class. It can be added to cell culture medium to induce plant cell elongation and division .
Dabigatran- 13C,d3 is the 13C- and deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
Sofosbuvir- 13C,d3 is the deuterium labeled Sofosbuvir. Sofosbuvir (PSI-7977) is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.
Lumateperone- 13C,d3 (ITI-007- 13C,d3) tosylate is 13C and deuterium labeled Lumateperone (tosylate). Lumateperone (ITI-007) tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia [3] .
Clindamycin- 13C,d3 is the 13C- and deuterium labeled Clindamycin. Clindamycin is an orally active and broad-spectrum bacteriostatic lincosamide antibiotic. Clindamycin can inhibit bacterial protein synthesis, possessing the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla). Clindamycin also can be used for researching malaria[1][2][3].
Cytidine-5'-triphosphate- 15N3 (Cytidine triphosphate- 15N3 dilithium; 5'-CTP- 15N3) dilithium is 15N labeled Cytidine-5'-triphosphate (HY-125818). Cytidine 5′-triphosphate (Cytidine triphosphate; 5'-CTP) is a nucleoside triphosphate and serves as a building block for nucleotides and nucleic acids, lipid biosynthesis. Cytidine triphosphate synthase can catalyze the formation of cytidine 5′-triphosphate from uridine 5′-triphosphate (UTP). Cytidine 5′-triphosphate is an essential biomolecule?in the de novo?pyrimidine biosynthetic pathway in?T. gondii.
Deoxycytidine triphosphate- 15N3 (dCTP- 15N3 dilithium; 2′-Deoxycytidine-5′-triphosphate- 15N3) dilithium is 15N labeled Deoxycytidine triphosphate (HY-101400). Deoxycytidine triphosphate (dCTP) is a nucleoside triphosphate that can be used for DNA synthesis. Deoxycytidine triphosphate has many applications, such as real-time PCR, cDNA synthesis, and DNA sequencing.
Fluralaner- 13C2, 15N,d3 is the deuterium, 13C-, and 15-labeled Fluralaner. Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels.
3,4-Dehydro Cilostazol-d11 is deuterated labeled 3,4-Dehydro Cilostazol (HY-135910). 3,4-Dehydro Cilostazol (OPC-13015) is an active metabolite of Cilostazol (CLZ; HY-17464). 3,4-Dehydro Cilostazol is used for pharmacokinetic study .
1,3,5-Trimethoxybenzene-d3 (Trimethyl phloroglucinol-d3) is the deuterium labeled 1,3,5-Trimethoxybenzene (HY-Y0678). 1,3,5-Trimethoxybenzene is a key component of the Chinese rose odor. 1,3,5-Trimethoxybenzene is synthesized in three successive methylation steps from phloroglucinol, the initial precursor .
4-Acetamidobutanoic acid-d3 is the deuterated analog of 4-Acetamidobutanoic acid (HY-101411). 4-Acetamidobutanoic acid (N-acetyl GABA), the main metabolite of GABA, exhibits antioxidant and antibacterial activities .
N-Acetyl-L-methionine-d3 is the deuterium labeled N-Acetyl-L-methionine. N-Acetyl-L-methionine, a human metabolite, is nutritionally and metabolically equivalent to L-methionine. L-methionine is an indispensable amino acid required for normal growth and development[1].
6β-Naltrexol-d3(6β-Hydroxynaltrexone-d3) is deuterium labeled 6β-Naltrexol. 6β-Naltrexol (6β-Hydroxynaltrexone), the primary metabolite of Naltrexone, is a peripherally selective opioid antagonist. 6β-Naltrexol selectively inhibits gastrointestinal opioid effects in human subjects and inhibits Morphine-induced slowing of gastrointestinal transit .
3-O-Methyltolcapone-d7 is a deuterium labeled 3-O-Methyltolcapone. 3-O-Methyltolcapone is a metabolite of Tolcapone. Tolcapone is an orally active, reversible, selective and potent COMT inhibitor. Tolcapone crosses the blood-brain barrier, and can be used for treatment of Parkinson's disease[1][2].
2-Acetylfuran-d3 is deuterated labeled Citreoviridin (HY-N6745). Citreoviridin, a toxin from Penicillium citreoviride NRRL 2579, inhibits brain synaptosomal Na +/K +-ATPase whereas in microsomes, both Na +/K +-ATPase and Mg 2+-ATPase activities are significantly stimulated in a dose-dependent manner . Citreoviridin inhibits cell proliferation and enhances apoptosis of human umbilical vein endothelial cells .
Ceftriaxone-d3 (disodium) is the deuterium labeled Ceftriaxone. Ceftriaxone is a third-generation cephalosporin antibiotic with excellent activity against many gram-negative, and reasonable activity against most gram-positive microorganisms. Anti-inflammatory and antioxidant characteristics[1][2].
L-Alanine-d3 is the deuterium labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
Calcifediol-d3 is a deuterium labeled Calcifediol. Calcifediol, is an effective VDR ligand and VD supplement. Calcifediol is a prohormone of the vitamin D endocrine system (VDES) and is hydroxylated in the liver to produce the active form, calcitriol. Calcifediol can rapidly increase serum VD levels [3].
Glycerol- 13C3 is the 13C labeled Glycerol[1]. Glycerol is used in sample preparation and gel formation for polyacrylamide gel electrophoresis[2][3][4].
Salmeterol-d3 (xinafoate) is the deuterium labeled Salmeterol xinafoate. Salmeterol (GR 33343X) xinafoate is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively[1].
Ercalcidiol-d3 is the deuterium labeled Ercalcidiol. Ercalcidiol is a metabolite of Vitamins D2. Ercalcidiol can be used as an indicator of vitamins D status .
Estriol- 13C3 is the 13C-labeled Estriol. Estriol is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.
DL-Alanine-d3 is the deuterium labeled DL-Alanine. DL-alanine, an amino acid, is the racemic compound of L- and D-alanine. DL-alanine is employed both as a reducing and a capping agent, used with silver nitrate aqueous solutions for the production of nanoparticles. DL-alanine can be used for the research of transition metals chelation, such as Cu(II), Zn(II), Cd(11). DL-alanine, a sweetener, is classed together with glycine, and sodium saccharin. DL-alanine plays a key role in the glucose-alanine cycle between tissues and liver[1][2][3][4][5][6].
2-Sec-butyl-3-methoxypyrazine-d3 is deuterated labeled cis-?Jasmone (HY-N7058). Cis-Jasmone is a plant-derived natural product. Cis-Jasmone is constitutively released by many flowers and sometimes by leaves as an attractant for pollinators or as a chemical cue for host location by insect flower herbivores. Cis-Jasmone treatment of crop plants not only induces direct defense against herbivores, but also induces indirect defense by releasing VOCs that attract natural enemies .
p-Toluic acid-d3 is the deuterium labeled p-Toluic acid[1]. p-Toluic acid (4-Methylbenzoic acid) is a substituted benzoic acid and can be used as an intermediate for the synthesis of para-aminomethylbenzoic acid (PAMBA), p-tolunitrile, etc.
(±)-Taxifolin-13C3 ((±)-Dihydroquercetin-13C3) is a derivative of (±)-Taxifolin, labeled with 13C3. (±)-Taxifolin is the racemate of Taxifolin. Taxifolin exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM . Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity .
Calcitriol-d3 is the deuterium labeled Calcitriol[1]. Calcitriol is the most active metabolite of vitamin D and also a vitamin D receptor (VDR) agonist[2][3][4][5].
3-Methyl-2-quinoxalinecarboxylic acid-d4 is the deuterium labeled 3-Methyl-2-quinoxalinecarboxylic acid. 3-Methyl-2-quinoxalinecarboxylic acid (MQCA), an important N-oxide reductive metabolite of Quinocetone or Olaquindox, potently inhibits the growth of Chang liver cells through S phase arrest of the cell cycle[1].
1,3-Dimethoxybenzene-d3 (Resorcinol dimethyl ether-d3) is the deuterium labeled 1,3-Dimethoxybenzene (HY-34487). 1,3-Dimethoxybenzene belongs to the class of organic compounds known as dimethoxybenzenes. 1,3-Dimethoxybenzene is an intermediate in synthesis of organic compounds .
3-O-Methyltolcapone-d4 is the deuterium labeled 3-O-Methyltolcapone. 3-O-Methyltolcapone (Ro 40-7591) is a metabolite of Tolcapone. Tolcapone is an orally active, reversible, selective and potent COMT inhibitor. Tolcapone crosses the blood-brain barrier, and can be used for treatment of Parkinson's disease[1][2].
Histamine- 15N3 is the 15N3-labeled Histamine (HY-B1204). Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter .
(E)-Ferulic acid-d3 is the deuterium labeled (E)-Ferulic acid. (E)-Ferulic acid is a isomer of Ferulic acid which is an aromatic compound, abundant in plant cell walls. (E)-Ferulic acid causes the phosphorylation of β-catenin, resulting in proteasomal degradation of β-catenin and increases the expression of pro-apoptotic factor Bax and decreases the expression of pro-survival factor survivin. (E)-Ferulic acid shows a potent ability to remove reactive oxygen species (ROS) and inhibits lipid peroxidation. (E)-Ferulic acid exerts both anti-proliferation and anti-migration effects in the human lung cancer cell line H1299[1].
Moxifloxacin-d3-1 hydrochloride (BAY 12-8039-d3-1) is a deuterium labeled Moxifloxacin (HY-66011A). Moxifloxacin is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia [3].
Fmoc-Asp(OtBu)-OH-d3 (4-tert-Butyl N-(fluoren-9-ylmethoxycarbonyl)-L-aspartate-d3) is deuterium labeled Fmoc-Asp(OtBu)-OH. Fmoc-Asp(OtBu)-OH (4-tert-Butyl N-(fluoren-9-ylmethoxycarbonyl)-L-aspartate) is a aspartate derivative containing amine protecting group Fmoc. Fmoc-Asp(OtBu)-OH can be used for peptide synthesis .
Cytidine- 15N3 is the 15N labeled Cytidine[1]. Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catecholamine synthesis, and mitochondrial function[2][3][4].
Cytidine 5′-monophosphate- 15N3 (5'-Cytidylic acid- 15N3 dilithium; 5'-CMP- 15N3) dilithium is 15N labeled Cytidine 5'-monophosphate (HY-W009162). Cytidine 5'-monophosphate (5'-Cytidylic acid) is a nucleotide which is used as a monomer in RNA. Cytidine 5'-monophosphate consists of the nucleobase cytosine, the pentose sugar ribose, and the phosphate group.
Deoxycytidine triphosphate- 13C9, 15N3 (dCTP- 13C9, 15N3 dilithium; 2′-Deoxycytidine-5′-triphosphate- 13C9, 15N3) dilithium is 13C and 15N-labeled Deoxycytidine triphosphate (HY-101400). Deoxycytidine triphosphate (dCTP) is a nucleoside triphosphate that can be used for DNA synthesis. Deoxycytidine triphosphate has many applications, such as real-time PCR, cDNA synthesis, and DNA sequencing.
Cytidine 5′-monophosphate- 13C9, 15N3 (5'-Cytidylic acid- 13C9, 15N3 dilithium; 5'-CMP- 13C9, 15N3) dilithium is 13C and 15N-labeled Cytidine 5'-monophosphate (HY-W009162). Cytidine 5'-monophosphate (5'-Cytidylic acid) is a nucleotide which is used as a monomer in RNA. Cytidine 5'-monophosphate consists of the nucleobase cytosine, the pentose sugar ribose, and the phosphate group.
Cytidine- 13C9, 15N3 is the 13C and 15N labeled Cytidine[1]. Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catecholamine synthesis, and mitochondrial function[2][3][4].
Sodium 2-oxopropanoate- 13C3 is the 13C-labeled Sodium 2-oxopropanoate. Sodium 2-oxopropanoate (Sodium pyruvate), a three-carbon metabolite of Glucose, is a compound produced in the glycolytic pathway. Sodium 2-oxopropanoate is a free radical scavenger that can scavenge ROS[1][2].
(E)-10-Hydroxynortriptyline-d3 is a deuterium labeled (E)-10-Hydroxy Nortriptyline. (E)-10-Hydroxy Nortriptyline is a metabolite of Nortriptyline. Nortriptyline is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and is used to relieve the symptoms of depression[1].
5-Methyl-1H-benzotriazole-d3(5-Methylbenzotriazole-d3) is the deuterium labeled 5-Methyl-1H-benzotriazole (HY-W086988). 5-Methyl-1H-benzotriazole is a biological material or organic compound that can be used in life science research .
3-Epiglycyrrhetinic acid-d2 (3α-Glycyrrhetic acid-d2) is the deuterium-labeled 3-Epiglycyrrhetinic acid. 3-Epiglycyrrhetinic acid is a derivative of glycyrrhetic acid. Glycyrrhetic acid and its derivative are considered to have anti-inflammatory, anti-ulcer, and antiviral activities .
Dantrolene- 13C3 is the 13C3 labeled Dantrolene. Dantrolene (F368), a muscle relaxant, non-competitively inhibits human erythrocyte glutathione reductase. Ki and IC50 values are 111.6 μM and 52.3 μM, respectively. Dantrolene is a ryanodine receptor antagonist and Ca2+ signaling stabilizer. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome.
Amiloride- 15N3 (hydrochloride) is the 15N labeled Amiloride hydrochloride[1]. Amiloride hydrochloride (MK-870 hydrochloride) is an inhibitor of both epithelial sodium channel (ENaC[2]) and urokinase-type plasminogen activator receptor (uTPA[3]). Amiloride hydrochloride is a blocker of polycystin-2 (PC2;TRPP2[4]) channel.
1-Bromo-3-methoxybenzene-d3 is the deuterium labeled 1-Bromo-3-methoxybenzene. Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Etbicyphat- 13C3 is the 13C labeled Etbicyphat (HY-139145). Etbicyphat is a potent GABA(A) receptors competitive antagonist. Etbicyphat induces epileptiform activities in hippocampal CA1 neurons, and binds to the GABA(A)-benzodiazepine receptors[1][2].
Varenicline-15N3 Hydrochloride (CP 526555-15N3 Hydrochloride) is the 15N labeled isotope of Varenicline hydrochloride (HY-10020). Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation [3] .
Favipiravir- 13C3 is the 13C labeled isotope of Favipiravir- 13C3(HY-14768 ).Favipiravir (T-705) is a potent viral RNA polymerase inhibitor, it is phosphoribosylated by cellular enzymes to its active form, Favipiravir-ribofuranosyl-5′-triphosphate (RTP). Favipiravir-RTP inhibits the influenza viral RNA-dependent RNA polymerase (RdRP) activity with an IC50 of 341 nM.
Trifluoperazine N-glucuronide-d3 is deuterium labeled Trifluoperazine N-Glucuronide. Trifluoperazine N-Glucuronide (UGT1A4), as one of the human UGT1A isoforms, is expressed in the liver. Trifluoperazine N-Glucuronide catalyzes the imipramine and trifluoperazine Nglucuronide formation[1].
Lactate-d3 sodium (60% in water) is the deuterium labeled Lactate sodium (60% in water). Lactate sodium (60% in water) is the product of glycogenolysis and glycolysis. Lactate sodium (60% in water) functions in a variety of biochemical processes .
Histamine- 13C5, 15N3 (Ergamine- 13C5, 15N3) is the 13C and 15N labeled isotope of Histamine (HY-B1204). Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter .
Ceftriaxone- 13C2,d3 triethylammonium salt is 13C and deuterated labeled Ceftriaxone (HY-B0712). Ceftriaxone (Ro 13-9904 free acid) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone is a covalent inhibitor of GSK3β with IC50 value of 0.78 mM. Ceftriaxone is an inhibitor of Aurora B. Ceftriaxone has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone can be used in the study of bacterial infections and meningitis [3] .
Nicotinamide- 15N, 13C3 is the 13C-labeled and 15N-labeled Nicotinamide. Nicotinamide is a form of vitamin B3 that plays essential roles in cell physiology through facilitating NAD+ redox homeostasis and providing NAD+ as a substrate to a class of enzymes that catalyze non-redox reactions. Nicotinamide is an inhibitor of SIRT1.
N-Hexanoyl-L-Homoserine lactone-d3(C6-HSL-d3) is deuterium labeled N-Hexanoyl-L-homoserine lactone. N-Hexanoyl-L-homoserine lactone is a short-chained N-acyl homoserine lactone (AHL). Diatoms are frequently found in association with Proteobacteria, many members of which employ cell-to-cell communication via AHLs in aquatic habitats .
Ibuprofen- 13C,d3 is the 13C- and deuterium labeled Ibuprofen. Ibuprofen is an anti-inflammatory agent targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively .
Indole-3-carboxaldehyde- 13C (3-Formylindole- 13C) is a 13C labeled Indole-3-carboxaldehyde (HY-W007376). Indole-3-carboxaldehyde (3-Formylindole), a banlangen extract, is the product of the oxidative degradation of indole-3-acetic acid (IAA) by crude enzyme preparations from etiolated pea seedlings. Indole-3-carboxaldehyde (3-Formylindole) is a biochemical used to prepare analogs of the indole phytoalexin cyclobrassinin .
Acetyl-L-carnitine-d3 (hydrochloride) is the deuterium labeled Acetyl-L-carnitine hydrochloride. Acetyl-L-carnitine hydrochloride is a blood-brain permeable acetyl ester of the amino acid L-carnitine found in the body. Acetyl-L-carnitine hydrochloride is often used as a dietary supplement, and exibits anti-stress-related psychiatric disorders[1].
Myrcene- 13C3 is 13C labeled trans-2-Decenal (HY-W015551). trans-2-Decenal is an important raw material and intermediate used in organic synthesis, medicine, pesticides and dyes.
Ercalcitriol-d3 is the deuterium labeled Ercalcitriol. Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Pyruvic acid-13C is isotype-labeled compound of Pyruvic acid. Pyruvic acid is an intermediate metabolite in the metabolism of carbohydrates, proteins, and fats .
Guanidine- 13C, 15N3 (hydrochloride)is the 13C-labeled and 15N-labeled Guanidine hydrochloride. Guanidine hydrochloride (Guanidinium chloride) a strong chaotrope, is also a strong denaturant of proteins[1][2].
L-Serine- 13C3, 15N is the 13C- and 15N-labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
L-DOPA- 13C6 is the 13C-labled L-DOPA . L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease [3] .
L-Histidine- 13C6, 15N3,d5 (hydrochloride hydrate) is the deuterium, 13C-, and 15-labeled L-Histidine hydrochloride hydrate. L-Histidine hydrochloride hydrate (H-His-OH.HCl.H2O) is an endogenous metabolite.
Doravirine-13C,d3 (MK-1439-13C,d3) is the deuterium labeled Doravirine (HY-16767). Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181Creverse transcriptase mutants, respectively .
5-Methylcytidine 5′-triphosphate-d3 trisodium is the deuterium labeled 5-Methylcytidine 5’-triphosphate trisodium (HY-147338A). 5-Methylcytidine 5′-triphosphate (5-Methyl-CTP) trisodium is a modified nucleoside triphosphate. 5-Methylcytidine 5′-triphosphate trisodium can apply in replacing unmodified mRNA, resulting in the increase of translational properties and stability, as well as the reduction of innate immune responses in human and other mammalian cells .
Chlortetracycline-13C,d3 hydrochloride (7-Chlorotetracycline-13C,d3 hydrochloride) is the 13C- and deuterium labeled Chlortetracycline hydrochloride (HY-B1327). Chlortetracycline hydrochloride is an orally active, selective antibiotic, that inhibits methanogenic bacteria through inhibition of bacterial protein synthesis. Chlortetracycline hydrochloride is a specific and potent calcium ionophore antibiotic, that inhibits binding of aminoacyl-tRNA to ribosomes [3] .
Apalutamide- 13C,d3 is the 13C- and deuterium labeled Apalutamide. Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM[1].
Axitinib- 13C,d3 is a 13C-labeled and deuterium labeled Axitinib. Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50 values of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively .
Pazopanib- 13C,d3 (hydrochloride) is the deuterium and 13C labeled Pazopanib hydrochloride[1]. Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively[2][3].
Sulfasalazine-d3,15N is 15N and deuterated labeled Sulfasalazine (HY-14655). Sulfasalazine (NSC 667219) is an anti-rheumatic agent for the research of rheumatoid arthritis and ulcerative colitis. Sulfasalazine can suppress NF-κB activity. Sulfasalazine is a type 1 ferroptosis inducer [3] .
Istradefylline- 13C,d3 is the 13C- and deuterium labeled Istradefylline. Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.
Medetomidine-13C,d3 (hydrochloride) is a deuterated labeled Medetomidine (hydrochloride) . Medetomidine hydrochloride is an orally active α2-adrenoceptor agonist (Ki: 1.08 nM). Medetomidine hydrochloride has sedative and analgesic effects. Medetomidine hydrochloride can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels [3] .
Moxonidine- 13C,d3 hydrochloride is 13C and deuterated labeled Moxonidine hydrochloride (HY-B0374A). Moxonidine (BDF5895) hydrochloride is an imidazoline type 1 receptor (I1-R) selective agonist and antihypertensive agent.
Pazopanib- 13C,d3 is the deuterium and 13C labeled Pazopanib[1]. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively[2][3].
Elagolix- 13C,d3 (sodium) is the 13C- and deuterium labeled Elagolix sodium. Elagolix sodium is a human GnRH receptor (GnRHR) antagonist with an IC50 and Ki of 0.25 and 3.7 nM, respectively.
Linagliptin- 13C,d3 is the 13C- and deuterium labeled Linagliptin. Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM. Linagliptin-13C,d3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Cilastatin- 15N,d3 is a 15N-labeled and deuterium labeled Cilastatin. Cilastatin (MK0791) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin is an antibacterial adjunct[1][2][3].
Raltegravir- 13C,d3 potassium is 13C labeled Raltegravir potassium (HY-10353A). Raltegravir (MK 0518) potassium is a potent integrase (IN) inhibitor, used to treat HIV infection.
Pravastatin- 13C,d3 (sodium) is the 13C- and deuterium labeled Pravastatin (sodium). Pravastatin sodium (CS-514 sodium) is an HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM.
Omeprazole- 13C,d3 is a 13C-labeled and deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
Flurbiprofen- 13C,d3 is the 13C- and deuterium labeled Flurbiprofen. Flurbiprofen (dl-Flurbiprofen) is a potent, orally active nonsteroidal anti-inflammatory agent (NSAIA/NSAID), with antipyretic and analgesic activities. Flurbiprofen is commonly used for the research of inflammatory diseases, including osteoarthritis and rheumatoid arthritis. Flurbiprofen is a non-selective cyclooxygenase (COX) inhibitor that can be used for the research of colorectal cancer[1][2][3].
Fluvoxamine- 13C, d3 maleate is 13C and deuterated labeled Fluvoxamine maleate (HY-B0103A). Fluvoxamine maleate (DU-23000 maleate) is an antidepressant which functions pharmacologically as a selective serotonin reuptake inhibitor.
Taltirelin- 13C,d3 (TA-0910- 13C,d3) is 13C and deuterated labeled Taltirelin (HY-B0596). Taltirelin (TA0910) is a superagonist at thyrotropin-releasing hormone receptor (TRH-R) with an IC50 of 910 nM and EC50 of 36 nM for stimulating an increase in cytosolic Ca 2+ concentration (Ca 2+ release).
Encorafenib- 13C,d3 is the 13C- and deuterium labeled Encorafenib. Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).
Velpatasvir- 13C,d3 (GS-5816- 13C,d3) is 13C and deuterium labeled Velpatasvir. Velpatasvir (VEL, GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons. Velpatasvir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 2.16 μM [3].
Zafirlukast- 13C,d3 is the 13C- and deuterium labeled Zafirlukast. Zafirlukast (ICI 204219) is a potent orally active leukotriene D4 (LTD4) receptor antagonist. Zafirlukast shows anti-asthmatic, anti-inflammatory and anti-bacterial effects.
L-Histidine- 15N3 (hydrochloride hydrate) is the 15N-labeled L-Histidine hydrochloride hydrate. L-Histidine hydrochloride hydrate (H-His-OH.HCl.H2O) is an endogenous metabolite.
Almorexant- 13C,d3 is the 13C- and deuterium labeled Almorexant. Almorexant (ACT 078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM, respectively.
Trelagliptin-13C,d3 is a deuterated labeled Trelagliptin . Trelagliptin (SYR-472) is a potent, orally active and highly selective DPP-4 inhibitor with an IC50 of 4 nM. Trelagliptin succinate improves glycemic control in vivo and can be used for the study of type 2 diabetes mellitus (T2DM) .
Trimegestone- 13C,d3 is 13C and deuterated labeled Trimegestone (HY-106827). Trimegestone (RU 27987) is an orally active 19-norpregnane progestin. Trimegestone binds to progesterone receptor (PR) with an IC50 value of 3.3 nM (rat PR). Trimegestone increases alkaline phosphatase activity (EC50=0.1 nM) but not luciferase activity. Trimegestone also shows a weak antiandrogenic activity (weak androgen receptor affinity). Trimegestone can be used in studies of contraception or menopausal syndromes .
Butenafine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled. Butenafine Hydrochloride (KP363 Hydrochloride) is a synthetic benzylamine antifungal, works by inhibiting the synthesis of sterols by inhibiting squalene epoxidase.
Nintedanib- 13C,d3 is the 13C- and deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
Rabeprazole-13C,d3 is a deuterated labeled Rabeprazole . Rabeprazole (LY307640) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H +/K +-ATPase. Rabeprazole induces apoptosis. Rabeprazole acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole can be used for the research of gastric ulcerations and gastroesophageal reflux [3] .
2,3-Diphosphoglyceric acid-d3 ammonium (2,3-DPG-d3 ammonium) is the deuterium labeled 2,3-Diphosphoglyceric acid (HY-113050). 2,3-Diphosphoglyceric acid (2,3-DPG) is an intermediate of the glycolytic pathway. 2,3-Diphosphoglyceric acid stabilizes the deoxygenated form of hemoglobin by allosteric binding and facilitates oxygen release at tissue sites. 2, 3-diphosphoglyceric acid has antiparasitic activity. 2,3-Diphosphoglyceric acid can be used in the study of Alzheimer's disease (AD) [3] .
Ketoprofen- 13C,d3 is the 13C- and deuterium labeled Ketoprofen. Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC50s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively[1].
Telmisartan- 13C,d3 is the 13C- and deuterium labeled Telmisartan. Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
Hydrocinnamic acid-2,3- 13C2 is the 13C-labeled Hydrocinnamic acid. Hydrocinnamic acid is the major rhizospheric compound with known growth regulatory activities.
L-Histidine- 13C6, 15N3 (hydrochloride hydrate) is the 13C- and 15N-labeled L-Histidine hydrochloride hydrate. L-Histidine hydrochloride hydrate (H-His-OH.HCl.H2O) is an endogenous metabolite.
β-Alanine- 13C3, 15N is the 13C- and 15N-labeled β-Alanine. β-Alanine is a non-essential amino acid that is shown to be metabolized into carnosine, which functions as an intracellular buffer.
Sorafenib- 13C,d3 is the 13C- and deuterium labeled Sorafenib. Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator[1].
Regorafenib- 13C,d3 is the 13C- and deuterium labeled Regorafenib. Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.
Triclabendazole sulfoxide- 13C,d3 is the 13C- and deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP[1][2].
Apixaban- 13C,d3 is a deuterium and 13C labeled Apixaban. Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively[1].
(Rac)-Fosfomycin (benzylamine)- 13C3 is the 13C labeled Fosfomycin[1]. Fosfomycin (MK-0955) is a broad-spectrum antibiotic. Fosfomycin can cross blood-brain barrier penetrating, and irreversibly inhibits an early stage in cell wall synthesis. Fosfomycin shows anti-bacteria activity for a range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria[2][3].
L-Alanine- 13C3 is the 13C-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
Caffeic acid- 13C3 is an 13C labeled caffeic acid. Caffeic acid is a phytonutrient belonging to the flavonoids. Caffeic acid and its derivatives, are potential antimicrobial agents, chronic infection induced by microbes such as bacteria, fungi, and viruses[1].
Acetyl-L-carnitine-d3-1 (hydrochloride) is the deuterium labeled Acetyl-L-carnitine hydrochloride. Acetyl-L-carnitine hydrochloride is a blood-brain permeable acetyl ester of the amino acid L-carnitine found in the body. Acetyl-L-carnitine hydrochloride is often used as a dietary supplement, and exibits anti-stress-related psychiatric disorders[1].
Moxifloxacin- 13C,d3 hydrochloride (BAY 12-8039- 13C,d3) is 13C and deuterated labeled Moxifloxacin (HY-66011A). Moxifloxacin is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia.
O-Phospho-L-serine- 13C3, 15N is the 13C- and 15N-labeled O-Phospho-L-serine. O-Phospho-L-serine is the immediate precursor to L-serine in the serine synthesis pathway, and an agonist at the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8); O-Phospho-L-serine also acts as a weak antagonist for mGluR1 and a potent antagonist for mGluR2[1].
Dehydro Nifedipine-13C,d3 is a deuterated labeled Dehydro Nifedipine . Dehydro nifedipine (BAY-b 4759) is a metabolite of Nifedipine (HY-B0284). Nifedipine (BAY-a-1040) is a potent calcium channel blocker and an agent of choice for cardiac insufficiencies .
Levomefolic acid- 13C,d3 is the deuterium labeled Levomefolic acid (HY-14781) . Levomefolic acid (5-MTHF) is an orally active, brain-penetrant natural active form of folic acid and is one of the most widely used folic acid food supplements [3].
Epinastine- 13C,d3 (hydrobromide) is the 13C- and deuterium labeled Epinastine. Epinastine (WAL801) is an antihistamine and mast cell stabilizer. Epinastine is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine also inhibits IL-8 release and has an antiallergic action[1][2][3][4].
13C20, 15N10-Cyclic di-GMP ( 13C20, 15N10-c-di-GMP) is 13C and 15N labeled Cyclic-di-GMP (disodium). Cyclic-di-GMP disodium is a STING agonist and a bacterial second messenger that coordinates different aspects of bacterial growth and behavior, including motility, virulence, biofilm formation, and cell cycle progression. Cyclic-di-GMP disodium has anti-cancer cell proliferation activity and also induces elevated CD4 receptor expression and cell cycle arrest. Cyclic-di-GMP disodium can be used in cancer research [3] .
L-Alanine- 13C3, 15N,d4 is the deuterium, 13C-, and 15-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
Paroxetine EP impurity D-d4 (hydrochloride) is deuterium labeled (3R,4S)-3-((benzo[d][1,3]dioxol-5-yloxy)methyl)-4-(4-fluorophenyl)piperidine?(Paroxetine Impurity).
(3S,5R)-Fluvastatin-d6 (sodium) is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway[1].
3,3'-Diiodo-L-thyronine- 13C6 is the 13C labeled 3,3'-Diiodo-L-thyronine[1]. 3,3'-Diiodo-L-thyronine (3,3'-T2) is an endogenous metabolite of thyroid hormone. 3,3'-Diiodo-L-thyronine significantly enhances COX activity[2][3].
Zidovudine O-β-D-glucuronide-d3 (sodium) (3'-Azido-3'-deoxythymidine β-D-glucuronide-d3 (sodium)) is a deuterium labeled Zidovudine O-β-D-glucuronide (sodium) (HY-137522). Zidovudine O-β-D-glucuronide (3'-Azido-3'-deoxythymidine β-D-glucuronide) sodium is the major metabolite of Zidovudine. Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection [3].
Felbamate-d5 is the deuterium labeled Felbamate[1]. Felbamate (W-554) is a potent nonsedative anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA)[2][3].
Oxypurinol- 13C, 15N2 is 15N and 13C labeled Oxypurinol (HY-19657). Oxipurinol (Oxipurinol), the major active metabolite of Allopurinol, is an inhibitor of xanthine oxidase. Oxipurinol can be used to regulate blood urate levels and treat gout .
Zidovudine-d4 is deuterated labeled Zidovudine (HY-17413). Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection.
Pretomanid-d4 is the deuterium labeled Pretomanid. Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL[1][2].
Tolterodine-d14 (hydrochloride) is the deuterium labeled Tolterodine hydrochloride[1]. Tolterodine hydrochloride is a potent muscarinic receptor antagonist[2][3].
Pentoxifylline-d5 is the deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation[1][2][3].
Pirenzepine-d8 (LS 519-d8; Pirenzepin-d8) dihydrochloride is a deuterium labeled Pirenzepine (dihydrochloride) (HY-17037). Pirenzepine (LS 519) dihydrochloride is a selective M1 mAChR (muscarinic acetylcholine receptor) antagonist. Pirenzepine dihydrochloride reduces gastric acid secretion and reduces muscle spasm, can be used in peptic ulcers research. Pirenzepine dihydrochloride shows anti-proliferative activity to cancer cells [3].
N-Desmethylclozapine-d8 is the deuterium labeled N-Desmethylclozapine. N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist[1][2].
N-Desmethylclozapine-d8 (hydrochloride) is the deuterium labeled N-Desmethylclozapine hydrochloride. N-Desmethylclozapine hydrochloride is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine hydrochloride is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine hydrochloride is also a δ-opioid agonist[1][2][3].
Dulcite-d2 is the deuterium labeled Dulcite. Dulcite is a sugar alcohol with a slightly sweet taste which is a metabolic breakdown product of galact[1][2].
Pentoxifylline-d6 is the deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation[1][2][3].
Camptothecin-d5 is the deuterium labeled Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM[1]. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells[2][3].
Demethoxycurcumin-d4 is the deuterium labeled Demethoxycurcumin. Demethoxycurcumin (Curcumin II) is a major active curcuminoid; possess anti-inflammatory properties[1].
Tetradecyltrimethylammonium-d29 (bromide) is the deuterium labeled Tetradecyltrimethylammonium (bromide)[1]. Tetradecyltrimethylammonium bromide, an organic building block, is a cationic surfactant with asymmetrical structure[2][3].
Tetradecyltrimethylammonium-d38 (bromide) is the deuterium labeled Tetradecyltrimethylammonium (bromide)[1]. Tetradecyltrimethylammonium bromide, an organic building block, is a cationic surfactant with asymmetrical structure[2][3].
Moricizine-d8 (Hydrochloride) is the deuterium labeled Moricizine Hydrochloride (HY-B0615A). Moricizine Hydrochloride is an orally active Class I antiarrhythmic agent. Moricizine Hydrochloride decreases the maximum rate of phase 0 depolarization; increases rates of phase 2 and 3 repolarization, decreases action potential duration, and decreases effective refractory period[1][2].
Demethoxycurcumin-d7 is the deuterium labeled Demethoxycurcumin. Demethoxycurcumin(Curcumin II), a major active curcuminoid, possess anti-inflammatory properties; also exert cytotoxic effects in human cancer cells via induction of apoptosis.
Picropodophyllin-d6 (AXL1717-d6) is deuterium labeled Picropodophyllin. Picropodophyllin (AXL1717) is a selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 of 1 nM.
L-Lactic acid- 13C3 ((S)-2-hydroxypropanoic- 13C3) sodium (20% in water) is the 13C labeled L-Lactic acid. L-Lactic acid- 13C3 sodium (20% in water) can be used for lactate metabolism research .
Tiagabine-d5 (hydrochloride) is deuterium labeled Tiagabine (hydrochloride). Tiagabine hydrochloride is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [ 3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively .
Acetaminophen-d7 is the deuterium labeled Acetaminophen. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.
Alpha-Estradiol-d2 is the deuterium labeled Alpha-Estradiol. Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia[1].
D-Glucose-d4 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molec
Isoniazid-d4 is the deuterium labeled Isoniazid. Isoniazid (INH) is a proagent and must be activated by a bacterial catalase-peroxidase enzyme KatG. Isoniazid is bactericidal to rapidly dividing mycobacteria and has anti-tuberculostatic activity[1][2][3][4].
D-Glucose-d22 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
Squalene-d6 is a deuterium labeled Squalene. Squalene (Super Squalene) is an intermediate product in the synthesis of cholesterol, and shows several pharmacological properties such as hypolipidemic, hepatoprotective, antiatherosclerotic, cardioprotective, antioxidant, and antitumour activity .
Irinotecan-d10 is a deuterium labeled Irinotecan ((+)-Irinotecan). Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex[1].
Tucidinostat-d4 is the deuterium labeled Tucidinostat. Tucidinostat is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, respectively[1].
D-Glucose-d77 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
Acetaminophen-d4 is the deuterium labeled Acetaminophen. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent[1][2][3]. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor[4].
D-Glucose-d is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molec
Indocyanine green-d7 (Foxgreen-d7) is the deuterium labeled Indocyanine green (HY-D0711). Indocyanine green is a low toxicic fluorescent agent that has been widely used in medical diagnostics, such as determining cardiac output, hepatic function, and liver blood flow, and for ophthalmic angiography .
Tauroursodeoxycholate-d4 (sodium) is the deuterium labeled Tauroursodeoxycholate sodium. Tauroursodeoxycholate (Tauroursodeoxycholic acid; TUDCA) sodium is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
Vitamin D2-d6 is the deuterium labeled Vitamin D2. Vitamin D2 (Ergocalciferol), drived from plant sources or dietary supplements, could be used as supplement of Vitamin D[1][2].
Enclomiphene-d4 (hydrochloride) is a deuterium labeled Enclomiphene. Enclomiphene-d4 (hydrochloride) is a potent and orally active oestrogen receptor antagonist, with antioestrogenic property[1].
Sudan IV-d6 is the deuterium labeled Sudan IV(HY-D0932).Sudan IV is a lysochrome (fat-soluble dye) diazo dye used for the staining of lipids, triglycerides and lipoproteins on frozen paraffin sections .
Irinotecan-d5 hydrochloride is deuterated labeled Irinotecan hydrochloride (HY-16562A). Irinotecan hydrochloride ((+)-Irinotecan hydrochloride) is a topoisomerase I inhibitor mainly used to treat colon cancer and rectal cancer .
Tucatinib-d6 (Irbinitinib-d6) is deuterium labeled Tucatinib. Tucatinib (Irbinitinib) is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM .
Tauroursodeoxycholate-d4 is deuterium labeled Tauroursodeoxycholate. Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
Tiagabine-d4 hydrochloride is deuterated labeled Tiagabine hydrochloride (HY-B0696A). Tiagabine hydrochloride is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [ 3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively .
Umbelliferone-d5 is the deuterium labeled Umbelliferone. Umbelliferone (7-Hydroxycoumarin), a natural product of the coumarin family, is a fluorescing compound which can be used as a sunscreen agent.
Zoledronic acid-d5 is deuterated labeled Zoledronic Acid (HY-13777). Zoledronic Acid (Zoledronate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic Acid inhibits the differentiation and apoptosis of osteoclasts. Zoledronic Acid also has anti-cancer effects .
Cyclosporin A- 13C2,d4 (Cyclosporine A- 13C2,d4; Ciclosporin A- 13C2,d4) is a 13C labeled Cyclosporin A (HY-B0579) . Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM . Cyclosporin A also inhibits CD11a/CD18 adhesion [3].
D-Glucose- 13C2,d2 is the deuterium and 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical si
1,2-Dihydropyridazine-3,6-dione-3,4,5,6- 13C4 (1,2-Dihydro-3,6-pyridazine- 13C4-dione) is 13C labeled Maleic hydrazide. Maleic hydrazide is extensively used as a systemic plant growth regulator and as a herbicide. Maleic hydrazide acts as an inhibitor of the synthesis of nucleic acids and proteins .
5-Aminosalicylic acid-d7 (5-ASA-d7; Mesalamie-d7; Mesalazie-d7) is deuterium labeled 5-Aminosalicylic Acid. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB. 5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN) .
Dimethoxycurcumin-d6 is the deuterium labeled Dimethoxycurcumin (HY-100977). Dimethoxycurcumin is a derivative of Curcumin that has anti-inflammatory and antioxidant activities .
N,N-Dimethylglycine-d6 (Dimethylglycine-d6) hydrochloride is the deuterium labeled N,N-Dimethylglycine hydrochloride (HY-W001158). N,N-Dimethylglycine (Dimethylglycine) is a natural N-methylated glycine, is a nutrient supplement and acts as an NMDAR glycine site partial agonist. N,N-Dimethylglycine is a methyl donor, could improve immunity, function as an antioxidant to prevent oxidative stress, and scavenge excess of free radicals. N,N-Dimethylglycine exhibits antidepressant-like and surfactant effects [3] .
Cortodoxone-d2 is the deuterium labeled Cortodoxone. Cortodoxone is a glucocorticoid steroid hormone that can be oxygenated to cortisol (Hydrocortisone)[1].
Cetrimonium-d9 (bromide) is the deuterium labeled Cetrimonium bromide[1]. Cetrimonium bromide (CTAB) is an amine based cationic quaternary surfactant, is one of the components of the topical antiseptic Cetrimide.
Erlotinib-d6 (CP-358774 D6) is a deuterium labeled Erlotinib (CP-358774). Erlotinib is a directly acting inhibitor EGFR tyrosine kinase inhibitor with an IC50 of 2 nM for human EGFR[1]. Erlotinib-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Urethane-d5 is the deuterium labeled Urethane. Urethane (Ethyl carbamate), the ethyl ester of carbamic acid, is a byproduct of fermentation found in various food products. Urethane has the ability to suppress bacterial, protozoal, sea urchin egg, and plant tissue growth in vitro[1].
Alectinib-d6 is deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
Elvitegravir-d8 is deuterium labeled Elvitegravir. Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.
Cetrimonium-d33 (bromide) is the deuterium labeled Cetrimonium bromide[1]. Cetrimonium bromide (CTAB) is an amine based cationic quaternary surfactant, is one of the components of the topical antiseptic Cetrimide.
Phosphorylethanolamine-d4 (Monoaminoethyl phosphate-d4; NSC 254167-d4) is a deuterium labeled Phosphorylethanolamine (HY-N5034). Phosphorylethanolamine is an endogenous metabolite.
Elvitegravir-d6 (GS-9137-d6) is deuterium labeled Elvitegravir. Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively .
Vemurafenib-d7 is deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively[1][4]. Vemurafenib induces cell autophagy[5].
Telbivudine-d4 is deuterium labeled Telbivudine. Telbivudine (Epavudine), an orally active thymidine nucleoside analog, is a potent antiviral inhibitor of hepatitis B virus (HBV) replication[1].
Erlotinib-d6 (hydrochloride) a deuterium labeled Erlotinib Hydrochloride. Erlotinib Hydrochloride inhibits purified EGFR kinase with an IC50 of 2 nM[1]. Erlotinib-d6 (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Oleoylethanolamide-d2 is the deuterium labeled Oleoylethanolamide. Oleoylethanolamide is a high affinity endogenous PPAR-α agonist, which plays an important role in the treatment of obesity and arteriosclerosis.
Pirenzepine-d8 is the deuterium labeled Pirenzepine dihydrochloride. Pirenzepine dihydrochloride (LS519) is a selective M1 muscarinic receptor antagonist.
Cyclosporin A-d4 is the deuterium labeled Cyclosporin A. Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of calcineurin with an IC50 of 5 nM. Cyclosporin A also inhibits CD11a/CD18 ad
Bortezomib-d8 is the deuterium labeled Bortezomib. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity[1][2].
Miglustat-d9 is the deuterium labeled Miglustat. Miglustat (N-Butyldeoxynojirimycin) is an inhibitor of glucosylceramide synthase, primarily to treat Type I Gaucher disease (GD1) .
Oleoylethanolamide-d4 is the deuterium labeled Oleoylethanolamide. Oleoylethanolamide is a high affinity endogenous PPAR-α agonist, which plays an important role in the treatment of obesity and arteriosclerosis.
Venetoclax-d8 is deuterium labeled Venetoclax. Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy[1][2][3].
Delafloxacin-d5 is deuterium labeled Delafloxacin. Delafloxacin (RX-3341; WQ-3034; ABT492) is a broad-spectrum fluoroquinolone antibiotic. Delafloxacin has a broad spectrum of activity that includes drug-resistant Staphylococcus aureus, Streptococcus pneumoniae, and Klebsiella pneumonia[1].
Sonidegib-d4 is a isotope of Sonidegib. Sonidegib is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively .
Avatrombopag-d8 (hydrochloride) is deuterium labeled Avatrombopag (hydrochloride). Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A[1][2][3].
Curcumin-d6is a deuterium labeled Curcumin (Turmeric yellow). Curcumin (Turmeric yellow) is a natural phenolic compound with diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin is an inhibitor of p300 histone acetylatransferase (HATs) and also shows inhibitory effects on NF-κB and MAPKs.
Miglustat-d9 (hydrochloride) is the deuterium labeled Miglustat (hydrochloride). Miglustat hydrochloride is an inhibitor of glucosylceramide synthase, primarily to treat Type I Gaucher disease (GD1)[1][2].
Alectinib-d8 is the deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
Cephalexin-d5 is deuterium labeled Cephalexin. Cephalexin (Cefalexin; Cephacillin) is a potent, orally active and the first-generation cephalosporin antibiotic. Cephalexin kills gram-positive and some gram-negative bacteria by disrupting the growth of the bacterial cell wall. Cephalexin monohydrate is used for the research of pneumonia, strep throat, and bacterial endocarditis, et al[1].
Ligustrazine-d12 (Chuanxiongzine-d12) is deuterium labeled Ligustrazine. Ligustrazine (Chuanxiongzine), an alkylpyrazine isolated from Ligusticum chuanxiong Hort. (Chuan Xiong) , is present in french fries, bread, cooked meats, tea, cocoa, coffee, beer, spirits, peanuts, filberts, dairy products and soy products as fragrance and flavouring ingredienexhibits. Ligustrazine also has potential nootropic and anti-inflammatory activities in rats [3] .
Hordenine-d6 (Ordenina-d6) is the deuterium labeled Hordenine. Hordenine, an alkaloid found in plants, inhibits melanogenesis by suppression of cyclic adenosine monophosphate (cAMP) production .
Diacerein-d6 is the deuterium labeled Diacerein[1]. Diacerein (Diacerhein), a interleukin-1 beta inhibitor, is a slow-acting medicine of the class anthraquinone used to treat joint diseases[2].
Acyclovir-d4 is the deuterium labeled Acyclovir. Acyclovir (Aciclovir) is a guanosine analogue and an orally active antiviral agent. Acyclovir inhibits HSV-1 (IC50 of 0.85 μM), HSV-2 (IC50 of 0.86 μM) and varicella-zoster virus. Acyclovir can be phosphorylated by viral thymidine kinase (TK), and Acyclovir triphosphate interferes with viral DNA polymerization through competitive inhibition with guanosine triphosphate and obligatory chain termination[1][2][3]. Acyclovir prevents bacterial infections during induction therapy for acute leukaemia[4].
Guanidine-d5 (hydrochloride) is the deuterium labeled Guanidine hydrochloride[1]. Guanidine hydrochloride (Guanidinium chloride) a strong chaotrope, is also a strong denaturant of proteins[2][3].
Procyclidine-d5 (Tricyclamol-d5) is deuterium labeled Procyclidine (hydrochloride). Procyclidine (Tricyclamol, (±)-Procyclidine) hydrochloride , an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine hydrochloride can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy [3].
Hydroxyzine-d4 (dihydrochloride) is the deuterium labeled Hydroxyzine dihydrochloride. Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder[1][2].
Sulfamethazine-d4 is a deuterium labeled Sulfamethazine (Sulfadimidine). Sulfamethazine is an antimicrobial that is widely used to treat and prevent various animal diseases (such as gastrointestinal and respiratory tract infections)[1][2].
4-Acetyl-N-methylaniline-13C,d3 (1-(4-(Methylamino)phenyl)ethanone-13C,d3) is a 13C and deuterated isotope of 4-Acetyl-N-methylaniline. Compounds labeled with stable or radioactive isotopes can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
4-Aminobenzoic acid-d4 is the deuterium labeled 4-Aminobenzoic acid. 4-Aminobenzoic acid is an intermediate in the synthesis of folate by bacteria, plants, and fungi.
Roflumilast-d4 is the deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells[1][2].
2-Phenylethanol-d9 is the deuterium labeled 2-Phenylethanol[1]. 2-Phenylethanol (Phenethyl alcohol), extracted from rose, carnation, hyacinth, Aleppo pine, orange blossom and other organisms, is a colourless liquid. It has a pleasant floral odor and also an autoantibiotic produced by the fungus Candida albicans[2]. It is used as an additive in cigarettes and also used as a preservative in soaps due to its stability in basic conditions.
Butylparaben-d4 is the deuterium labeled Butylparaben. Butylparaben is an organic compound, has proven to be a highly successful antimicrobial preservative in cosmetics, also used in medication suspensions, and as a flavoring additive in food.
2-Phenylethanol-d5 is the deuterium labeled 2-Phenylethanol[1]. 2-Phenylethanol (Phenethyl alcohol), extracted from rose, carnation, hyacinth, Aleppo pine, orange blossom and other organisms, is a colourless liquid. It has a pleasant floral odor and also an autoantibiotic produced by the fungus Candida albicans[2]. It is used as an additive in cigarettes and also used as a preservative in soaps due to its stability in basic conditions.
2-Phenylethanol-d4 is the deuterium labeled 2-Phenylethanol[1]. 2-Phenylethanol (Phenethyl alcohol), extracted from rose, carnation, hyacinth, Aleppo pine, orange blossom and other organisms, is a colourless liquid. It has a pleasant floral odor and also an autoantibiotic produced by the fungus Candida albicans[2]. It is used as an additive in cigarettes and also used as a preservative in soaps due to its stability in basic conditions.
Toremifene-d6 (Z-Toremifene-d6) hydrochloride is deuterium labeled Toremifene. Toremifene is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively .
Phenylbutyrate-d11 (sodium) is deuterium labeled Sodium 4-phenylbutyrate. Sodium 4-phenylbutyrate (4-PBA sodium) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research[1].
D-erythro-Sphingosine-13C2,d2 is a deuterated labeled D-erythro-Sphingosine . D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator [3] .
L-Tryptophan- 15N2,d8 is the deuterium and 15N-labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3[1].
Cisapride-d6 (R51619-d6) is deuterium labeled Cisapride. Cisapride (R 51619) is an orally active 5-HT4 receptor agonist with an EC50 value of 140 nM. Cisapride is a hERG blocker with an IC50 value of 9.4 nM. Cisapride is a gastroprokinetic agent that stimulates gastrointestinal motor activity [3] .
L-Tryptophan-d8 is the deuterium labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3[1].
Rifampicin-d8 (Rifampin-d8) is the deuterium labeled Rifampicin. Rifampicin is a potent and broad spectrum antibiotic against bacterial pathogens. Rifampicin has anti-influenza virus activities.
Oxaprozin-d5 is deuterium labeled Oxaprozin. Oxaprozin is an inhibitor of both COX-1 and COX-2 with IC50s of 2.2 μM and 36 μM for human platelet COX-1 and IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin also inhibits the activation of NF-κB.
Thymidine-d4 is the deuterium labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[1][2][3].
Miltefosine-d4 (HePC-d4) is deuterium labeled Miltefosine. Miltefosine is a broad spectrum antimicrobial, anti-leishmanial, phospholipid agent acting by inhibiting the PI3K/Akt activity [3] . Miltefosine is an inhibitor of CTP-phosphocholine cytidyltransferase (CCT) .
Levamlodipine-d4 is the deuterium labeled Levamlodipine. Levamlodipine ((S)-Amlodipine) is a powerful dihydropyridine calcium channel blocker, possessing vasodilation properties and used in the treatment of hypertension and angina[1].
Norverapamil-d7 is a deuterium labeled Norverapamil ((±)-Norverapamil). Norverapamil, an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor[1][2].
Pitolisant-d5 hydrochloride (Ciproxidine-d5 hydrochloride) is the deuterium labeled Pitolisant hydrochloride (HY-12199B). Pitolisant hydrochloride is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM) .
Loratadine-d4 is the deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
Dexamethasone-d5 is the deuterium labeled Dexamethasone. Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses[1][2].
Adefovir-d4 is the deuterium labeled Adefovir. Adefovir (GS-0393) is an adenosine monophosphate analog antiviral agent that after intracellular conversion to Adefovir diphosphate inhibits HBV DNA polymerase. Adefovir has an IC50 of 0.7 μM against HBV in the HepG2.2.15 cell line. Adefovir has good antiviral activity against several viruses, including HBV and herpesviruses[1][2][3].
Bisdemethoxycurcumin-d8 is the deuterium labeled Bisdemethoxycurcumin. Bisdemethoxycurcumin(Curcumin III; Didemethoxycurcumin) is a natural derivative of curcumin with anti-inflammatory and anti-cancer activities.
Estrone-d2 is the deuterium labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells[1][2].
N-Nitrosodiethylamine-d4 is the deuterium labeled N-Nitrosodiethylamine[1]. N-Nitrosodiethylamine (Diethylnitrosamine) is a potent hepatocarcinogenic dialkylnitrosoamine. N-Nitrosodiethylamine is mainly present in tobacco smoke, water, cheddar cheese, cured, fried meals and many alcoholic beverages. N-Nitrosodiethylamine is responsible for the changes in the nuclear enzymes associated with DNA repair/replication. N-Nitrosodiethylamine results in various tumors in all animal species. The main target organs are the nasal cavity, trachea, lung, esophagus and liver.
Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].
Piperin-d10 is deuterium labeled Piperine. Piperine is an alkaloid, can be isolated from pepper. Piperine can inhibit the activity of P-glycoprotein and CYP3A4. Piperine inhibits HeLa cells with an IC50 of 61.94±0.054 μg/mL [3] .
Omadacycline-d9 (PTK 0796-d9; Amadacycline-d9) is the deuterium labeled Omadacycline (HY-14865) that can be used as the internal standard for the analysis of Omadacycline .
Thymidine-d2 is the deuterium labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[1
N-Nitrosodiethylamine-d10 is the deuterium labeled N-Nitrosodiethylamine[1]. N-Nitrosodiethylamine (Diethylnitrosamine) is a potent hepatocarcinogenic dialkylnitrosoamine. N-Nitrosodiethylamine is mainly present in tobacco smoke, water, cheddar cheese, cured, fried meals and many alcoholic beverages. N-Nitrosodiethylamine is responsible for the changes in the nuclear enzymes associated with DNA repair/replication. N-Nitrosodiethylamine results in various tumors in all animal species. The main target organs are the nasal cavity, trachea, lung, esophagus and liver.
Altrenogest-d5 is the deuterium labeled Altrenogest. Altrenogest (Allyltrenbolone) is a progestogen structurally related to veterinary steroid trenbolone.
Bambuterol-d9 (hydrochloride) is the deuterium labeled Bambuterol. Bambuterol ((±)-Bambuterol) hydrochloride is a long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma; it also is a prodrug of terbutaline.
Dexamethasone-d4 is deuterium labeled Dexamethasone. Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
Leriglitazone-d4 (MIN-102-d4; Hydroxypioglitazone-d4) is deuterium labeled Leriglitazone. Leriglitazone is an orally active and a BBB-penatrable PPARγ agonist with an EC50 of 9 μM. Leriglitazone, as a regulator of mitochondrial function, has neuroprotective, anti-inflammatory and antioxidant effects. Leriglitazone can be used in the study of neuroinflammatory and neurodegenerative diseases .
Sucralose-d6 is deuterium labeled Sucralose. Sucralose (E955; Trichlorosucrose) is a non-nutritive artificial sweetener and sugar substitute. Sucralose can activate a conserved neural fasting response and thereby exerts an appetite-stimulating effect in rodents[1][2].
Spermine-d20 (NSC 268508-d20) is deuterium labeled Spermine. Spermine (NSC 268508) functions directly as a free radical scabenger to protect DNA from free radical attack. Spermine has antiviral effects .
Sulfameter-d4 (Sulfametoxydiazine-d4; 5-Methoxysulfadiazine-d4) is the deuterium labeled Sulfameter (HY-B0213) . Sulfameter (Sulfametoxydiazine; 5-Methoxysulfadiazine) is an effective long-acting sulfonamide antibiotic with antibacterial activities. Sulfameter can be used for the research of urinary tract infections and lepriasis .
Mitoxantrone-d8 dihydrochloride is deuterated labeled Mitoxantrone dihydrochloride (HY-13502A). Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity [3] . Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively .
Rifampicin-d4 is the deuterium labeled Rifampicin. Rifampicin is a potent and broad spectrum antibiotic against bacterial pathogens. Rifampicin has anti-influenza virus activities.
Rifabutin-d7 is the deuterium labeled Rifabutin. Rifabutin (Ansamycin) is a semisynthetic ansamycin antibiotic with potent antimycobacterial properties. Rifabutin inhibits DNA-dependent RNA polymerase.
Exemestane-d2 is the deuterium labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research[1][2].
Rebamipide-d4 is deuterium labeled Rebamipide. Rebamipide is a mucoprotective agent. Rebamipide induces COX-2 expression, increases PGE2 levels, and enhances gastric mucosal defense in a COX-2-dependent manner[1].
Salbutamol-d9 (acetate) is the deuterium labeled Salbutamol[1]. Salbutamol is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease (COPD).
(±)-Penbutolol-d9 (hydrochloride) is a deuterium labeled (±)-Penbutolol hydrochloride. (+)-Penbutolol hydrochloride is a β-adrenoceptor antagonist, with an IC50 of 0.74 μM[1].
L-Tryptophan-d5 is the deuterium labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3[1].
Rifampicin-d11 (Rifampin-d11; Rifamycin AMP-d11) is the deuterium labeled Rifampicin (HY-B0272) . Rifampicin is a potent and broad spectrum antibiotic against bacterial pathogens. Rifampicin has anti-influenza virus activities. Rifampicin shows anti-orthopoxvirus activity .
Mecillinam-d12 is deuterium labeled Mecillinam. Mecillinam (Amdinocillin), the β-lactam antibiotic, has a broad spectrum of activity against gram-negative organisms[1].
Salbutamol-d9 is the deuterium labeled Salbutamol. Salbutamol is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease (COPD).
Guanosine-d13 (DL-Guanosine-d13) is a deuterium of Guanosine (HY-N0097). Guanosine (DL-Guanosine) is a purine nucleoside comprising guanine attached to a ribose (ribofuranose) ring via a β-N9-glycosidic bond. Guanosine possesses anti-HSV activity .
Norverapamil-d6 ((±)-Norverapamil-d6) hydrochloride is deuterium labeled Norverapamil (hydrochloride). Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor [3].
Nateglinide-d5 is a deuterium labeled Nateglinide. Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K+ channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus[1][2].
DL-Mevalonolactone-d7 is the deuterium labeled DL-Mevalonolactone. DL-Mevalonolactone ((±)-Mevalonolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone (Mevalonolactone) decreases mitochondrial membrane potential (∆Ψm), NAD(P)H content and the capacity to retain Ca2+ in the brain, besides inducing mitochondrial swelling[1][2].
Sulfabrom-d4 (N 3517-d4) is is the deuterium labeled Sulfabrom (HY-U00131). Sulfabrom is a long-acting Sulfonamide that is used for the treatment of coccidiosis and various bacterial infections in the poultry, swine and cattle .
Aspirin-d4 is the deuterium labeled Aspirin. Aspirin is a non-selective and irreversible inhibitor of COX-1 and COX-2 with IC50s of 5 and 210 μg/mL[1][2].
Ritonavir-d8 is deuterated labeled Ritonavir (HY-90001). Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.61 μM.
Estrone-d4 is the deuterium labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells[1][2].
Thymidine-d14 (DThyd-d14; NSC 21548-d14) is deuterium labeled Thymidine (HY-N1150). Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication.
Mitoxantrone-d8 (mitozantrone-d8) is the deuterium labeled Mitoxantrone. Mitoxantrone is a topoisomerase II inhibitor and also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM[1][2].
Ritonavir-d6 is the deuterium labeled Ritonavir. Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.61 μM[1][2].
Loratadine-d5 is the deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
Imidaprilate-d5 is deuterium labeled Imidaprilate. Imidaprilate is an active metabolite of TA-6366, acts as a potent angiotensin converting enzyme (ACE) inhibitor, with an IC50 of 2.6 nM, and is used in the research of hypertensive disease.
Nicotinamide-d4 is the deuterium labeled Nicotinamide. Nicotinamide is a form of vitamin B3 that plays essential roles in cell physiology through facilitating NAD+ redox homeostasis and providing NAD+ as a substrate to a class of enzymes that catalyze non-redox reactions. Nicotinamide is an inhibitor of SIRT1.
D-Alanine-d7 is the deuterium labeled D-Alanine. D-Alanine is a weak GlyR (inhibitory glycine receptor) and PMBA agonist, with an EC50 of 9 mM for GlyR.
Citicoline-d9 (Cytidine diphosphate-choline-d9) sodium is the deuterium labeled Citicoline sodium (HY-B0739A). Citicoline sodium is an endogenous intermediate in the synthesis of phosphatidylcholine which is a component of cell membranes. Citicoline sodium inhibits reactive oxygen species (ROS) and apoptosis. Citicoline sodium can be used for neurological disease and hearing loss study [3] .
Propylthiouracil-d5 is the deuterium labeled Propylthiouracil. Propylthiouracil (6-Propyl-2-thiouracil) is a thyroperoxidase and 5'-deiodinase inhibitor.
D-Alanine-d4 is the deuterium labeled D-Alanine. D-Alanine is a weak GlyR (inhibitory glycine receptor) and PMBA agonist, with an EC50 of 9 mM for GlyR.
Cabazitaxel-d6 is the deuterium labeled Cabazitaxel. Cabazitaxel is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity[1][2].
Cabazitaxel-d9 is deuterium labeled Cabazitaxel. Cabazitaxel is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity.
(-)-(S)-Cibenzoline-d4 (Escibenzoline-d4) is deuterium labeled (-)-(S)-Cibenzoline. (-)-(S)-Cibenzoline (Escibenzoline), a S(+)-enantiomer of Cibenzoline, is an antiarrhythmic agent .
Obeticholic acid-d5 is the deuterium labeled Obeticholic acid. Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy[1][2][3].
Clomipramine-d6 (hydrochloride) is the deuterium labeled Clomipramine hydrochloride. Clomipramine (Chlorimipramine) hydrochloride is a potent 5-HT reuptake blocker with the IC50 value of 1.5 nM. Clomipramine hydrochloride is a tricyclic antidepressant that can be used for the research of depression and obsessive compulsive disorder (OCD)[1].
D-Alanine-d is the deuterium labeled D-Alanine. D-Alanine is a weak GlyR (inhibitory glycine receptor) and PMBA agonist, with an EC50 of 9 mM for GlyR[1].
Raloxifene-d10-1 is the deuterium labeled Raloxifene[1]. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research[2].
Benzoin-d10 (DL-Benzoin-d10) is the deuterium labeled Benzoin (HY-B1550). Benzoin (DL-Benzoin), a natural balsamic resin, is a PI3Kα inhibitor with anticancer effects. Benzoin inihits the growth of colon cancer cell line (HCT-116). Benzoin can be used as a food additive .
Daclatasvir- 13C2,d6 (BMS-790052- 13C2,d6) is 13C and deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 μM and 3.27 μM, respectively [3] .
3-Hydroxykynurenine- 13C3, 15N (3-Hydroxy-DL-kynurenine- 13C3, 15N) is the 13C and 15N labeled 3-Hydroxykynurenine (HY-113294) . 3-Hydroxykynurenine, a metabolite of tryptophan, is a potential endogenous neurotoxin whose increased levels have been described in several neurodegenerative disorders. 3-Hydroxykynurenine induces neuronal apoptosis .
L-Alanine- 13C3, 15N is the 13C- and 15N-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
Estradiol-d2 is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway[1][2][3].
D-Glucose-d1-2 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
Retinoic acid-d6 is the deuterium labeled Retinoic acid[1]. Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha[2][3][4][5][6][7].
Estradiol-d5 is deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway[1][2][3].
Vincristine-d6 (sulfate) is the deuterium labeled Vincristine sulfate. Vincristine sulfate is an antitumor vinca alkaloid which inhibits microtubule formation in mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. It binds to microtubule with a Ki of 85 nM.
D-Glucose-d12-12 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
D-Glucose-d2-1 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling mol
Retinoic acid-d5 is the the deuterium labeled Retinoic acid (HY-14649). Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha [3] .
Doxifluridine-d2 is the deuterium labeled Doxifluridine[1]. Doxifluridine is a thymidine phosphorylase activator for PC9-DPE2 cells with IC50 of 0.62 μM.
Estradiol-d4 is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway[1][2][3].
D-Glucose-d-44 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
Tauroursodeoxycholate-d4-1 is the deuterium labeled Tauroursodeoxycholate. Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
D-Glucose-d2-2 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling mol
D-Glucose-d-11 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
Molnupiravir-d7 is the deuterium labeled Molnupiravir. Molnupiravir (EIDD-2801) is an orally bioavailable prodrug of the ribonucleoside analog EIDD-1931. Molnupiravir has broad spectrum antiviral activity against influenza virus and multiple coronaviruses, such as SARS-CoV-2, MERS-CoV, SARS-CoV. Molnupiravir has the potential for the research of COVID-19, and seasonal and pandemic influenza[1][2].
Adenosine-d13 (Adenine riboside-d13; D-Adenosine-d13) is deuterium labeled Adenosine (HY-B0228). Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation.
Dapivirine-d4 (TMC120-d4) is deuterium labeled Dapivirine. Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations [3].
Paquinimod-d5 is a deuterated analog of Paquinimod (HY-100442). Paquinimod (ABR 215757) is a specific and orally active inhibitor of S100A8/S100A9. Paquinimod rescues the pneumonia with substantial reduction of viral loads in SARS-CoV-2-infected mice [3].
Naftopidil-d5 is deuterium labeled Naftopidil. Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia[1][2].
(±)-Leucine-d10 is the deuterium labeled (±)-Leucine. (±)-Leucine (DL-Leucine), an isomer of Leucine, chemosterilant and dietary additive. (±)-Leucine inhibits growth of Escherichia coli HfrH by 92.08%[1].
Etoricoxib-d4 is a deuterium labeled Etoricoxib. Etoricoxib is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.
Vitamin K1-d4 is the deuterium labeled Vitamin K1. Vitamin K1 a naturally occurring vitamin required for blood coagulation and bone and vascular metabolism[1].
L-Carnitine-d9 (chloride)e is the deuterium labeled L-Carnitine chloride. L-Carnitine chloride, a highly polar, small zwitterion, is an essential co-factor for the mitochondrial β-oxidation pathway. L-Carnitine chloride functions to transport long chain fatty acyl-CoAs into the mitochondria for degradation by β-oxidation. L-Carnitine chloride is an antioxidant. L-Carnitine chloride can ameliorate metabolic imbalances in many inborn errors of metabolism[1][2][3].
Pantoprazole-d6 is deuterium labeled Pantoprazole. Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI)[1]. Pantoprazole, a substituted benzimidazole, is a potent H+/K+-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142)[3][4].
Amantadine-d15 is the deuterium labeled Amantadine. Amantadine (1-Adamantanamine) is an antiviral agent with activity against influenza A viruses. Amantadine blocks the proton flow through the M2 ion channel (M2 proton channel of influenza A) and thus prevents the release of viral RNA into the cytoplasm of the infected cells. Amantadine is an antiparkinsonian agent[1][2].
Dalbavancin-d6 is the deuterium labeled Dalbavancin[1]. Dalbavancin (MDL-63397) is a semisynthetic lipoglycopeptide antibiotic with potent bactericidal activity against Gram-positive bacteria. Dalbavancin inhibits Staphylococcus aureus and Bacillus anthracis with MIC90s of 0.06 μg/mL and 0.25 μg/mL, respectively[2][3].
Fosamprenavir-d4 is deuterium labeled Fosamprenavir. Fosamprenavir (Amprenavir phosphate;GW 433908) is a phosphate ester proagent of the antiretroviral protease inhibitor Amprenavir, with improved solubility[1]. Anti-HIV infection[1].
Lapatinib-d4 is the deuterium labeled Lapatinib (HY-50898). Lapatinib is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1][2].
Lapatinib-d5 is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1].
Lapatinib-d4 (GW572016-d4) tosylate is deuterium labeled Lapatinib (tosylate). Lapatinib (GW572016) tosylate is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively .
Tulathromycin A-d7 (Tulathromycin-d7) is deuterium labeled Tulathromycin A. Tulathromycin A (Tulathromycin), a macrolide antibiotic, inhibits protein synthesis (IC50=0.26 μM) by targeting bacterial ribosome. Tulathromycin A is used for the research of respiratory disease in cattle and swine. Immunomodulatory effects [3] .
Samidorphan-d4 is the deuterium labeled Samidorphan(HY-123689).Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo .
Etravirine-d4 is the deuterium labeled Etravirine. Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.
Molindone-d8 is the deuterium labeled Molindone. Molindone hydrochloride (EN-1733A) is a therapeutic antipsychotic, used in the treatment of schizophrenia, works by blocking the effects of dopamine in the brain, leading to diminished psychoses[1][2].
Dacomitinib-d10 is deuterium labeled Dacomitinib. Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively[1].
Atropine-d5 is the deuterium labeled Atropine (sulfate monohydrate). Atropine (Tropine tropate) sulfate monohydrate is a broad-spectrum and competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect[1].
Amantadine-d6 is the deuterium labeled Amantadine[1]. Amantadine (1-Adamantanamine) is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine also has anti-orthopoxvirus and anticancer activity. Amantadine can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research[2][3][4][5][6][7].
Daclatasvir-d6 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively[1][2][3].
(±)-Leucine-d7 is the deuterium labeled (±)-Leucine. (±)-Leucine (DL-Leucine), an isomer of Leucine, chemosterilant and dietary additive. (±)-Leucine inhibits growth of Escherichia coli HfrH by 92.08%[1].
Lifitegrast-d6 (SAR 1118-d6) is deuterium labeled Lifitegrast. Lifitegrast (SAR 1118) is a potent integrin antagonist. Lifitegrast blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. Lifitegrast can be used for researching dry eye disease .
Levodropropizine-d8 is deuterium labeled Levodropropizine. Levodropropizine (DF-526) is a histamine receptor inhibitor, Levodropropizine is an effective and very well tolerated peripheral antitussive agent.
Docosahexaenoic acid-d5 is the deuterium labeled Docosahexaenoic Acid. Docosahexaenoic Acid (DHA) is an omega-3 fatty acid abundantly present brain and retina. It can be obtained directly from fish oil and maternal milk.
Mavacamten-d6 (MYK461-d6; SAR439152-d6) is deuterium labeled Mavacamten (HY-109037). Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
Mifepristone-d6 is deuterated labeled Mifepristone (HY-13683). Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay .
D-Sorbitol-d4 is the deuterium labeled D-Sorbitol. D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and diet
Irbesartan-d7 is deuterated labeled Irbesartan (HY-B0202). Irbesartan (SR-47436) is an orally active Ang II type 1 (AT1) receptor blocker (ARB). Irbesartan can relax the blood vessels, low blood pressure and increase the supply of blood and oxygen to the heart. Irbesartan can be used for the research of high blood pressure, heart failure, and diabetic kidney disease .
Cobimetinib-d4 hydrochloride is deuterated labeled Cobimetinib (HY-13064). Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK1 inhibitor with an IC50 of 4.2 nM for MEK1.
Baloxavir-d4 (Baloxavir acid-d4; S-033447-d4) is the deuterium-labeled Baloxavir (HY-109025A). Baloxavir-d4 (Baloxavir-d4 acid), derived from the proagent Baloxavir-d4 marboxil, is a first-in-class, potent and selective cap-dependent endonuclease (CEN) inhibitor within the polymerase PA subunit of influenza A and B viruses. Baloxavir-d4 inhibits viral RNA transcription and replication and has potently antiviral activity .
Selexipag-d6 is deuterium labeled Selexipag. Selexipag (NS-304) is an orally available and potent agonist for the Prostacyclin (PGI2) receptor (IP receptor).
Navtemadlin-d7 is the deuterium labeled Navtemadlin. Navtemadlin (AMG 232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC50 of 0.6 nM. Navtemadlin binds to MDM2 with a Kd of 0.045 nM[1][2].
N-Benzylaniline-d2 (N-Phenylbenzylamine-d2) is the deuterium labeled N-Benzylaniline (HY-W016321). N-Benzylaniline is an N-alkyl-ated derivative of aniline .
Serotonin-d4 (5-Hydroxytryptamine-d4) hydrochloride is the deuterium labeled Serotonin (hydrochloride) (HY-B1473) . Serotonin (5-Hydroxytryptamine) hydrochloride is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin hydrochloride is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM .
Octacosane-d58 is the deuterium labeled Octacosane[1]. Octacosane is an endogenous metabolite with antibacterial activity. Octacosane shows high cytotoxicity against murine melanoma B16F10-Nex2 cells besides inducing protection against a grafted subcutaneous melanoma. Octacosane has the larvicidal activity against mosquito Culex quinquefasciatus with the LC50 concentration of 7.2 mg/l[2][3][4].
Fexofenadine-d10 (hydrochloride) is deuterium labeled Fexofenadine (hydrochloride). Fexofenadine hydrochloride (MDL-16455 hydrochloride), a H1R antagonist, is an anti-allergic agent used in seasonal allergic rhinitis and chronic idiopathic urticarial (person aged ≥16 years)[1].
D-Sorbitol-d2 is the deuterium labeled D-Sorbitol. D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and diet
Pergolide-d7 (mesylate) is the deuterium labeled Pergolide mesylate. Pergolide mesylate (Pergolide methanesulfonate), an Ergoline derivative, is a potent and orally active dopamine D1 and D2 receptors agonist. Pergolide mesylate can be used for Parkinson's disease and hyperprolactinaemia research[1][2].
Procainamide-d4 hydrochloride is deuterated labeled Procainamide. Procainamide hydrochloride is an antiarrhythmic agent used in the study of cardiac arrhythmias.
Secnidazole-d6 is the deuterium labeled Secnidazole. Secnidazole (RP-14539;PM-185184) is an orally active azole antibiotic with a longer half-life than metronidazole (HY-B0318). Secnidazole is against the vaginosis-associated bacteria and has the potential for bacterial vaginosis research[1].
Entinostat-d4 is the deuterium labeled Entinostat[1]. Entinostat is an oral and selective class I HDAC inhibitor, with IC50s of 243 nM, 453 nM, and 248 nM for HDAC1, HDAC2, and HDAC3, respectively[2].
Ondansetron-d6 (hydrochloride) is the deuterium labeled Ondansetron hydrochloride[1]. Ondansetron hydrochloride is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy[2][3][4][5][6][7].
Lornoxicam-d4 is the deuterium labeled Lornoxicam. Lornoxicam (Chlortenoxicam), a COX-1 and COX-2 inhibitor, is a new nonsteroidal anti-inflammatory agent (NSAID).
Chlorambucil-d8 is the deuterium labeled Chlorambucil. Chlorambucil (CB-1348), an orally active antineoplastic agent, is a bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease[1][2][3][4].
Olaparib-d5 (AZD2281-d5) is the deuterium labeled Olaparib (HY-10162). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator [3] .
Entecavir-d2 is the deuterium labeled Entecavir. Entecavir (SQ 34676; BMS 200475) is a potent and selective inhibitor of HBV, with an EC50 of 3.75 nM in HepG2 cell.
D-Sorbitol-d8 is the deuterium labeled D-Sorbitol. D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and dietary supplement[1].
Boceprevir-d9 is the deuterium labeled Boceprevir. Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a Ki of 14 nM in both enzyme assay and an EC90 of 350 nM in cell-based replicon assay[1][2][3][4][5]. Boceprevir inhibits SARS-CoV-2 3CLpro activity[6].
Dehydroaripiprazole-d8 is deuterium labeled Dehydroaripiprazole. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole[1][2][3].
Adenosine-d9 is the deuterium labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physio .
Penciclovir-d4 is the deuterium labeled Penciclovir. Penciclovir is reported to be potent against HSV types 1 and 2 with IC50 of 0.04-1.8 μg/mL and 0.06-4.4 μg/mL, respectively[1][2].
Tasimelteon-d5 is the deuterium labeled Tasimelteon. Tasimelteon (BMS-214778) is an orally active and selective dual melatonin receptor agonist (DMRA). Tasimelteon has 2.1-4.4 times greater affinity for the MT2 receptor than for the MT1 receptor. Tasimelteon is a circadian regulator and has the potential for Non-24-Hour Sleep-Wake Disorder (Non-24)[1][2].
Lifitegrast-d4 (SAR 1118-d4) is deuterium labeled Lifitegrast. Lifitegrast (SAR 1118) is a potent integrin antagonist. Lifitegrast blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. Lifitegrast can be used for researching dry eye disease .
Cysteamine-d4 (hydrochloride) is the deuterium labeled Cysteamine hydrochloride. Cysteamine hydrochloride (2-Aminoethanethiol hydrochloride) is an orally active agent for the treatment of nephropathic cystinosis and an antioxidant.
Cabozantinib-d6 is the deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively[1][2][3].
Samidorphan-d5 (ALKS-33-d5) is is a deuterated compound of Samidorphan. Samidorphan is an orally active opioid system modulator that binds with high affinity to μ-opioid, κ-opioid, and δ-opioid receptors. Samidorphan is a μ-opioid receptor antagonist and a partial agonist at k-opioid and δ-opioid receptors. Samidorphan acts primarily as an opioid receptor antagonist in vivo [3] .
Adenosine-d2 is the deuterium labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physio
Isavuconazole-d4 is a deuterium labeled Isavuconazole (BAL-4815). Isavuconazole is a triazole proagent with antifungal activity against yeasts, molds, and dimorphic fungi[1].
Fluralaner-d5 (A1443-d5) is deuterium labeled Fluralaner. Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels .
Glycochenodeoxycholic acid-d7 (sodium) is the deuterium labeled Glycochenodeoxycholic acid (sodium salt). Glycochenodeoxycholic acid sodium salt (Chenodeoxycholylglycine sodium salt) is a bile acid formed in the liver from chenodeoxycholate and glycine. It acts as a detergent to solubilize fats for absorption and is itself absorbed. Glycochenodeoxycholic acid sodium salt (Chenodeoxycholylglycine sodium salt) induces hepatocyte apoptosis[1][2].
Mirtazapine-d4 is deuterium labeled Mirtazapine. Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively[1][2].
Lapatinib-d7 (dihydrochloride) is the deuterium labeled Lapatinib dihydrochloride. Lapatinib (GW572016) dihydrochloride is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1].
Dacomitinib-d10 (dihydrochloride) is the deuterium labeled Dacomitinib dihydrochloride. Dacomitinib (PF-00299804) dihydrochloride is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively[1].
Cephalexin-d5 (monohydrate) is the deuterium labeled Cephalexin monohydrate. Cephalexin monohydrate is a potent, orally active and the first-generation cephalosporin antibiotic. Cephalexin monohydrate kills gram-positive and some gram-negative bacteria by disrupting the growth of the bacterial cell wall. Cephalexin monohydrate is used for the research of pneumonia, strep throat, and bacterial endocarditis, et al[1].
Tivozanib-d6 (AV-951-d6) is deuterium labeled Tivozanib. Tivozanib (AV-951; KRN951) is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib exhibits antitumor efficacy .
Defactinib-d6 is a deuterium labeled Defactinib (HY-12289). Defactinib is a novel FAK inhibitor with potential antiangiogenic and antineoplastic activities .
Midostaurin-d5 is a deuterium labeled Midostaurin. Midostaurin is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM[1].
Palmitoylethanolamide-d4 is the deuterium labeled Palmitoylethanolamide. Palmitoylethanolamide (Palmidrol) is an active endogenous compound which can used for preventing virus infection of the respiratory tract.
Actinine-d9 chloride is the deuterium labeled Actinine chloride. Actinine chloride is angiopathic substance produced as an intermediary metabolite by gut microbiota that feed on carnitine in dietary red meat[1][2].
6-Mercaptopurine-d2 is the deuterium labeled 6-Mercaptopurine. 6-Mercaptopurine is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive agent[1][2].
Cyclamic acid-d11 (Sodium cyclamate-d11) sodiumis deuterium labeled Cyclamic acid (sodium). Cyclamic acid sodium (Sodium cyclamate) is a commonly used sweetener. Cyclamic acid sodium is toxic to osteoblasts and can inhibit cell proliferation, induce apoptosis and reduce cell mineralization. Cyclamic acid sodium causes focal necrosis of bladder organs in rats in vitro, which can promote bladder cancer, but some studies have shown that low doses of Cyclamic acid sodium have no carcinogenic effect. In addition, Cyclamic acid sodium has no effect on insulin and glucagon secretion induced by arginine [3] .
Undecanoic acid-d2 is the deuterium labeled Undecanoic acid. Undecanoic acid (Undecanoate) is a monocarboxylic acid with antimycotic property, which inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum[1].
Mavacamten-d1 (MYK461-d1; SAR439152-d1) is deuterium labeled Mavacamten (HY-109037). Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
Ambrisentan-d10 (BSF 208075-d10; LU 208075-d10) is the deuterium labled Ambrisentan (HY-13209). Ambrisentan is a selective ET type A receptor (ETAR) antagonist.
Gestodene-d6is the deuterium labeled Gestodene. Gestodene(SHB 331) is a progestogen hormonal contraceptive[1][2]. Gestodene-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Lubiprostone-d7 (RU-0211-d7) is the deuterium labeled Lubiprostone. Lubiprostone (RU0211) is a gastrointestinal agent used for the treatment of idiopathic chronic constipation[1][2].
Tegoprazan (CJ-12420; RQ-00000004), a potassium-competitive acid blocker, is a reversible, oral active and highly selective inhibitor of gastric H+/K+-ATPase that could control gastric acid secretion and motility, with IC50 values ranging from 0.29-0.52 μM for porcine, canine, and human H +/K +-ATPases in vitro. Tegoprazan significantly improves colitis in mice and enhances the intestinal epithelial barrier function. Tegoprazan is promising for research of Inflammatory bowel, gastric acid-related, motilityimpaired diseases [3].
Duloxetine-d7 hydrochloride ((S)-Duloxetine-d7 hydrochloride) is the deuterium labeled Duloxetine hydrochloride (HY-B0161A). Duloxetine hydrochloride ((S)-Duloxetine hydrochloride) is a serotonin-norepinephrine reuptake inhibitor (SNRI) with a Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD) .
Glimepiride-d4-1 is deuterium labeled Glimepiride. Glimepiride (Glimperide) is a medium-to-long acting sulfonylurea anti-diabetic compound with an ED50 of 182 μg/kg.
Darolutamide-d4 (ODM-201-d4) is deuterium labeled Darolutamide. Darolutamide (ODM-201;BAY-1841788) is a potent androgen receptor (AR) antagonist with an IC50 of 26 nM in in vitro assay .
Resveratrol-d4 is the deuterium labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].
Resiquimod-d5 is deuterium labeled Resiquimod. Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α .
Caspofungin-d4 (acetate) is the deuterium labeled Caspofungin diacetate[1]. Caspofungin (MK-0991) diacetate is a potent antifungal agent. Caspofungin diacetate inhibits the synthesis of the fungal cell wall component β-(l,3)-D-glucan[2][3].
Citronellol-d6 is deuterated labeled Linalool (HY-N0368). Linalool is a natural monoterpene which is a competitive NMDA receptor antagonist. Linalool is orally active and crosses the blood-brain barrier. Linalool has anticancer, antibacterial, anti-inflammatory, neuroprotective, anxiolytic, antidepressant, anti-stress, cardioprotective, hepatoprotective, nephroprotective and pulmonary protective activities [3] .
Ondansetron-d5 is the deuterium labeled Ondansetron. Ondansetron (GR 38032; SN 307) is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy.
Fusidic acid-d6 is the deuterium labeled Fusidic acid. Fusidic acid (Fusidate) a bacteriostatic antibiotic produced from the Fusidium coccineum fungus, belongs to the class of steroids. Fusidic acid has no corticosteroid effects. Fusidic acid inhibits the growth of bacteria by preventing the release of translation elongation factor G (EF-G) from the ribosome[1][2].
L-Serine-d2 is the deuterium labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
Sparsentan-d5 is deuterium labeled Sparsentan. Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively[1].
Irbesartan-d7 hydrochloride is deuterated labeled Irbesartan hydrochloride (HY-B0202A). Irbesartan (SR-47436) hydrochloride is an orally active Ang II type 1 (AT1) receptor blocker (ARB). Irbesartan hydrochloride can relax the blood vessels, low blood pressure and increase the supply of blood and oxygen to the heart. Irbesartan hydrochloride can be used for the research of high blood pressure, heart failure, and diabetic kidney disease .
Pregnanediol-d5 is the deuterium labeled Pregnanediol. Pregnanediol is the major metabolite of progesterone and can be excreted via urine. Pregnanediol offers an indirect way to measure progesterone levels in vivo[1].
Crisaborole-d4 is deuterium labeled Crisaborole. Crisaborole (AN-2728) is a potent inhibitor of PDE4 and cytokine release; inhibit PDE4 with an IC50 of 0.49 μM.
(-)-Epigallocatechin Gallate-d4 (EGCG-d4) is the deuterium labeled (-)-Epigallocatechin Gallate (HY-13653). (-)-Epigallocatechin Gallate (EGCG) is a major polyphenol in green tea, which can inhibit cell proliferation and induce cell apoptosis. (-)-Epigallocatechin Gallate inhibits glutamate dehydrogenase 1/2 (GDH1/2, GLUD1/2) activity. (-)-Epigallocatechin Gallate has a potent anticancer, antioxidant and anti-inflammatory properties against various types of cancers such as colorectal cancer, myeloid leukemia, thyroid carcinoma [3] .
Sparfloxacin-d5 is deuterium labeled Sparfloxacin (HY-B0308). Sparfloxacin is a fluoroquinolone antibiotic, shows broad and potent antibacterial activity .
Everolimus-d4 is the deuterium labeled Everolimus. Everolimus (RAD001) is a Rapamycin derivative and a potent, selective and orally active mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities[1][2].
Olaparib-d8 (AZD2281-d8) is the deuterium labeled Olaparib (HY-10162). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator [3] .
Baricitinib-d5 is the deuterium labeled Baricitinib. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
Barnidipine-d5 (hydrochloride) is the deuterium labeled Barnidipine hydrochloride. Barnidipine hydrochloride (Mepirodipine hydrochloride) is an L-type calcium antagonist (CaA) with high affinity for [3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors[1].Barnidipine hydrochloride (Mepirodipine hydrochloride) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action[2].
Fedratinib-d9 (TG-101348-d9) is deuterium labeled Fedratinib. Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research [3].
Verapamil-d6 (CP-16533-1-d6) hydrochloride is the deuterium labled Verapamil (hydrochloride) (HY-A0064). Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research [3].
Phenylephrine-d6 (hydrochloride) is deuterium labeled Phenylephrine (hydrochloride). (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
Secnidazole-d4 is the deuterium labeled Secnidazole[1]. Secnidazole (RP-14539) is an orally active azole antibiotic and a imidazole mitigator of Serratia marcescens virulence. Secnidazole, as an analog of acylhomoserine lactones, effectively inhibits QS resulting in the attenuation of Pseudomonas aeruginosa pathogenesis. Secnidazole has antimicrobial activity against many anaerobic Gram-negative and Gram-positive bacterial species in vitro. Secnidazole can be used for the research of various diseases, such as amoebiasis and giardiasis, and bacterial vaginitis[1][2][3].
Lomitapide-d8 is deuterium labeled Lomitapide. Lomitapide (AEGR-733; BMS-201038) is a potent inhibitor of microsomal triglyceride-transfer protein (MTP) with an IC50 of 8 nM in vitro.
Pyridoxine-d5 (hydrochloride) is the deuterium labeled Pyridoxine hydrochloride[1]. Pyridoxine hydrochloride (Pyridoxol;Vitamin B6) is a pyridine derivative. Pyridoxine (Pyridoxol;Vitamin B6) exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway[2].
Verapamil-d7 is the deuterium labeled Verapamil (HY-14275). Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research [3].
Serotonin-d4 is deuterium labeled Serotonin. Serotonin is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM.
Albendazole sulfoxide-d7 is the deuterium labeled Albendazole sulfoxide. Albendazole sulfoxide (Ricobendazole), the main active metabolite of Albendazole, exhibits anti-parasite effect against Echinococcus multilocularis Metacestodes[1].
Ranolazine-d8 (dihydrochloride) is the deuterium labeled Ranolazine dihydrochloride. Ranolazine dihydrochloride (CVT 303 dihydrochloride) is an anti-angina agent that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine dihydrochloride is also a partial fatty acid oxidation inhibitor[3].
Undecanoic acid-d21 is the deuterium labeled Undecanoic acid. Undecanoic acid (Undecanoate) is a monocarboxylic acid with antimycotic property, which inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum[1].
Caspofungin-d4 (MK-0991-d4; L-743872-d4) is a deuterium labeled Caspofungin (HY-17006A). Caspofungin is a potent antifungal agent. Caspofungin inhibits the synthesis of the fungal cell wall component β-(l,3)-D-glucan [3].
L-Serine-d7 is the deuterium labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
Cabozantinib-d4 is deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
Dapivirine-d11 is the deuterium labeled Dapivirine. Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations[1][2].
L-Carnitine-d9 is the deuterium labeled L-Carnitine. L-Carnitine (Levocarnitine) is an endogenous molecule involved in fatty acid metabolism, biosynthesized within the human body using amino acids: L-lysine and L-methionine, as substrates. L-Carnitine functions to transport long chain fatty acyl-CoAs into the mitochondria for degradation by β-oxidation. L-carnitine can ameliorate metabolic imbalances in many inborn errors of metabolism[1][2].
Daclatasvir-d16 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively[1][2][3].
Mavacamten-d5 (MYK461-d5; SAR439152-d5) is deuterium labeled Mavacamten (HY-109037). Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
Verlukast-d6 is a deuterium labeled Verlukast. Verlukast is a potent, selective, and orally active antagonist of leukotriene receptor. Verlukast has the potential for the research of asthma[1].
Volinanserin-d4 (hydrochloride) is the deuterium labeled Volinanserin hydrochlorid. Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity[1][2].
Baloxavir-d5 is deuterium labeled Baloxavir. Baloxavir (Baloxavir acid), derived from the proagent Baloxavir marboxil, is a first-in-class, potent and selective cap-dependent endonuclease (CEN) inhibitor within the polymerase PA subunit of influenza A and B viruses. Baloxavir inhibits viral RNA transcription and replication and has potently antiviral activity[1][2].
Methionine-d4 is the deuterium labeled Methionine. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
Ribavirin- 15N, d2 is 15N and deuterated labeled Ribavirin (HY-B0434). Ribavirin (ICN-1229) is an antiviral agent against a broad spectrum of viruses including HCV, HIVl, and RSV. Ribavirin also has anti-orthopoxvirus and anti-variola activities.
Metaxalone-d6 is deuterium labeled Metaxalone. Metaxalone (AHR438; NSC170959) is an FDA-approved muscle relaxant. Metaxalone acts mainly on the central nervous system and achieves muscle relaxation by inhibiting polysynaptic reflex arcs. In addition, Metaxalone is an inhibitor of MAO-A, which has anti-inflammatory and antioxidant effects. Metaxalone inhibits IL-1β-induced inflammatory phenotype, modulates NF-κB and other related signaling pathways, and decreases MAO-A expression and activity in IL-1β-treated microglia [3].
Cyclosporin A acetate-d4 (Cyclosporine A acetate-d4; Ciclosporin A acetate-d4) is a deuterium labeled Cyclosporin A (HY-B0579) . Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM . Cyclosporin A also inhibits CD11a/CD18 adhesion [3].
Maribavir-d6 (1263W94-d6) is a deuterium labeled Maribavir (HY-16305). Maribavir is a potent inhibitor of histone phosphorylation catalyzed by wild-type pUL97 in vitro, with an IC50 of 3 nM .
D-erythro-Sphingosine-d7 is the deuterium labeled D-erythro-Sphingosine. D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator[1][2][3][4].
Ibudilast-d7-1 is the deuterium labeled Ibudilast[1]. Ibudilast (KC-404;AV-411;MN-166) is a cyclic AMP phosphodiesterase (PDE) inhibitor. Ibudilast has platelet anti-aggregatory effects. Ibudilast can be used for the research of asthma for its inhibitory effects on tracheal smooth muscle contractility. Ibudilast may be a useful neuroprotective and anti-dementia agent counteracting neurotoxicity in activated microglia[2].
Glutathione oxidized- 13C4, 15N2 is the 13C and 15N labeled Glutathione oxidized (HY-D0844). Glutathione oxidized is produced by the oxidation of glutathione. Detoxification of reactive oxygen species is accompanied by production of glutathione oxidized. Glutathione oxidized can be used for the research of sickle cells and erythrocytes .
Estradiol-d2-1 is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway[1][2][3][4].
Dabrafenib-d9 is the deuterium labeled Dabrafenib. Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively[4].
Ethynyl Estradiol-d4 is the deuterium labeled Ethynyl Estradiol. Ethynyl Estradiol (17α-Ethynylestradiol;Ethynylestradiol) is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills. Ethynyl Estradiol-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Propylparaben-d4 is the deuterium labeled Propylparaben[1]. Propylparaben (Propyl parahydroxybenzoate) is an antimicrobial preservative which can be produced naturally by plants and bacteria. Propylparaben is prevalently used in cosmetics, pharmaceuticals, and foods. Propylparaben disrupts antral follicle growth and steroidogenic function by altering the cell-cycle, apoptosis, and steroidogenesis pathways. Propylparaben also decreases sperm number and motile activity in rats[2][3][4].
Ethyl linoleate-d2 (Linoleic Acid ethyl ester-d2; Mandenol-d2) is the deuterium labeled Ethyl linoleate (HY-W013812). Ethyl linoleate (Linoleic Acid ethyl ester) inhibit the development of atherosclerotic lesions and the expression of inflammatory mediators .
Imatinib-d4 is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity[1][2].
Labetalol-d6 hydrochloride (AH5158-d6 hydrochloride; Sch-15719W-d6) is a deuterium labeled Labetalol (HY-121383). Labetalol is an orally active α1- and β-adrenergic receptors competitive antagonist, which exhibits anti-hypertensive property .
Flibanserin-d4 is a deuterium labeled Flibanserin (BIMT-17). Flibanserin is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM)[1].
Prostaglandin E1-d9 is deuterium labeled Prostaglandin E1.Prostaglandin E1 is a prostanoid receptor ligand, with Kis of 1.1 nM, 2.1 nM, 10 nM, 33 nM and 36 nM for mouse EP3, EP4, EP2, IP and EP1, respectively. Prostaglandin E1 induces vasodilation and inh
Licarbazepine-d4 is the deuterium labeled Licarbazepine (HY-108506). Licarbazepine is a voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects[1][2].
Tamsulosin-d4 (hydrochloride) is deuterium labeled Tamsulosin (hydrochloride). Tamsulosin hydrochloride ((R)-(-)-YM12617) is an inhibitor of α1-adrenergic receptor. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth in animal models[1].
Vildagliptin-d7 is deuterium labeled Vildagliptin. Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity[1].
Ethyl linoleate-d11 (Linoleic Acid ethyl ester-d11) is deuterium labeled Ethyl linoleate. Ethyl linoleate (Linoleic Acid ethyl ester) inhibit the development of atherosclerotic lesions and the expression of inflammatory mediators .
i-Inositol-d6 is the deuterium labeled i-Inositol. i-Inositol is a chemical compound, associated lipids are found in many foods, in particular fruit, especially cantaloupe and oranges.
Thiamine-d4 (hydrochloride) is deuterium labeled Thiamine (hydrochloride). Thiamine hydrochloride (Thiamine chloride hydrochloride) is an essential micronutrient needed as a cofactor for many central metabolic enzymes.
Fosaprepitant-d4 (dimeglumine) is deuterium labeled Fosaprepitant (dimeglumine). Fosaprepitant dimeglumine (MK-0517) is a proagent of Aprepitant (HY-10052). Fosaprepitant dimeglumine is a neurokinin-1 receptor antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV)[1].
Nefazodone-d6 (hydrochloride) is the deuterium labeled Nefazodone hydrochloride. Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity[1][2].
Prostaglandin E2-d9 is the deuterium labeled Prostaglandin E2. Prostaglandin E2 (PGE2) is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation[1][2].
Phenylacetylglutamine-d5 (NSC 203800-d5) is the deuterium labeled Phenylacetylglutamine (HY-W050026). Phenylacetylglutamine is a colonic microbial metabolite from amino acid fermentation .
Deoxycholic acid-d6 is the deuterium labeled Deoxycholic acid. Deoxycholic acid is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.
Panobinostat-d4 is the deuterium labeled Panobinostat. Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities[1][2]. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells[4]. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma[3].
Panobinostat-d4 (hydrochloride) is deuterium labeled Panobinostat. Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities[1][2]. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells[4]. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma[3].
Ethylparaben-d5 (Ethyl parahydroxybenzoate-d5) is deuterium labeled Ethylparaben. Ethylparaben is the ethyl ester of paraben and is used as an antifungal preservative and food additive .
Enrofloxacin-d5 is the deuterium labeled Enrofloxacin. Enrofloxacin (BAY Vp 2674) is an effective antibiotic with an MIC90 of 0.312 μg/mL for Mycoplasma bovis.
Dapsone-d4 is the deuterium labeled Dapsone. Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities[1]. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al[2][3].
Valproic acid-d15 is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches[1][2].
Nefazodone-d6 (dihydrochloride) is deuterium labeled Nefazodone (hydrochloride). Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity[1][2].
Ranolazine-d5 is the deuterium labeled Ranolazine. Ranolazine (CVT 303) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor[3]. Antianginal agent.
Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC50 values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice [3] .
Valproic acid-d4 is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches[1][2].
Tamsulosin-d5 (hydrochloride) is the deuterium labeled Tamsulosin hydrochloride. Tamsulosin hydrochloride ((R)-(-)-YM12617) is an inhibitor of α1-adrenergic receptor. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth in animal models[1].
N-Acetylglycine-d2 (Aceturic acid-d2) is the deuterated labeled N-Acetylglycine (HY-Y0069). N-Acetylglycine (Aceturic acid) is a minor constituent of numerous foods. N-Acetylglycine is a flavor enhancer which elicits Monosodium glutamate (MSG)-like sensory experiencesN-Acetylglycine .
Imatinib-d8 is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity[1][2].
Chloroxylenol-d6 is the deuterium labeled Chloroxylenol. Chloroxylenol is a broad spectrum antimicrobial chemical compound used to control bacteria, algae, fungi and virus.
Adenine-d is the deuterium labeled Adenine. Adenine (6-Aminopurine), a purine, is one of the four nucleobases in the nucleic acid of DNA. Adenine acts as a chemical component of DNA and RNA. Adenine also plays an important role in biochemistry involved in cellular respiration, the form of both ATP and the cofactors (NAD and FAD), and protein synthesis[1][2][3].
Taurocholic acid-d8 (sodium) is deuterium labeled Taurocholic acid (sodium). Taurocholic acid sodium (Sodium taurocholate) has marked bioactive effects such as an inhibitory potential against hepatic artery ligation induced biliary damage by upregulation of VEGF-A expression. Taurocholic acid sodium has immunoregulation effect .
Mycophenolate Mofetil-d4 hydrochloride is deuterated labeled Mycophenolate mofetil hydrochloride (HY-B0199A). Mycophenolate mofetil (RS 61443) hydrochloride is a immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPD) type I/II with IC50s of 39 nM and 27 nM, respectively.
Ebastine-d6 is deuterated labeled Ebastine (HY-B0674). Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research .
Valproic acid-d6 is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches[1][2].
Clopidogrel carboxylic acid-d4 is a deuterated derivative of Clopidogrel carboxylic acid, which is an inactive metabolite of the antiplatelet agent Clopidogrel (HY-15283) in plasma. Clopidogrel carboxylic acid-d4 can be used to further explore the metabolic characteristics of Clopidogrel .
N-Acetylglycine-d5 (Aceturic acid-d5) is the deuterium labeled N-Acetylglycine (HY-Y0069). N-Acetylglycine (Aceturic acid) is a minor constituent of numerous foods. N-Acetylglycine is a flavor enhancer which elicits Monosodium glutamate (MSG)-like sensory experiencesN-Acetylglycine .
Theophylline-d6 is the deuterium labeled Theophylline. Theophylline is a nonselective phosphodiesterase (PDE) inhibitor, adenosine receptor blocker, and histone deacetylase (HDAC) activator.
Enrofloxacin-d5 (hydrochloride) is deuterium labeled Enrofloxacin (monohydrochloride). Enrofloxacin monohydrochloride (BAY Vp 2674 monohydrochloride) is an effective antibiotic with an MIC90 of 0.312 μg/mL for Mycoplasma bovis.
Valproic acid-d4 (sodium) is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
Prostaglandin E2-d4 is the deuterium labeled Prostaglandin E2. Prostaglandin E2 (PGE2) is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation[1][2].
Paroxetine-d4 (hydrochloride) is deuterium labeled Paroxetine (hydrochloride). Paroxetine hydrochloride is a potent selective serotonin-reuptake inhibitor, commonly prescribed as an and has GRK2 inhibitory ability with IC50 of 14 μM. Paroxetine hydrochloride can be used for the research of depressive disorder[1][2][3].
Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice [3].
Dapsone-d8 is a deuterium labeled Dapsone. Dapsone is an orally active and blood-brain penetrant sulfonamide antibiotic with antibacterial, antigenic and anti-inflammatory activities[1]. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone can be used as an anticonvulsant and also in the research of skin and glioblastoma diseases[2][3][4][5].
N-Desmethylolanzapine-d8 hydrochloride (N-Demethylolanzapine-d8 hydrochloride) is the deuterium labeled N-Desmethylolanzapine (HY-W009247). N-Desmethylolanzapine is an antipsychotic drug. The formation of N-Desmethylolanzapine correlates with the level and activity of human liver flavin-containing monooxygenase (FMO3). N-Desmethylolanzapine can be used in the study of antipsychotic drugs .
Propylparaben-d7 (Propyl parahydroxybenzoate-d7) is the deuterium labeled Propylparaben (HY-N2026) . Propylparaben (Propyl parahydroxybenzoate) is an antimicrobial preservative which can be produced naturally by plants and bacteria. Propylparaben is prevalently used in cosmetics, pharmaceuticals, and foods. Propylparaben disrupts antral follicle growth and steroidogenic function by altering the cell-cycle, apoptosis, and steroidogenesis pathways. Propylparaben also decreases sperm number and motile activity in rats [3] .
Sofosbuvir-d6 is the deuterium labeled Sofosbuvir. Sofosbuvir (PSI-7977) is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.
N-Acetyl-S-(3-hydroxypropyl-1-methyl)-L-cysteine-d3 (MethylN-acetyl-S-(3-hydroxypropyl)-L-cysteinate-d3) is the deuterium labeled N-Acetyl-S-(3-hydroxypropyl-1-methyl)-L-cysteine.
Toremifene-d6 is deuterium labeled Toremifene. Toremifene (Z-Toremifene) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively[1][2].
NAD+-d4 is the deuterium-labeled NAD+ (HY-B0445). NAD+-d4 is a coenzyme composed of ribosylnicotinamide 5'-diphosphate coupled to adenosine 5'-phosphate by pyrophosphate linkage.
sn-Glycero-3-phosphocholine-d9 is the deuterium labeled sn-Glycero-3-phosphocholine. sn-Glycero-3-phosphocholine (Choline Alfoscerate) is a precursor in the biosynthesis of brain phospholipids and increases the bioavailability of choline in nervous tissue. sn-Glycero-3-phosphocholine (Choline Alfoscerate) has significant effects on cognitive function with a good safety profile and tolerability, and is effective in the treatment of Alzheimer's disease and dementia[1][2].
Pimelic acid-d4 is the deuterium labeled Pimelic acid[1]. Pimelic acid is the organic compound and its derivatives are involved in the biosynthesis of the amino acid called lysine.
Thymidine- 13C10, 15N2 is the 13C and 15N labeled Thymidine[1]. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[2][3][4].
(±)-1,2-Propanediol-d2 is the deuterium labeled (±)-1,2-Propanediol. (±)-1,2-Propanediol (1,2-(RS)-Propanediol) is an aliphatic alcohol and frequently used as an excipient in many agent formulations to increase the solubility and stability of agents .
(±)-1,2-Propanediol-d8 is the deuterium labeled (±)-1,2-Propanediol. (±)-1,2-Propanediol (1,2-(RS)-Propanediol) is an aliphatic alcohol and frequently used as an excipient in many agent formulations to increase the solubility and stability of agents .
Menaquinone-7-d7 is the deuterium labeled Menaquinone-7. Menaquinone-7 (Vitamin K2-7), belongs to a class of K2-vitamin homologs, is originally discovered as the anti-hemorrhagic factors[1]. Menaquinone-7 (Vitamin K2-7) is identified as the most bioactive cofactor for the carboxylation reaction of Gla-proteins [2]. Supplementation with Menaquinone-7 (Vitamin K2-7) is a pharmacological option for activating matrix Gla protein and intervening in the progression of calcific aortic valve stenosis (CAVS)[3].
6-Aminocaproic acid-d6 is deuterium labeled 6-Aminocaproic acid. 6-Aminocaproic acid (EACA), a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders[1][2].
6-Aminocaproic acid-d10 is the deuterium labeled 6-Aminocaproic acid. 6-Aminocaproic acid (EACA), a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders[1][2].
(±)-1,2-Propanediol-d6 is the deuterium labeled (±)-1,2-Propanediol. (±)-1,2-Propanediol (1,2-(RS)-Propanediol) is an aliphatic alcohol and frequently used as an excipient in many agent formulations to increase the solubility and stability of agents .
Coenzyme Q10-d9 is the deuterium labeled Coenzyme Q10. Coenzyme Q10 is an essential cofactor of the electron transport chain and a potent antioxidant agent.
Higenamine-d4-1 (Norcoclaurine-d4-1) hydrochloride is deuterium labeled Higenamine (hydrochloride). Higenamine hydrochloride is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine (Norcoclaurine) can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine hydrochloride protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine hydrochloride can be used to study cancer, inflammation, cardiorenal syndrome and other diseases [3] .
4-Phenylbutyric acid-d2 is the deuterium labeled 4-Phenylbutyric acid[1]. 4-Phenylbutyric acid (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.
Diethyltoluamide-d7 is the deuterium labeled Diethyltoluamide[1]. Diethyltoluamide is the most common active ingredient in insect repellents. It is intended to provide protection against mosquitoes, ticks, fleas, chiggers, leeches, and many other biting insects[2].
Barnidipine-d5 is the deuterium-labeled Barnidipine (HY-107322A). Barnidipine-d5 (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors . Barnidipine-d5 (Mepirodipine) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action .
Estrone-d2-1 is the deuterium labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells[1][2].
L-Ascorbic acid-d2 is the deuterium labeled L-Ascorbic acid. L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a colla
Triacetin-d5 is the deuterium labeled Triacetin. Triacetin is an artificial chemical compound, is the triester of glycerol and acetic acid, and is the second simplest fat after triformin.
Dorzolamide-d5(hydrochloride) (L671152 hydrochloride-d5) is deuterium labeled Dorzolamide (hydrochloride). Dorzolamide (L671152) hydrochloride is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity .
L-5-Hydroxytryptophan-d4 (L-5-HTP-d4; Oxitriptan-d4) is a deuterium labeled L-5-Hydroxytryptophan (HY-B1716). L-5-Hydroxytryptophan (L-5-HTP), a naturally occurring amino acid and a dietary supplement for use as an antidepressant, appetite suppressant, and sleep aid, is the immediate precursor of the neurotransmitter serotonin and a reserpine antagonist . L-5-Hydroxytryptophan (L-5-HTP) is used to treat fibromyalgia, myoclonus, migraine, and cerebellar ataxia [3] .
N-Desmethyl Sildenafil-d8 is the deuterium labeled N-Desmethyl Sildenafil (HY-117605). N-Desmethyl Sildenafil is a major metabolite of Sildenafil. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor[1][2][3].
Levocarnitine propionate-d5 (hydrochloride) is the deuterium labeled Levocarnitine propionate hydrochloride. Levocarnitine propionate hydrochloride (L-Propionylcarnitine chloride; ST-261) is used to treat the deterioration of renal function, congestive heart failure, intermittent claudication, and other diseases.
Retinyl acetate-d4 is the deuterium labeled Retinyl acetate[1]. Retinyl acetate is a synthetic acetate ester form derived from retinol and has potential antineoplastic and chemo preventive activities[2].
Levulinic acid-d5 is the deuterium labeled Levulinic acid[1]. Levulinic acid is a precursor for the synthesis of biofuels, such as ethyl levulinate[2].
rel-Ritonavir-d6 (rel-ABT 538-d6; rel-RTV-d6) is the deuterium labeled Ritonavir (HY-90001). Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.61 μM .
Loratadine-d4-1 (Loratidine-d4-1) is deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators .
Glyceryl Triacetate-d9 is the deuterium labeled Triacetin[1]. Triacetin is an artificial chemical compound, is the triester of glycerol and acetic acid, and is the second simplest fat after triformin.
Folic acid-d4 is the deuterium labeled Folic acid. Folic acid (Vitamin M; Vitamin B9) is a B vitamin; is necessary for the production and maintenance of new cells, for DNA synthesis and RNA synthesis.
2-Methoxyestradiol-d5 is the deuterium labeled 2-Hydroxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa[1][2][3][4][5][6][7].
4-Phenylbutyric acid-d11 is the deuterium labeled 4-Phenylbutyric acid. 4-Phenylbutyric acid (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.
4-Phenylbutyric acid-d5 is the deuterium labeled 4-Phenylbutyric acid[1]. 4-Phenylbutyric acid (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research[2][3][4].
17α-Hydroxyprogesterone-d8 is the deuterium labeled 17α-Hydroxyprogesterone. 17α-Hydroxyprogesterone (17-Hydroxyprogesterone) is an endogenous progestogen as well as chemical intermediate in the biosynthesis of other steroid hormones, including the corticosteroids and the androgens and the estrogens.
Folic acid-d2 (Vitamin B9-d2) is the deuterium labeled Folic acid. Folic acid (Vitamin M; Vitamin B9) is a B vitamin; is necessary for the production and maintenance of new cells, for DNA synthesis and RNA synthesis.
N,N'-Dinitrosopiperazine-d8 is the deuterium labeled N,N'-Dinitrosopiperazine[1]. N,N'-Dinitrosopiperazine (1,4-Dinitrosopiperazine;DNP) is a carcinogen with specificity for nasopharyngeal epithelium and facilitates NPC metastasis. N,N'-Dinitrosopiperazine regulates multiple signaling pathways through protein phosphorylation, including LYRIC at serine 568[2].
Pitavastatin-d4 (hemicalcium) is deuterium labeled Pitavastatin (Calcium). Pitavastatin Calcium (NK-104 hemicalcium) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin Calcium (NK-104 hemicalcium) inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin Calcium is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Anti-cancer activity[1][2][3].
Tetrabenazine-d7 (TBZ-d7-d7) is deuterium labeled Tetrabenazine. Tetrabenazine (Ro 1-9569) is a reversible inhibitor of the vesicular monoamine transporter VMAT2 with the Kd value of 1.34 nM. Tetrabenazine can be used for research on diseases related to hyperactive movement disorders such as Huntington's disease [3] .
Diethyltoluamide-d10 is the deuterium labeled Diethyltoluamide[1]. Diethyltoluamide is the most common active ingredient in insect repellents. It is intended to provide protection against mosquitoes, ticks, fleas, chiggers, leeches, and many other biting insects[2].
Mitotane-d8 is the deuterium labeled Mitotane[1]. Mitotane (2,4′-DDD), an isomer of DDD and derivative of dichlorodiphenyltrichloroethane (DDT), is an antineoplastic agent, can be used to research adrenocortical carcinoma. Mitotane exert its adrenocorticolytic effect at least in part through lipotoxicity induced by intracellular free cholesterol (FC) accumulation. Mitotane can have direct pituitary effects on corticotroph cells. Mitotane can induce CYP3A4 gene expression via steroid and xenobiotic receptor (SXR) activation, and has agent-agent interactions[2][3][4][5].
Coenzyme Q10-d6 is deuterium labeled Coenzyme Q10. Coenzyme Q10 is an essential cofactor of the electron transport chain and a potent antioxidant agent.
Pyridoxine-d2 (hydrochloride) is the deuterium labeled Pyridoxine hydrochloride. Pyridoxine hydrochloride is a pyridine derivative. Pyridoxine (Pyridoxol; Vitamin B6) exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
Ganciclovir-d5 is the deuterium labeled Ganciclovir. Ganciclovir (BW 759), a nucleoside analogue, is an orally active antiviral agent with activity against CMV. Ganciclovir also has activity in vitro against members of the herpes group and some other DNA viruses. Ganciclovir inhibits the in vitro replication of human herpes viruses (HSV 1 and 2, CMV) and adenovirus serotypes 1, 2, 4, 6, 8, 10, 19, 22 and 28. Ganciclovir has an IC50 of 5.2 μM for feline herpesvirus type-1 (FHV-1)[1][2][3].
(R)-Hydroxytolterodine-d14 is deuterated labeled Desfesoterodine (HY-76569). Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) [3]. Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
Dexamethasone-d5-1 is deuterium labeled Dexamethasone. Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
L-Tryptophan- 13C11, 15N2 is the 13C- and 15N-labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3[1].
5'-Guanylic acid- 15N5,d12 (5'-GMP- 15N5,d12 dilithium; 5'-guanosine monophosphate- 15N5,d12) dilithium is deuterium and 15N labeled 5'-Guanylic acid (HY-N5134). 5'-Guanylic acid (5'-GMP) is involved in several metabolic disorders, including the AICA-ribosiduria pathway, adenosine deaminase deficiency, adenine phosphoribosyltransferase deficiency (aprt), and the 2-hydroxyglutric aciduria pathway.
Guanosine- 13C10, 15N5 is the 13C and 15N labeled Guanosine (HY-N0097). Guanosine (DL-Guanosine) is a purine nucleoside comprising guanine attached to a ribose (ribofuranose) ring via a β-N9-glycosidic bond. Guanosine possesses anti-HSV activity .
α-Lipoic Acid-d5 is the deuterium labeled α-Lipoic Acid. α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation[1][2][3]. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells[4].
Secnidazole- 13C2, 15N2 is the 13C2, 15N2 labeled Secnidazole. Secnidazole (RP-14539;PM-185184) is an orally active azole antibiotic with a longer half-life than metronidazole (HY-B0318). Secnidazole is against the vaginosis-associated bacteria and has the potential for bacterial vaginosis research.
p-Anisic acid-d4 is the deuterium labeled p-Anisic acid[1]. p-Anisic acid (4-Methoxybenzoic acid) is one of the isomers of anisic acid, with anti-bacterial and antiseptic properties[2].
Acetyl-L-carnitine-d9 (O-Acetyl-L-carnitine-d9) is deuterium labeled Acetyl-L-carnitine. Acetyl-L-carnitine (O-Acetyl-L-carnitine) is a compound involved in human metabolic research. It has relevant applications in predicting metabolite biomarker changes using the Recon 2 metabolic reconstruction model and integrating and analyzing multiple data types, but its specific activity mechanism is not described in detail based on the existing information [3].
Lapatinib-d4-1 is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1].
D-Sorbitol-d-2 is the deuterium labeled D-Sorbitol. D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and di
Dinoprost-d4 is the deuterium labeled Dinoprost. Dinoprost (Prostaglandin F2α) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost plays a key role in the onset and progression of labour[1][2].
Dinoprost-d9 is the deuterium labeled Dinoprost. Dinoprost (Prostaglandin F2α) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost plays a key role in the onset and progression of labour[1][2].
N-(3-Indolylacetyl)-L-alanine-d4 (Indoleacetylalanine-d4) is the deuterium labeled N-(3-Indolylacetyl)-L-alanine (HY-W141858). N-(3-Indolylacetyl)-L-alanine is an indoleacetylamino acid. N-(3-Indolylacetyl)-L-alanine appears to increase callus growth and reduces the ability of growths to differentiate into shoots of Phalaenopsis orchids .
Levomilnacipran-d10 ((1S,2R)-Milnacipran-d10) hydrochloride is deuterium labeled Levomilnacipran. Levomilnacipran (F2696; (1R,2S)-milnacipran), an enantiomer of milnacipran, is a selective serotonin and norepinephrine (5-HT/NE) reuptake inhibitor. Levomilnacipran also is a human alpha-adrenergic receptor antagonist, with an IC50 of 3.4 μM. (patent WO2013014263A1) .
Atomoxetine-d5 (hydrochloride) is the deuterium labeled Atomoxetine hydrochloride. Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5, 77 and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively)[1][2].
Paquinimod-d5-1 is a deuterated analog of Paquinimod (HY-100442). Paquinimod (ABR 215757) is a specific and orally active inhibitor of S100A8/S100A9. Paquinimod rescues the pneumonia with substantial reduction of viral loads in SARS-CoV-2-infected mice [3].
Norgestimate metabolite norelgestromin-d6 is the deuterium labeled Norgestimate metabolite norelgestromin. Norelgestromin is a metabolite of Norgestimate, which is a progestin or synthetic progestogen. Norgestimate metabolite norelgestromin-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
D-Sorbitol-d2-2 is the deuterium labeled D-Sorbitol. D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and di
D-(+)-Trehalose-d2 is the deuterium labeled D-(+)-Trehalose. D-(+)-Trehalose, isolated from Saccharomyces cerevisiae, can be used as a food ingredient and pharmaceutical excipi[1][2].
D-Sorbitol-d2-1 is the deuterium labeled D-Sorbitol. D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and di
(S)-Timolol-d9 (maleate) is deuterium labeled (S)-Timolol (Maleate). (S)-Timolol Maleate (L-714,465 Maleate) is a non-cardioselective hydrophilic β-adrenoceptor blocker. (S)-Timolol Maleate is widely used as standard medication for intraocular pressure (glaucoma) by preventing the production of aqueous humor. (S)-Timolol Maleate can be used for hypertension, angina pectoris and myocardial infarction[1][2][3].
L-Norleucine-d9 is the deuterium labeled L-Norleucine. L-Norleucine ((S)-2-Aminohexanoic acid) is an isomer of leucine, specifically affects protein synthesis in skeletal muscle, and has antivirus activity.
Meta-Fexofenadine-d6 is the deuterium labeled meta-Fexofenadine. meta-Fexofenadine (meta-MDL-16455) is an impurity of Fexofenadine[1]. Fexofenadine, a H1R antagonist, is an anti-allergic agent used in seasonal allergic rhinitis and chronic idiopathic urticarial[2].
Olaparib-d4-1 (AZD2281-d4-1) is the deuterium labeled Olaparib (HY-10162). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator [3] .
β-Nicotinamide mononucleotide-d4 is the deuterium labeled β-Nicotinamide mononucleotide. β-nicotinamide mononucleotide (β-NM) is a product of the nicotinamide phosphoribosyltransferase (NAMPT) reaction and a key NAD+ intermediate. The pharmacological activities of β-nicotinamide mononucleotide include its role in cellular biochemical functions, cardioprotection, diabetes, Alzheimer's disease, and complications associated with obesity[1].
Safinamide-d4-1 is deuterium labeled Safinamide. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM)[1]. Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al[2][3].
Alfacalcidol-d7 is the deuterium labeled Alfacalcidol. Alfacalcidol (1-hydroxycholecalciferol) is a vitamin D active metabolites, acts as a non-selective VDR activator medication, and widely be used in the management of osteoporosis[1][2][3][4].
D-(+)-Trehalose-d14 is the deuterium labeled D-(+)-Trehalose. D-(+)-Trehalose, isolated from Saccharomyces cerevisiae, can be used as a food ingredient and pharmaceutical excipi[1][2].
Escitalopram-d4 (oxalate) is deuterium labeled Escitalopram (oxalate). Escitalopram ((S)-Citalopram) oxalate, the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram oxalate has ∼30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram oxalate is an antidepressant for the research of major depression[1][2].
Cortisone-d2 is the deuterium labeled Cortisone. Cortisone (17-Hydroxy-11-dehydrocorticosterone), an oxidized metabolite of Cortisol (a Glucocorticoid). Cortisone acts as an immunosuppressant and anti-inflammatory agent. Cortisone can partially intervene in binding of Glucocorticoid to Glucocorticoid-receptor at high concentrations[1][3][4][5].
Palmitoylethanolamide-d5 (Palmidol-d5, PEA-15,15,16,16,16-d5) is deuterium labeled Palmitoylethanolamide. Palmitoylethanolamide (Palmidrol) is an active endogenous compound which can used for preventing virus infection of the respiratory tract .
Chlorambucil-d8-1 is the deuterium labeled Chlorambucil. Chlorambucil (CB-1348), an orally active antineoplastic agent, is a bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease[1][2][3][4].
13-Methyltetradecanoic acid-d6 is a deuterated labeled 13-Methyltetradecanoic acid . 13-Methyltetradecanoic acid (13-MTD), a saturated branched-chain fatty acid with potent anticancer effects. 13-Methyltetradecanoic acid induces apoptosis in many types of human cancer cells [3].
C6 Ceramide-d11 is deuterated labeled C6 Ceramide (HY-19542). C6-ceramide, a ceramide pathway activator, shows activity against a variety of cancer cell lines. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects .
Chlophedianol- 13C6 is the 13C labeled Chlophedianol (HY-A0161). Chlophedianol is an orally active and potent antitussive agent. Chlophedianol can be used for the research of acute cough due to upper respiratory tract infections (URIs)[1][2][3].
2-Deoxy-D-glucose-d is the deuterium labeled 2-Deoxy-D-glucose. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase[1][2].
Clascoterone-d5 (Cortexolone 17 alpha-propionate-d5) is the deuterated analog of Clascoterone. Clascoterone is a topical and peripheral androgen antagonist [3].
Clascoterone-d6 (Cortexolone 17 alpha-propionate-d6) is deuterium labeled Clascoterone. Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist .
Maribavir-d6 TFA (1263W94-d6 TFA; BW1263W94-d6 TFA; GW257406X-d6 TFA) is a deuterium labeled Maribavir (HY-16305). Maribavir is an orally active antiviral agent for cytomegalovirus (CMV) through inhibition of protein kinase UL97 and the following CMV DNA replication .
L-Asparagine- 15N2 (monohydrate) is the 15N-labeled L-Asparagine. L-Asparagine ((-)-Asparagine) is a non-essential amino acid that is involved in the metabolic control of cell functions in nerve and brain tissue.
L-Asparagine- 13C4 (monohydrate) is the 13C-labeled L-Asparagine. L-Asparagine ((-)-Asparagine) is a non-essential amino acid that is involved in the metabolic control of cell functions in nerve and brain tissue.
Adenine- 13C5,15C5 (6-Aminopurine- 13C5,15C5; Vitamin B4- 13C5,15C5) is 13C-labeled Adenine (HY-B0152). Adenine (6-Aminopurine), a purine, is one of the four nucleobases in the nucleic acid of DNA. Adenine acts as a chemical component of DNA and RNA. Adenine also plays an important role in biochemistry involved in cellular respiration, the form of both ATP and the cofactors (NAD and FAD), and protein synthesis.
Riboflavin- 13C4, 15N2is the 13C-labeled and 15N-labeled Riboflavin. Riboflavin is an easily absorbed micronutrient with a key role in maintaining health in humans and other animals.
L-Arginine- 13C6, 15N4,d7 (hydrochloride) is the deuterium, 13C-, and 15-labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
D-Glucose- 13C2 is the 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
5-Azacytidine- 15N4 is 13C and 15N labeled 5-Azacytidine. 5-Azacytidine (Azacitidine; 5-AzaC; Ladakamycin) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation. 5-Azacytidine is incorporated into DNA to covalently trap DNA methyltransferases and contributes to reverse epigenetic changes. 5-Azacytidine induces cell autophagy[3] .
Epeleuton-d5 (15(S)-HEPE-d5ethyl ester) is deuterium labeled Epeleuton. Epeleuton is a second-generation synthetic N-3 fatty acid derivative with activity in patients with non-alcoholic fatty liver disease, although it did not reach the primary endpoints of alanine aminotransferase and liver stiffness, but it can significantly reduce triglycerides, glycated hemoglobin, plasma glucose and inflammatory markers .
Acetaminophen-13C6 (Paracetamol-13C6) is the 13C-labeled Acetaminophen. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent [3]. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor .
Aliskiren-d6 (hemifumarate) is a deuterium labeled Aliskiren hemifumarate. Aliskiren hemifumarate is a direct and orally active renin inhibitor with an IC50 of 1.5 nM[1][2].
Efavirenz- 13C6 is the 13C-labeled Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture[1].
α-Hydroxyglutaric acid-d4 (disodium) is the deuterium labeled α-Hydroxyglutaric acid disodium[1]. α-Hydroxyglutaric acid (2-Hydroxyglutarate) disodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid disodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases[2].
D-Glucose- 13C6 is a stable isotope-labeled counterpart of D-glucose (HY-B0389). D-Glucose- 13C6 can be used as a metabolic tracer to trace glucose-related synthetic catabolism or as synthesis ingredient, minimal media reagent, and internal standard [3].
DCVC- 13C3, 15N is 15N and 13C labeled DCVC. DCVC (S-[(1E)-1,2-Dichloroethenyl]-L-cysteine) is a bioactive metabolite of trichloroethylene (TCE). DCVC inhibits pathogen-stimulated pro-inflammatory cytokines IL-1β, IL-8, and TNF-α release from tissue cultures .
Tazarotene-13C2,d2 (AGN 190168-13C2,d2) is the 13C and deuterium labeled isotope of Tazarotene (HY-15388). Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris. Tazarotene is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups .
Acotiamide-d6 is a deuterium labeled Acotiamide. Acotiamide is an orally active and first-in-class gastroprokinetic agent for the treatment of functional dyspepsia[1][2].
Nitroxoline-d4 is the deuterium labeled Nitroxoline. Nitroxoline is an antibiotic that has proven to be very effective at combating biofilm infections. Nitroxoline functions by chelating Fe2+ and Zn2+ ions from the biofilm matrix[1][2].
p,p'-DDE-d8 is the deuterium labeled p,p'-DDE[1]. p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent androgen receptor antagonist, with an IC50 of 5 μM and a Ki of 3.5 μM[2].
Valproic acid-d4-1 is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches[1][2].
Rufinamide-d2 (CGP 33101-d2) is the deuterium labeled Rufinamide. Rufinamide (E 2080) is a new antiepileptic agent that differs structurally from other antiepileptic drugs and is approved as adjunctive therapy for Lennox-Gastaut syndrome (LGS).
(Rac)-5-Hydroxymethyl Tolterodine-d14 is the deuterium labeled (Rac)-5-Hydroxymethyl Tolterodine. (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research[1].
Lipoic acid-d4 ((R)-(+)-α-Lipoic acid-d4) is deuterium labeled Lipoic acid. Lipoic acid ((R)-(+)-α-Lipoic acid) is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. (R)-(+)-α-Lipoic acid is more effective than racemic Lipoic acid .
Enrofloxacin-d5 (hydriodide) is the deuterium labeled Enrofloxacin (monohydrochloride). Enrofloxacin monohydrochloride (BAY Vp 2674 monohydrochloride) is an effective antibiotic with an MIC90 of 0.312 μg/mL for Mycoplasma bovis.
Flibanserin-d4-1 is deuterium labeled Flibanserin. Flibanserin (BIMT-17) is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM). Flibanserin binds to dopamine D4 receptors (4-24 nM), and has negligible affinity for a variety of other neurotransmitter receptors and ion channels. Flibanserin is efficacious in treating hypoactive sexual desire disorder (HSDD)[1][2].
Uridine triphosphate-d13 (UTP-d13 dilithium; Uridine 5'-triphosphate-d13) dilithium is deuterium labeled Uridine triphosphate (HY-107372). Uridine triphosphate (UTP;Uridine 5'-triphosphate) is a nucleotide that regulates the functions of the pancreas in endocrine and exocrine secretion, proliferation, channels, transporters, and intracellular signaling under normal and disease states.
Treprostinil- 13C2,d is the 13C- and deuterium labeled Treprostinil. Treprostinil (UT-15) is a potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively.
rel-Paroxetine-d4 (hydrochloride) is an isotope-labeled Paroxetine hydrochloride (HY-B0492). Paroxetine hydrochloride is an orally active and selective serotonin-reuptake inhibitor, commonly prescribed as an GRK2 inhibitor with IC50 of 14 μM. Paroxetine hydrochloride can be used for the research of depressive disorder[1][2][3][4].
N-Decyl-N,N-dimethyldecan-1-aminium-d6 (chloride) is a deuterated labeled N-Decyl-N,N-dimethyldecan-1-aminium (chloride) . N-Decyl-N,N-dimethyldecan-1-aminium chloride (Didecyldimethylammonium chloride) is a dialkyl-quaternary ammonium compound that is used in numerous products for its bactericidal, virucidal and fungicidal properties .
N-Desmethyl imatinib-d4 is the deuterium-labeled N-Desmethyl imatinib (HY-G0017). N-Desmethyl imatinib-d4 (Norimatinib) is a metabolite of Imatinib (HY-15463). Imatinib is a multi-target inhibitor of v-Abl, c-Kit and PDGFR .
Indinavir-d6 is the deuterium labeled Indinavir. Indinavir (MK-639; L735524) is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability.
Bzo-poxizid-d9 (5C-MDA-19-d9, Petyl MDA-19-d9) is deuterium labeled Bzo-poxizid. Bzo-poxizid is a synthetic cannabinoid that is a psychoactive substance .
O-Desmethyl Midostaurin-d5 is a deuterium labeled O-Desmethyl PKC412. O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) is the active metabolite of Midostaurin (HY-10230) via cytochrome P450 liver enzyme metabolism[1].
Cinnamic acid-d6 is the deuterium labeled Cinnamic acid. Cinnamic acid has potential use in cancer intervention, with IC50s of 1-4.5 mM in glioblastoma, melanoma, prostate and lung carcinoma cells.
Tamoxifen-d5 is a deuterium labeled Tamoxifen. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM). Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity .
rac Timolol-d5 (maleate) is a labelled racemic (S)-Timolol maleate. (S)-Timolol Maleate (L-714,465 Maleate) is a non-cardioselective hydrophilic β-adrenoceptor blocker. (S)-Timolol Maleate is widely used as standard medication for intraocular pressure (glaucoma) by preventing the production of aqueous humor. (S)-Timolol Maleate can be used for hypertension, angina pectoris and myocardial infarction[1][2][3].
Licarbazepine-d4-1 is deuterium labeled Licarbazepine. Licarbazepine (BIA 2-005; GP 47779) is a voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects[1].
Estradiol- 13C6 is the 13C-labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway[1][2][3].
Estradiol- 13C2 is the 13C-labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway[1][2][3].
5-Aminosalicylic acid- 13C6 is the 13C labeled 5-Aminosalicylic Acid[1]. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB[2][3][4].
Adenosine monophosphate- 13C10, 15N5,d12 (AMP- 13C10, 15N5,d12) dilithium is 13C and 15N-labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction [3].
Erlotinib- 13C6 (hydrochloride) is the 13C labeled Erlotinib Hydrochloride[1]. Erlotinib Hydrochloride (CP-358774 Hydrochloride) inhibits purified EGFR kinase with an IC50 of 2 nM[2]. Erlotinib-13C6 (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
5-Aminosalicylic acid-13C6 hydrochloride?(Mesalamine-13C6 hydrochloride; 5-ASA-13C6 hydrochloride; Mesalazine-13C6 hydrochloride) is the 13C labeled 5-Aminosalicylic Acidhydrochloride. 5-Aminosalicylic acid-13C6 hydrochloride?acts as a PPARγ agonist, and also inhibits p21-activated kinase 1 (PAK1) and NF-κB [3].
Hydrocortisone-d7 is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex[1].
Dyclonine-d9 (hydrochloride) is deuterium labeled Dyclonine (hydrochloride). Dyclonine hydrochloride (Dyclocaine hydrochloride) is an effective component of Runhou tablets. Dyclonine hydrochloride has significant bactericidal and fungicidal activity[1][2].
Amodiaquine-d10 hydrochloride is deuterated labeled Amodiaquine (HY-B1322A). Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect [3] .
Sulfanilamide-d4 is the deuterium labeled Sulfanilamide. Sulfanilamide is a competitive inhibitor for bacterial enzyme dihydropteroate synthetase with IC50 of 320 μM.
Phenformin-d5 (hydrochloride) is the deuterium labeled Phenformin hydrochloride. Phenformin hydrochloride is an anti-diabetic agent from the biguanide class, can activate AMPK activity[1][2].
Ramiprilat-d4 hydrochloride is deuterated labeled Ramiprilat (HY-A0115). Ramiprilat (HOE 498 diacid), an active metabolite of Ramipril, is a potent and orally active angiotensin converting enzyme (ACE) inhibitor with a Ki value of 7 pM. Ramiprilat can be used for high blood pressure and heart failure research .
Sulfacetamide-d4 (Sulphacetamide-d4) is the deuterium labeled Sulfacetamide (HY-N7123). Sulfacetamide (Sulphacetamide) is a sulfonamide antibiotic that can be used for the study of ocular infections. Sulfacetamide has antifungal and antibacterial activities .
Fenoverine-d8 is the deuterium labeled Fenoverine[1]. Fenoverine (Spasmopriv) is an antispasmodic agent and inhibits calcium channel currents[2]. Fenoverine induces rhabdomyolysis[3].
Dipivefrin-d6 (hydrochloride) is deuterium labeled Dipivefrin (hydrochloride). Dipivefrin hydrochloride (Dipivefrine hydrochloride) is an antiglaucoma proagent that is hydrolyzed to the active compound, epinephrine, by esterases in the cornea[1][2].
Diphenylmethane-d2 (Benzylphenyl-d2) is the deuterium labeled Diphenylmethane (HY-W008814). Diphenylmethane (Benzylphenyl) is a kind of biological materials or organic compounds that are widely used in life science research .
Ethambutol-d4 dihydrochloride is deuterated labeled Ethambutol dihydrochloride (HY-B0535A). Ethambutol dihydrochloride is an antimycobacterial compound that prevents cell wall formation by inhibiting arabinosyltransferase activity.
Levofloxacin-d8 is the deuterium labeled Levofloxacin. Levofloxacin, a synthetic fluoroquinolone, is an antibacterial agent that inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication.
Deltamethrin-d5 is the deuterium labeled Deltamethrin. Deltamethrin (Decamethrin), a neurotoxic pyrethroid insecticide, produces a reversible sequence of motor symptoms in rats involving hind limb rigidity and choreoathetosis[1][2].
Sulfadimethoxine-d4 is a deuterium labeled Sulfadimethoxine (Sulphadimethoxine). Sulfadimethoxine is a sulfonamide antibiotic used to treat many infections including treatment of respiratory, urinary tract, enteric, and soft tissue infections[1].
Temephos-d12 is the deuterium labeled Temephos[1]. Temefos is an organophosphate larvicide, used to treat water infested with disease-carrying insects including mosquitoes, midges, and black fly larvae. Temefos affects the central nervous system through inhibition of cholinesterase, results in death before reaching the adult stage[2][3].
Pyridoxine-d5 (Pyridoxol-d5) is a deuterium labeled Pyridoxine (HY-B1328). Pyridoxine (Pyridoxol) is a pyridine derivative. Pyridoxine exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
Lidocaine-d6 (hydrochloride) is deuterium labeled Lidocaine (hydrochloride). Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative and a agent to treat ventricular arrhythmia and an effective tumor-inhibitor[2].
Salcaprozate-d4 (sodium) is a deuterated labeled Salcaprozate (sodium) . Salcaprozate sodium (SNAC), an oral absorption promoter, and has the potential as a delivery agent for oral forms of heparin and insulin. Salcaprozate sodium could increase passive transcellular permeation across small intestinal epithelia based on increased lipophilicity arising from non-covalent macromolecule complexation [3].
Salvigenin-d9 is the deuterium labeled Salvigenin. Salvigenin is a natural polyphenolic compound, with neuroprotective effect. Salvigenin has antitumor cytotoxic and immunomodulatory properties[1][2].
Isoprenaline-d7 (hydrochloride) is a deuterated labeled Isoprenaline (hydrochloride) . Isoprenaline (Isoproterenol) hydrochloride is a non-selective, orally active β-adrenergic receptor agonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma [3] .
Hexadecanal-d5 (Palmitaldehyde-d5) is deuterium labeled Hexadecanal. Hexadecanal (Palmitaldehyde) , a volatile long-chain aliphatic aldehyde, is emitted from human feces, skin, and breath. The receptor for hexadecanal(OR37B) is highly conserved across mammals. Hexadecanal may exert its effects by modulating functional connectivity between the brain substrates of social appraisal and the brain substrates of aggressive execution. Also, Hexadecanal is confirmed to be highly deterrent to the ant Lasius niger. Hexadecanal is promising for the research of startle responses and aggression [3]
Indomethacin-d4 is a deuterium labeled Indomethacin. Indomethacin is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells[1]. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes[2].
Meclizine-d8 is a deuterium labeled Meclizine. Meclizine is a histamine H1 receptor antagonist and has the potential to treat nausea and motion sickness. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR[1][2][3].
Imperatorin-d6 (Ammidin-d6) is the deuterium labeled Imperatorin. Imperatorin is a BChE inhibitor and HIV-1 replication inhibitor. Imperatorin shows mild activity against Gram-negative bacteria .
Dicyclomine-d4 is the deuterium labeled Dicyclomine[1]. Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively[2]. Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo[3].
Drospirenone-d4 is the deuterium labeled Drospirenone. Drospirenone (Dihydrospirorenone) is a synthetic progestin that is an analog to spironolactone[1][2].
Ethambutol-d10 is the deuterium labeled Ethambutol. Ethambutol is a bacteriostatic antimycobacterial agent, which obstructs the formation of cell wall by inhibiting arabinosyl transferases.
Hydrocortisone-d2 is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex[1][2].
Lumefantrine-d9 is the deuterium labeled Lumefantrine. Lumefantrine is an antimalarial drug, used in combination with Artemether. The artemether-lumefantrine (AL) as the first- and second-line anti-malarial drugs.
Anandamide-d11 is deuterium labeled Anandamide. Anandamide is an immune modulator in the central nervous system acts via not only cannabinoid receptors (CB1 and CB2) but also other targets (e.g., GPR18/GPR55)[1][2].
Sulfachloropyridazine-d4 is the deuterium labeled Sulfachloropyridazine. Sulfachloropyridazine is a broad spectrum sulfonamide used against both Gram-positive and Gram-negative aerobic bacteria[1].
Sulfisomidin-d4 (Sulfaisodimidine-d4) is deuterium labeled Sulfisomidin. Sulfisomidin (Sulfaisodimidine) is an orally active short-acting sulfonamide antibacterial. Sulfisomidin can be used for the research of lower urinary tract infections .
Cletoquine-d4 is deuterium labeled Cletoquine. Cletoquine (Desethylhydroxychloroquine) is a major active metabolite of Hydroxychloroquine. Cletoquine is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune diseases treatment[1][2].
Nefopam-d4 (hydrochloride) is deuterium labeled Nefopam (hydrochloride). Nefopam hydrochloride (Fenazoxine hydrochloride) is a centrally-acting but non-opioid analgesic drug, for the relief of moderate to severe pain. Nefopam hydrochloride targets β-catenin protein level in mesenchymal cells in-vitro and in-vivo[1][2].
Acetylcholine-d9 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs)[1][2]. Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro[5].
Ethambutol-d4 is the deuterium labeled Ethambutol. Ethambutol is a bacteriostatic antimycobacterial agent, which obstructs the formation of cell wall by inhibiting arabinosyl transferases.
Dibenzylamine-d4 (Bisbenzylamine-d4) is the deuterium labeled Dibenzylamine (HY-Y1067). Dibenzylamine is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Alimemazine-d6 hydrochloride (Trimeprazine-d6 hydrochloride) is the deuterium labeled Alimemazine (HY-12752). Alimemazine is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist.Alimemazine (Trimeprazine) is also acts as a partial agonist against the histamine H1 receptor (H1R) and other GPCRs. Alimemazine displays antiserotonin, antispasmodic, and antiemetic properties .
Prednisone-d7 (Dehydrocortisone-d7) is deuterium labeled Prednisone. Prednisone (Adasone) is a corticosteroid agent with anti-inflammatory and immunosuppressive effects that can be used to study diseases related to systemic lupus erythematosus .
Pramocaine-d9 (hydrochloride) is deuterium labeled Pramocaine (hydrochloride). Pramocaine hydrochloride decreases the permeability of neuronal membranes to sodium ions, blocking both initiation and conduction of nerve impulses.
Hydrochlorothiazid-d2 is the deuterium labeled Hydrochlorothiazide. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect[1][2][3].
Ethotoin-d5 is the deuterium labeled Ethotoin[1]. Ethotoin (Peganone) is an orally active anticonvulsant agent used in epilepsy research, Ethotoin is a hydantoin, similar to phenytoin[2].
Acenaphthylene-d8 is the deuterium labeled Acenaphthylene[1]. Acenaphthylene is a polycyclic aromatic hydrocarbon (PAH). PAHs are derived naturally from coal and tar deposits, and produced by incomplete combustion of organic matter[2].
Hydrocortisone-d4 is the deuterium labeled Hydrocortisone. Hydrocortisone (Cortisol) is a steroid hormone or glucocorticoid secreted by the adrenal cortex[1].
Racecadotril-d5 is the deuterium labeled Racecadotril. Racecadotril (Acetorphan) is a neutral endopeptidase (NEP) inhibitor. Racecadotril and its active metabolite Thiorphan inhibits purified NEP activity from mouse brain with Kis of 4500 and 6.1 nM, , respectively. Antidiarrheal agent[1].
Torsemide-d7 is the deuterium labeled Torsemide. Torsemide (Torasemide) is an orally active loop diuretic. Torsemide has anti-aldosterone and vasodilatory effects. Torsemide also can be used for the research of heart failure, renal disease and hepatic cirrhosis[1][1][3].
Piperacillin-d5 is deuterium labeled Piperacillin. Piperacillin is kind of semisynthetic penicillins. Piperacillin has a broad spectrum of activity against Gram-positive and Gram-negative aerobic and anaerobic bacteria. Piperacillin has shown greater activity against β-lactamase-producing organisms than the other penicillins[1].
Sulfadoxine-d4 is the deuterium labeled Sulfadoxine. Sulfadoxine(Sulphadoxine) is a long acting sulfonamide that is used, usually in combination with other agents, for respiratory, urinary tract and malarial infections. Sulfadoxine inhibits HIV replication in peripheral blood mononuclear cells.
Bestatin-d7 (hydrochloride) is deuterium labeled Bestatin (hydrochloride). Bestatin hydrochloride is an inhibitor of CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase, used for cancer research.
Psychosine-d7 is deuterium labeled Psychosine. Psychosine, a substrate of the galactocerebrosidase (GALC) enzyme, is a potential biomarker for Krabbe disease. Psychosine is a highly cytotoxic lipid, capable of inducing cell death in a wide variety of cell
Atovaquone-d5 is the deuterium labeled Atovaquone. Atovaquone (Atavaquone) is a potent, selective and orally active inhibitor of the parasite’s mitochondrial cytochrome bc1 complex. Atovaquone is against human and P. falciparum cytochrome bc1 activity with IC50 values of 460 nM and 2.0 nM, respectively. Atovaquone is an antimalarial agent and has the potential for the investigation of neumocystis pneumonia, toxoplasmosis, malaria, and babesia[1][2].
Dibucaine-d9 is the deuterium labeled Dibucaine(HY-B0552).Dibucaine (Cinchocaine) is a sodium channel inhibitor. Dibucaine is a potent SChE inhibitor .
Pitolisant-d10 (Tiprolisant-d10) is deuterium labeled Pitolisant. Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM) .
Prednisone-d8 is the deuterium labeled Prednisone. Prednisone (Adasone) is a synthetic corticosteroid agent that is particularly effective as an immunosuppressant compound.
THIP-d4 (Gaboxadol-d4) is the deuterium labeled THIP (HY-10232). THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 μM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders [3].
Phenacetin-d5 is the deuterium labeled Phenacetin. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats[1][2][3].
Ditiocarb-d10 sodium (Sodium diethyldithiocarbamate-d10) is the deuterium labeled Ditiocarb sodium. Ditiocarb sodium is a copper reagent. The reaction with Cu 2+ solution resulted in the formation of a complex, which increased the copper displacement precipitation rate. Ditiocarb sodium can reduce HIV infection and can be used in adjuvant immune research of high-risk breast cancer [3].
Anandamide-d8 is a deuterated labeled Anandamide . Anandamide is an endocannabinoid. Anandamide modulates both neuronal and immune functions through two protein-coupled cannabinoid receptors (CB1 and CB2). Anandamide can activate numerous other receptors like PPARS, TRPV1, and GPR18/GPR55. Anandamide also has potential anti-fungal and anti-inflammatory activities. Anandamide can be used for the research of Alzheimer’s disease (AD) and ulcerative colitis [3] .
Psychosine-d5 is deuterium labeled Psychosine. Psychosine, a substrate of the galactocerebrosidase (GALC) enzyme, is a potential biomarker for Krabbe disease. Psychosine is a highly cytotoxic lipid, capable of inducing cell death in a wide variety of cell.
Desmethylcitalopram-d4 hydrochloride is deuterated labeled Desmethylcitalopram hydrochloride (HY-113739). Desmethylcitalopram (DCIT) hydrochloride is the active metabolite of Citalopram (HY-121203). Desmethylcitalopram has antidepressant effects. Desmethylcitalopram also inhibits cytochrome P450-2D6, -2C19 with IC50s of 39.5 and 53.5 μM .
Bisphenol AF-d4 is the isotope labelled analog of Bisphenol AF (HY-W013782). Bisphenol AF is a full agonist for the estrogen receptor. Bisphenol AF acts as an endocrine-disrupting chemical (EDC), activating estrogen through the estrogen receptor Era. Bisphenol AF-d4 can be used for the research of endocrinology and cancer .
Colfosceril miristate-d63 (DMPC-d63) is deuterium labeled Colfosceril miristate. Colfosceril miristate a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
Deoxycytidine triphosphate-d14 (dCTP-d14 dilithium; 2′-Deoxycytidine-5′-triphosphate-d14) dilithium is deuterium labeled Deoxycytidine triphosphate (HY-101400). Deoxycytidine triphosphate (dCTP) is a nucleoside triphosphate that can be used for DNA synthesis. Deoxycytidine triphosphate has many applications, such as real-time PCR, cDNA synthesis, and DNA sequencing.
Ezetimibe phenoxy glucuronide-d4 is the deuterium labeled Ezetimibe phenoxy glucuronide. Ezetimibe phenoxy glucuronide is the active metabolite of Ezetimibe. Antihyperlipoproteinemic activity[1]. Ezetimibe is a potent cholesterol absorption inhibitor[2].
VcMMAE-d8 is an isotope of VcMMAE (HY-15575). VcMMAE-d8 is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc) .
p,p'-DDD-d8 is the deuterium labeled p,p'-DDD[1]. p,p'-DDD (4,4’-DDD) is an organochlorine insecticide, a major metabolite of p,p'-DDT. p,p'-DDD is an agonist at estrogen receptor α(ERα) and ERβ. p,p'-DDD increases DNA damage, apoptosis and necrosis in peripheral blood. p,p'-DDD stimulates cell proliferation in SKBR3 cells. p,p'-DDD activates the AP-1 transcription factor. p,p'-DDD decreases sleep times of barbiturates and steroids in rats [3] .
D-Fructose- 13C6,d7 is the deuterium and 13C labeled D-Fructose. D-Fructose (D(-)-Fructose) is a naturally occurring monosaccharide found in many plants[1].
Menaquinone-4-d7 (Vitamin K2(MK-4)-d7) is the deuterium labeled Menaquinone-4. Menaquinone-4 is a vitamin K, used as a hemostatic agent, and also a adjunctive therapy for the pain of osteoporosis.
5,6-Epoxyeicosatrienoic acid-d11 (5,6-EET-d11) is deuterium labeled 5,6-Epoxyeicosatrienoic acid. 5,6-Epoxyeicosatrienoic acid (5,6-EET; (±)5,6-EpETrE) is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5,6-Epoxyeicosatrienoic acid degrades into 5,6-DiHET and 5,6-δ-lactone, which can be converted to 5,6-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5,6-Epoxyeicosatrienoic acid has been implicated in the mobilization of calcium and hormone secretion. 5,6-Epoxyeicosatrienoic acid is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50=0.54 μM), and Cav3. and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2, as measured by oxygen consumption and product formation assays when used at a concentration of 50 μM. (±)5,6-Epoxyeicosatrienoic acid is provided as a mixture of the free acid and lactone .
Oleic acid-d9 is deuterium labeled Oleic acid (HY-N1446). Oleic acid is an abundant monounsaturated fatty acid. Oleic acid is a Na+/K+ ATPase activato .
α-Vitamin E-d11 ((+)-α-Tocopherol-d11) is the deuterium labeled α-Vitamin E (HY-N0683). α-Vitamin E ((+)-α-Tocopherol), a naturally occurring vitamin E form, is a potent antioxidant .
Colfosceril miristate-d9 (DMPC-d9) is deuterium labeled Colfosceril miristate. Colfosceril miristate a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
Mono-(2-ethylhexyl) phthalate-d4 is a deuterium labeled Mono-(2-ethylhexyl) phthalate (HY-W018392). Mono-(2-ethylhexyl) phthalate (MEHP) is a major bioactive metabolite of diethylhexyl phthalate (DEHP). Mono-(2-ethylhexyl) phthalate can promote fatty acid synthesis in hepatocytes by regulating the expression of relevant genes and proteins, contributing to non-alcoholic fatty liver disease (NAFLD) .
Leukotriene B4-d4 is the deuterium labeled Leukotriene B4. Leukotriene B4 (LTB4) is known as one of the most potent chemoattractants and activators of leukocytes and is involved in inflammatory diseases. Leukotriene B4 is also an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1][2][3].
1,2-Dimyristoyl-sn-glycero-3-phosphocholine-d67 is deuterium labeled 1,2-Dimyristoyl-sn-glycero-3-phosphocholine. 1,2-Dimyristoyl-sn-glycero-3-phosphocholine (DMPC) is a synthetic phospholipid used in liposomes. 1,2-Dimyristoyl-sn-glycero-3-phosphocholine
Colfosceril miristate-d13 (DMPC-d13) is deuterium labeled Colfosceril miristate. Colfosceril miristate a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
Colfosceril miristate-d58 (DMPC-d58) is deuterium labeled Colfosceril miristate. Colfosceril miristate a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
Tazarotenic acid-13C2,d2 (AGN 190299-13C2,d2) is the 13C and deuterium labeled isotope of Tazarotenic acid (HY-101108). Tazarotenic acid is the metabolite of Tazarotene. Tazarotenic acid binding to retinoic acid receptors (RARs) is the probable molecular target of retinoid action. Tazarotenic acid has the potential for the research of warty dyskeratoma [3].
Colfosceril miristate-d4 (DMPC-d4) is deuterium labeled Colfosceril miristate. Colfosceril miristate is a synthetic phospholipid used in liposomes. Colfosceril miristate is used to study lipid monolayers, bilayers and drug delivery .
Docosahexaenoic acid-d5methyl ester is the deuterium labeled Docosahexaenoic Acid methyl ester. Docosahexaenoic Acid methyl ester is a methylated docosahexaenoic acid analog which can be intercalated into membrane phospholipids without being oxidized or hydrolyzed[1][2].
Oleic acid-d2) is the deuterium labeled Oleic acid (HY-N1446). Oleic acid (9-cis-Octadecenoic acid) is an abundant monounsaturated fatty acid ]. Oleic acid is a Na+/K+ ATPase activator .
Carvedilol metabolite 4-Hydroxyphenyl Carvedilol-d4 is deuterated labeled Carvedilol metabolite 4-Hydroxyphenyl Carvedilol (HY-12767). 4-Hydroxyphenyl Carvedilol is a metabolite of Carvedilol.
L-Arginine- 15N4,d7 (hydrochloride) is the deuterium and 15N-labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
Urea- 15N2 is the 15N-labeled Urea. Urea is a powerful protein denaturant via both direct and indirect mechanisms[1]. A potent emollient and keratolytic agent[2]. Used as a diuretic agent. Blood urea nitrogen (BUN) has been utilized to evaluate renal function[3]. Widely used in fertilizers as a source of nitrogen and is an important raw material for the chemical industry.
Thymidine- 15N2 is the 15N labeled Thymidine[1]. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[2][3][4].
Oleic acid-d17 is the deuterium labeled Oleic acid (HY-N1446). Oleic acid (9-cis-Octadecenoic acid) is an abundant monounsaturated fatty acid . Oleic acid is a Na+/K+ ATPase activator .
Tamsulosin-d4 ((R)-(-)-YM12617 (free base)-d4) is deuterium labeled Tamsulosin. Tamsulosin ((R)-(-)-YM12617 free base) is an inhibitor of α1-adrenergic receptor. Tamsulosin is used for the research of prostatic hyperplasia. Tamsulosin attenuates abdominal aortic aneurysm growth in animal models .
Cytidine-5'-triphosphate-d14 (Cytidine triphosphate-d14 dilithium; 5'-CTP-d14) dilithium is deuterium labeled Cytidine-5'-triphosphate (HY-125818). Cytidine 5′-triphosphate (Cytidine triphosphate; 5'-CTP) is a nucleoside triphosphate and serves as a building block for nucleotides and nucleic acids, lipid biosynthesis. Cytidine triphosphate synthase can catalyze the formation of cytidine 5′-triphosphate from uridine 5′-triphosphate (UTP). Cytidine 5′-triphosphate is an essential biomolecule?in the de novo?pyrimidine biosynthetic pathway in?T. gondii.
L-Glutamine- 13C5, 15N2,d5 is the deuterium, 13C-, and 15-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells .
Fosfructose- 13C6 (tetrasodium hydrate) is the 13C labeled Fosfructose (HY-106950). Fosfructose is a cytoprotective natural sugar phosphate for the potential treatment of cardiovascular ischemia, sickle cell anemia and asthma[1].
Butylparaben- 13C6 is the 13C labeled Butylparaben[1]. Butylparaben is an organic compound, has proven to be a highly successful antimicrobial preservative in cosmetics, also used in medication suspensions, and as a flavoring additive in food.
Riboflavin-5-Phosphate- 13C4, 15N2-1 is the 13C-labeled and 15N-labeled Riboflavin. Riboflavin is an easily absorbed micronutrient with a key role in maintaining health in humans and other animals.
5'-Guanylic acid- 13C10, 15N5 (5'-GMP- 13C10, 15N5 dilithium; 5'-guanosine monophosphate- 13C10, 15N5) dilithium is 13C and 15N-labeled 5'-Guanylic acid (HY-N5134). 5'-Guanylic acid (5'-GMP) is involved in several metabolic disorders, including the AICA-ribosiduria pathway, adenosine deaminase deficiency, adenine phosphoribosyltransferase deficiency (aprt), and the 2-hydroxyglutric aciduria pathway.
Chlorogenic acid- 13C3 (Heriguard- 13C3; NSC-407296- 13C3) is 13C- and 15N-labeled Chlorogenic acid (HY-N0055). Chlorogenic acid is a major phenolic compound in Lonicera japonica Thunb.. It plays several important and therapeutic roles such as antioxidant activity, antibacterial, hepatoprotective, cardioprotective, anti-inflammatory, antipyretic, neuroprotective, anti-obesity, antiviral, anti-microbial, anti-hypertension .
Clascoterone-d5-1 (Cortexolone 17 alpha-propionate-d5-1) is deuterium labeled Clascoterone. Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist .
Cytidine-d13 (Cytosine β-D-riboside-d13; Cytosine-1-β-D-ribofuranoside-d13) is deuterium labeled Cytidine (HY-B0158). Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catecholamine synthesis, and mitochondrial function [3].
Thymidine- 13C10 (DThyd- 13C10; NSC 21548- 13C10) is 13C-labeled Thymidine (HY-N1150). Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication.
Cytidine 5′-monophosphate-d12 (5'-Cytidylic acid-d12 dilithium; 5'-CMP-d12) dilithium is deuterium labeled Cytidine 5'-monophosphate (HY-W009162). Cytidine 5'-monophosphate (5'-Cytidylic acid) is a nucleotide which is used as a monomer in RNA. Cytidine 5'-monophosphate consists of the nucleobase cytosine, the pentose sugar ribose, and the phosphate group.
5'-Guanylic acid-d12 (5'-GMP-d12 dilithium; 5'-guanosine monophosphate-d12) dilithium is deuterium labeled 5'-Guanylic acid (HY-N5134). 5'-Guanylic acid (5'-GMP) is involved in several metabolic disorders, including the AICA-ribosiduria pathway, adenosine deaminase deficiency, adenine phosphoribosyltransferase deficiency (aprt), and the 2-hydroxyglutric aciduria pathway.
L-Glutathione reduced-d2 (GSH-d2; γ-L-Glutamyl-L-cysteinyl-glycine-d2) is deuterated-labeled L-Glutathione reduced (HY-D0187). L-Glutathione reduced is an endogenous antioxidant and oxygen free radical scavenger.
Guanosine- 15N5 is the 15N labeled Guanosine[1]. Guanosine (DL-Guanosine) is a purine nucleoside comprising guanine attached to a ribose (ribofuranose) ring via a β-N9-glycosidic bond. Guanosine possesses anti-HSV activity[2].
Nicotinamide- 13C6 is the 13C-labeled Nicotinamide. Nicotinamide is a form of vitamin B3 that plays essential roles in cell physiology through facilitating NAD+ redox homeostasis and providing NAD+ as a substrate to a class of enzymes that catalyze non-redox reactions. Nicotinamide is an inhibitor of SIRT1.
Guanosine triphosphate- 15N5,d14 (GTP- 15N5,d14) dilithium is deuterium and 15N labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19.
L-Tryptophan- 13C11 is the 13C-labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3[1].
Sulfameter- 13C6 is the 13C6 labeled Sulfameter. Sulfameter (Sulfametoxydiazine; 5-Methoxysulfadiazine) is an effective long-acting sulfonamide antibiotic with antibacterial activities. Sulfameter can be used for the research of urinary tract infections and lepriasis.
Cytidine-d2 is the deuterium labeled Cytidine. Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catecholamine synthesis, and mitochondrial function[1][2][3].
(Rac)-Atomoxetine-d7 (hydrochloride) is a deuterium labeled (Rac)-Atomoxetine hydrochloride. (Rac)-Atomoxetine hydrochloride is a racemic form of Atomoxetine hydrochloride. Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5 nM, 77 nM and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively)[1].
Estrone- 13C2 is the 13C-labeled Estrone. Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells[1][2].
L-Tryptophan- 15N2 is the 15N-labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3 .
(E,E)-Farnesol-d6 is deuterium labeled Farnesol. Farnesol is a sesquiterpene alcohol that modulates cell-to-cell communication in Candida albicans, and has the activity in inhibiting bacteria.
(R,R)-Secoisolariciresinol diglucoside-d6 is deuterated labeled (R,R)-Secoisolariciresinol diglucoside (HY-N6937). (R,R)-Secoisolariciresinol diglucoside ((R,R)-SDG) is the minor isomer of Secoisolariciresinol diglucoside in flaxseed. (R,R)-Secoisolariciresinol diglucoside ((R,R)-SDG) possesses antioxidant and free radical scavenging activities and DNA-radioprotective properties. (R,R)-Secoisolariciresinol diglucoside ((R,R)-SDG) inhibits myeloperoxidase (MPO) activity by suppressing both the peroxidase and chlorination cyclesin inflammatory cells [3].
Guanosine- 13C10 is the 13C labeled Guanosine (HY-N0097). Guanosine is a purine nucleoside comprising guanine attached to a ribose (ribofuranose) ring via a β-N9-glycosidic bond. Guanosine possesses anti-HSV activity .
Adenosine monophosphate- 15N5,d12 (AMP- 15N5,d12) dilithium is deuterium and 15N labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction [3].
Cytidine-d is the deuterium labeled Cytidine. Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catechol
D-Glucose- 13C,d is the deuterium and 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical sig
D-Glucose- 13C,d2 is the deuterium and 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical sig
D-Glucose- 13C2-4 is the 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
Tacrolimus- 13C,d2 is a 13C-labeled and deuterium labeled Tacrolimus. Tacrolimus (FK506), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties[1].
((2R,3S,4R,5R)-5-(4-Amino-2-oxopyrimidin-1(2H)-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl phosphate- 13C9, 15N3 (sodium) is the 13C and 15N labeled Sodium ((2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1(2H)-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl phosphate[1].
Pentamidine-d4 (dihydrochloride) is the deuterium labeled Pentamidine dihydrochloride. Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dihydrochloride inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dihydrochloride is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dihydrochloride has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities[1][2][3][4].
Guaiacol-d7 is the deuterium labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
Pitavastatin-d5 (sodium) is the deuterium labeled Pitavastatin sodium. Pitavastatin (NK-104) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Anti-cancer activity.
Mirogabalin-d4 (DS5565-d4) is a deuterated compound of Mirogabalin (HY-12650), a ligand that selectively targets the voltage-sensitive calcium channel complex α2δ-1 .
Benzyl alcohol-d7 is the deuterium labeled Benzyl alcohol. Benzyl alcohol is an aromatic alcohol; a colorless liquid with a mild pleasant aromatic odor.
Gemfibrozil-d6 is the deuterium labeled Gemfibrozil. Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.
Agomelatine-d4 is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively[1]. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively[2].
Ambroxol-d5 (hydrochloride) is the deuterium labeled Ambroxol hydrochloride. Ambroxol hydrochloride (NA-872 hydrochloride), an active metabolite of the proagent Bromhexine, has potent expectorant effects. Ambroxol hydrochloride is a glucocerebrosidase (GCase) chaperone and increases glucocerebrosidase activity. Ambroxol hydrochloride induces lung autophagy and has the potential for Parkinson disease and neuronopathic Gaucher disease research[1][2].
Mequinol-d4 is the deuterium labeled Mequinol[1]. Mequinol (4-Methoxyphenol) is one of bioactive components in Mercurialis. Mequinol is used for skin depigmentation[2].
Efinaconazole-d4 is the deuterium labeled Efinaconazole. Efinaconazole (KP-103) is a triazole antifungal agent and againsts T. mentagrophytes SM-110 and C. albicans ATCC 10231 with MICs of 0.0039 μg/mL and 0.00098 μg/mL, respectively[1]. Efinaconazole has a potent in vitro activity against fungal pathogens including dermatophytes, Candida and Malassezia species[1].
Netupitant-d6 is the deuterium labeled Netupitant (CID-6451149), which is a highly potent and selective, orally active neurokinin-1 (NK1) receptor antagonist[1].
Phytosphingosine-d7 (4-Hydroxysphinganine-d7) is deuterium labeled Phytosphingosine. Phytosphingosine is a phospholipid with anti-inflammatory, antibacterial, and anti-cancer activities, which can induce apoptosis. Phytosphingosine is an immune regulator and can be used in the study of inflammatory skin diseases. Phytosphingosine is also an activator of GPR120 with an IC50 value of 33.4 μM and can be used in the study of type II diabetes [3] .
Norfloxacin-d8 is the deuterium labeled Norfloxacin. Norfloxacin (MK-0366) is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria, which functions by inhibiting DNA gyrase.
Ceftazidime-d5 is the deuterium labeled Ceftazidime. Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Ponesimod-d7 (ACT-128800-d7) is the deuterium-labeled Ponesimod (HY-10569). Ponesimod-d7 (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod-d7 activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod-d7 can protect against lymphocyte-mediated tissue inflammation [3].
Eliglustat-d15 (Genz 99067-d15) is deuterium labeled Eliglustat. Eliglustat is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC50 of 24 nM .
Rabeprazole-d4 (sodium) is the deuterium labeled Rabeprazole sodium. Rabeprazole sodium (LY307640 sodium) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H+/K+-ATPase. Rabeprazole sodium induces apoptosis. Rabeprazole sodium acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole sodium can be used for the research of gastric ulcerations and gastroesophageal reflux[1][2][3].
DL-dithiothreitol-d6 is the deuterated form of DL-dithiothreitol. DL-dithiothreitol (DTT) is a strong reductant with anti-disulfidptosis activity. DL-dithiothreitol is oxidized to form a stable six-membered ring with an internal disulfide bond .
Mozavaptan-d6 (OPC-31260-d6) is the deuterium labeled Mozavaptan. Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment .
Sucrose-d14 is the deuterium labeled Sucrose. Sucrose (D-(+)-Saccharose) is a disaccharide which is composed of two monosaccharides, glucose and fructose. Sucrose can be applied in some animal models, including metabolic disease, obesity, diet on preferen
Chlortetracycline-d6 (hydrochloride) is the deuterium labeled Chlortetracycline hydrochloride. Chlortetracycline hydrochloride (7-Chlorotetracycline hydrochloride) is a specific and potent calcium ionophore antibiotic, inhibits binding of aminoacyl-tRNA to ribosomes.
Bexarotene-d4 is a deuterium labeled Bexarotene (LGD1069). Bexarotene (LGD1069) is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma[1][2][3][4][5].
Lenvatinib-d4 is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities[1][2].
2-Hydroxyestrone-d4 is the deuterium labeled 2-Hydroxyestrone. 2-Hydroxyestrone (Catecholestrone) is a specific receptor-mediated antiestrogenic agent. 2-Hydroxyestrone is anticarcinogenic[1][2].
Imiquimod-d6 is the deuterium labeled Imiquimod. Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19[1][2].
Homosalate-d4 is the deuterium labeled Homosalate. Homosalate is an organic compound used in some sunscreens, it is used as a chemical UV filter, protecting the skin from sun damage.
Pomalidomide-d4 is the deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors<
Dienogest-d6 is deuterium labeled Dienogest (HY-B0084). Dienogest is an orally active progesterone receptor agonist that can be used in the study of endometriosis [3].
Oseltamivir-d5 (phosphate) is the deuterium labeled Oseltamivir phosphate. Oseltamivir phosphate (GS 4104) is a neuraminidase inhibitor recommended for the treatment and prophylaxis of influenza A and B[1][2].
Evocalcet-d4 (KHK7580-d4) is deuterium labeled Evocalcet. Evocalcet (KHK7580) is an orally active calcium sensing receptor (CaSR) agonist. Evocalcet inhibits the secretion of parathyroid hormone (PTH) from parathyroid gland cells. Evocalcet can be used for the research of hyperparathyroidism .
Ledipasvir-d6 hydrochloride is deuterated labeled Ledipasvir acetone (HY-15602A). Ledipasvir acetone (GS-5885 acetone) is the active ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
Upadacitinib-d5 is the deuterium labeled Upadacitinib. Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Pravastatin-d9 sodium is deuterated labeled Pravastatin (HY-B0165). Pravastatin (CS-514) is a competitive HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM .
Cariprazine-d6 is a deuterium labeled Cariprazine. Cariprazine Cariprazine is an antipsychotic agent that exhibits high affinity for the D3 (Ki of 0.085 nM) and D2 (Ki of 0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki of 2.6 nM)[1].
Ertugliflozin-d9 is deuterated labeled Ertugliflozin (HY-15461). Ertugliflozin (PF-04971729) is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), with an IC50 of 0.877 nM for h-SGLT2 . Has the potential for the treatment of type 2 diabetes mellitus .
Carboplatin-d4 is the deuterium labeled Carboplatin. Carboplatin (NSC 241240) is a DNA synthesis inhibitor which binds to DNA, inhibits replication and transcription and induces cell death. Carboplatin (NSC 241240) is a derivative of CDDP and a potent anti-cancer agent.
Oxcarbazepine-d4 (GP 47680-D4) is the deuterium labeled Oxcarbazepine. Oxcarbazepine is a sodium channel blocker[1]. Oxcarbazepine significantly inhibits glioblastoma cell growth and induces apoptosis or G2/M arrest in glioblastoma cell lines[2]. Anti-cancer and anticonvulsant effects[2][3].
Penicillin G-d5 (potassium) is the deuterium labeled Penicillin G potassium. Penicillin G potassium is a fast-acting antibiotic; used to treat bacterial infections that affect the blood, heart, lungs, joints, and genital areas[1][2].
Trandolapril-d5 is a deuterium labeled Trandolapril (RU44570). Trandolapril is an orally active angiotensin converting enzyme (ACE) inhibitor for hypertension and congestive heart failure (CHF)[1].
Levobupivacaine-d9 ((S)-(–)-Bupivacaie-d9) hydrochloride is deuterium labeled Levobupivacaine (hydrochloride). Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine hydrochloride exerts agent that can suppress or relieve pain. and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer [3] .
Posaconazole-d5 is a deuterium-labeled form of Posaconazole. Posaconazole is a broad-spectrum, second generation, triazole compound with antifungal activity[1].
Ergothioneine-d9 is the deuterium labeled Ergothioneine. Ergothioneine, an imidazole-2-thione derivative of histidine betaine, is synthesized by certain bacteria and fungi. Ergothioneine is generally considered an antioxidant[1].
Cuminaldehyde-d8 is deuterated labeled Cuminaldehyde (HY-Y0790). Cuminaldehyde is the major component of Cuminum cyminum, a natural aldehyde with inhibitory effect on alpha-synuclein fibrillation and cytotoxicity. Cuminaldehyde shows anticancer activity .
Odevixibat-d5 is deuterated labeled Odevixibat (HY-109120). Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis .
Amoxapine-d8 is the deuterium labeled Amoxapine. Amoxapine (CL-67772) is a norepinephrine reuptake blocker and a 5-HT2/5-HT3 antagonist. Amoxapine can be used for the research of depression. Amoxapine has antibacterial activity. Amoxapine can enhance the killing effect of macrophages on mycobacterium by inducing autophagy, while protecting the cells from death [3] .
Terconazole-d4 is the deuterium labeled Terconazole. Terconazole is a broad-spectrum antifungal medication for the treatment of vaginal yeast infection.
Lenvatinib-d5 is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities[1][2].
Resorufin-d6 is the deuterium labeled Resorufin. Resorufin (NSC 12097) is a highly fluorescent pink dye for the detection of ROS/RNS and a second analyte[1].
4-Hydroxytolbutamide-d9 is the deuterium labeled 4-Hydroxytolbutamide. 4-Hydroxytolbutamide (Hydroxytolbutamide) is a metabolite of Tolbutamide. 4-Hydroxytolbutamide is metabolized by CYP2C8 and CYP2C9. Tolbutamide is a first generation potassium channel blocker and a sulfonylurea oral antidiabetic[1][2].
Cilostazol-d4 is deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM[1][2].
Palbociclib-d8 is a deuterium labeled Palbociclib. Palbociclib is a selective and orally active CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research[1].
Arachidonic acid-d11 is the deuterium labeled Arachidonic acid. Arachidonic acid is an essential fatty acid and a major constituent of biomembranes[1][2].
Itraconazole-d5 is the deuterium labeled Itraconazole. Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects[1][2][3].
Sotalol-d6 (hydrochloride) is a deuterium labeled Sotalol hydrochloride. Sotalol hydrochloride is an orally active, non-selective competitive β-adrenergic receptor blocker. Sotalol hydrochloride is a potent antiarrhythmic agent that can be used for the research of pediatric arrhythmias. Sotalol hydrochloride blocks β-receptors, and potassium KCNH2 channels[1][2].
Bezafibrate-d4 is deuterium labeled Bezafibrate. Bezafibrate is an agonist of PPAR, with EC50s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent.
Darifenacin-d4 is the deuterium labeled Darifenacin[1]. Darifenacin(UK88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9. IC50 value: 8.9 (pKi)[2].
Fingolimod-d4 (hydrochloride) is the deuterium labeled Fingolimod hydrochloride. Fingolimod hydrochloride (FTY720) is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod hydrochloride (FTY720) also is a pak1 activator, a immunosuppressant[1].
Troglitazone-d4 is deuterium labeled Troglitazone. Troglitazone is a PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively.
Abiraterone-d4 is the deuterium labeled Abiraterone. Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.
Treprostinil-d7 (UT-15-d7) is a deuterated version of Treprostinil (HY-100441). Treprostinil is a highly potent DP1 and EP2 agonist with EC50s of 0.6 nM and 6.2 nM, respectively [3] .
Anastrozole-d12 is the deuterium labeled Anastrozole. Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC50 of 15 nM[1][2].
Montelukast-d6 (sodium) is the deuterium labeled Montelukast (sodium). Montelukast sodium is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (Cysltr1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage[1].
Diaveridine-d6 (EGIS-5645-d6) is deuterium labeled Diaveridine. Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent .
Siponimod-d11 is deuterium labeled Siponimod (HY-12355). Siponimod is an orally active and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod is selective for S1P1 and S1P5 over S1P2, S1P3, and S1P4, with EC50s of 0.4, 0.98, >10000, >1000, and 750 nM, respectively. Siponimod can be used for multiple sclerosis (MS) research [3] .
Equilin-d4 is the deuterium labeled Equilin. Equilin (7-Dehydroestrone) is an important member of the large group of oestrogenic substances and is chemically related to menformon (oestrone). Equilin increases the growth of cortical neurons via an NMDA receptor-dependent mechanism[1][2].
Lauryl benzalkonium-d7 (Dimethylaurylbenzylammonium-d7) chloride is the deuterium labeled Lauryl benzalkonium chloride. Lauryl benzalkonium chloride is a cationic surfactant .
Dolasetron-d5 is deuterated labeled Dolasetron (HY-B0750). Dolasetron (MDL-73147) is a 5-HT3 receptor antagonist with potential for treatment of chemotherapy-induced nausea and vomiting.
Topiroxostat-d4 is deuterium labeled Topiroxostat. Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 value of 5.3 nM and a Ki value of 5.7 nM. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment[1][2].
Cimaterol-d7 is the deuterium labeled Cimaterol. Cimaterol is a potent agonist of β-adrenergic receptors (pEC50s=8.13, 8.78, and 6.62 for human β1, β2, and β3, respectively). Cimaterol has been used in farmed animals to increase carcass mass and to alter muscle and fat deposition.
Benzyl alcohol-d5 is the deuterium labeled Benzyl alcohol. Benzyl alcohol is an aromatic alcohol; a colorless liquid with a mild pleasant aromatic odor.
Azaperone-d4 is the deuterium labeled Azaperone. Azaperone (R-1929) acts as a dopamine antagonist but also has some antihistaminic and anticholinergic properties. Azaperone is a pyridinylpiperazine and butyrophenone neuroleptic agent with antiemetic effects, which is used mainly as a tranquilizer in veterinary medicine.
Levonorgestrel-d8 is the deuterium labeled Levonorgestrel. Levonorgestrel is a synthetic progestogen used as an active ingredient in some hormonal contraceptives[1][2]. Levonorgestrel-d8 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Ropinirole-d14 hydrochloride is deuterated labeled Ropinirole hydrochloride (HY-B0623A). Ropinirole (SKF 101468) hydrochloride is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease .
Valproic acid-d7 (sodium) is the deuterium labeled Valproic acid (sodium salt). Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium salt activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches[1][2].
Canagliflozin-d6 is the deuterium labeled Canagliflozin[1]. Canagliflozin (JNJ 28431754) is a selective SGLT2 inhibitor with IC50s of 2 nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and hSGLT2 in CHOK cells, respectively[2].
Losartan-d2 is the deuterium labeled Losartan[1]. Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.
Telmisartan-d4 is the deuterium labeled Telmisartan. Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM[1][2].
Apalutamide-d4 is a deuterium labeled Apalutamide. Apalutamide is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM[1].
Pemetrexed-d5 is the deuterium labeled Pemetrexed[1]. Pemetrexed (LY231514) is an antifolate, the Ki values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively[2].
Apremilast-d8 (CC-10004-d8) is deuterium labeled Apremilast. Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM .
Acetylcholine-d4 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs)[1][2]. Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro[5].
Clomifene-d5 (hydrochloride) is a deuterium labeled Clomifene. Clomifene is an orally active compound used for infertility. Clomifene is a simple, relatively safe, easily administered and well-tolerated efficacious compound to induce ovulation[1].
Acalabrutinib-d4 is a deuterium labeled Acalabrutinib. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor[1]. Acalabrutinib-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Carvedilol-d4 is the deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker[1]. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure[2]. Carvedilol is an autophagy inducer that inhibits the NLRP3inflammasome[3].
Crizotinib-d9 hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition [3].
Methylprednisolone-d2 is the deuterium labeled Methylprednisolone. Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels[3][4].
Posaconazole-d4 is a deuterium-labeled form of Posaconazole. Posaconazole is a broad-spectrum, second generation, triazole compound with antifungal activity[1].
Icotinib-d4 is the deuterium-labeled Icotinib (HY-15164A). Icotinib-d4 (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib-d4 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Debutyldronedarone-d7 hydrochloride is deuterated labeled Debutyldronedarone hydrochloride (HY-12753A). Debutyldronedarone (SR35021) hydrochloride, the main metabolite of Dronedarone, is a selective thyroid hormone receptor α1 (TRα1) inhibitor. Debutyldronedarone hydrochloride inhibits T3 binding to TRα1 and TRβ1 by 77% and 25%, respectively. Debutyldronedarone hydrochloride can be used for the research of arrhythmic .
Tigecycline-d9 is deuterium labeled Tigecycline. Tigecycline (GAR-936) is a broad-spectrum glycylcycline antibiotic. The mean inhibitory concentration (MIC) of Tigecycline for E. coli (MG1655 strain) is approximately 125 ng/mL[1]. MIC50 and MIC90 are 1 and 2 mg/L for Acinetobacter baumannii (A. baumannii), respectively[2].
Risedronic acid-d4 (Risedronate-d4) is the deuterium labeled Risedronic acid (HY-B0148).Risedronic acid (Risedronate) sodium, a bisphosphonate, is a potent anti-resorption agent that inhibits osteoclast-mediated bone resorption and changes the bone metabolism. Risedronic acid sodium suppresses osteoblast differentiation and induced caspase- and isoprenoid depletion-dependent apoptosis. Risedronic acid sodium inhibits blood stages of Plasmodium falciparum (IC50 of 20.3 μM). Risedronic acid sodium inhibits the transfer of the farnesyl pyrophosphate group to parasite proteins [3] .
Donepezil-d5 (hydrochloride) is deuterium labeled Donepezil (Hydrochloride). Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE[1]. Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity[2].
Permethrin-d9 is the deuterium labeled Permethrin. Permethrin (NRDC-143) is an insecticide, acaricide, and insect repellent; functions as a neurotoxin, affecting neuron membranes by prolonging sodium channel activation.
Losartan-d9 is the deuterium labeled Losartan[1]. Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.
Azilsartan-d4 is the deuterium labeled Azilsartan[1]. Azilsartan is an orally active, potent, selective and specific angiotensin II type 1 receptor (AT1) antagonist. Azilsartan induces ROS formation and apoptosis in HepG2 cells. Azilsartan shows neuroprotective and anticancer activity. Azilsartan can be used for hypertension and stroke research[2][3][4][5][6].
Desloratadine-d4 is the deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities[1][2].
Desloratadine-d5 is deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities[1][2].
Alfuzosin-d7 is the deuterium labeled Alfuzosin[1]. Alfuzosin (SL 77499-10) is an orally active, selective and competitive α1-adrenoceptor antagonist. Alfuzosin relaxes the muscles of the prostate and bladder neck, aiding in urination. Alfuzosin can be used in study of benign prostatic hyperplasia (BPH)[2][3].
Enzalutamide-d6 (MDV3100-d6) is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells .
1-Octanol-d5 is deuterated labeled Carvacrol (HY-N0711). Carvacrol is an orally active monoterpenic phenol that can be extract from an abundant number of aromatic plants, including thyme and oregano, possessing antioxidant, antibacterial, antifungal, anticancer, anti-inflammatory, hepatoprotective, spasmolytic, and vasorelaxant properties. Carvacrol also causes cell cycle arrest in G0/G1, downregulates Notch-1, and Jagged-1, and induces apoptosis. Carvacrol is used in low concentrations as a food flavoring ingredient and preservative, as well as a fragrance ingredient in cosmetic formulations .
Leniolisib-d5 is a deuterated labeled Leniolisib . Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor. Leniolisib has the potential for immunodeficiency disorders treatment.
Treprostinil-d9 (UT-15-d9) is the deuterium-labeled Treprostinil (HY-100441) . Treprostinil (UT-15) is a potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively.
1-Octanol-d17 is the deuterium labeled 1-Octanol[1]. 1-Octanol (Octanol), a saturated fatty alcohol, is a T-type calcium channels (T-channels) inhibitor with an IC50 of 4 μM for native T-currents[2]. 1-Octanol is a highly attractive biofuel with diesel-like properties[3].
Diphenyl Phosphate-d10 (DPhP-d10) is the deuterium labled Diphenyl Phosphate (HY-W008151). Diphenyl Phosphate inhibits growth and energy metabolism of zebrafish in a sex-specific manner.
Cefiderocol-d6 (S-649266-d6) is a deuterated labeled Cefiderocol (HY-17628). Cefiderocol is a siderophore cephalosporin which has a potent activity against a broad range of aerobic Gram-negative bacterial species with MIC50s of 2 μg/mL or less .
Paroxetine-d4 (BRL29060-d4) is deuterium labeled Paroxetine. Paroxetine is an oral inhibitor that falls under the category of selective serotonin reuptake inhibitors (SSRIs). Paroxetine is also a very weak norepinephrine (NE) reuptake inhibitor, capable of inducing cell apoptosis and having anti-tumor activity. Paroxetine has antidepressant, anti-anxiety, and pain-relieving effects, and it can help improve conditions like obsessive-compulsive disorder, panic disorder, post-traumatic stress disorder, premenstrual anxiety, and chronic headaches [3] .
Tetrahydrozoline-d4 (hydrochloride) is the deuterium labeled Tetrahydrozoline hydrochloride. Tetrahydrozoline hydrochloride (Tetryzoline hydrochloride), a derivative of imidazoline, is an α-adrenergic agonist that causes vasoconstriction. Tetrahydrozoline hydrochloride is widely used for the research of nasal congestion and conjunctival congestion[1][2].
Creatinine-d5 is the deuterium labeled Creatinine. Creatinine (NSC13123) is a break-down product of creatine phosphate in muscle, and is usually produced at a fairly constant rate by the body [3].
Tandospirone-d8 (SM-3997-d8) is deuterium labeled Tandospirone. Tandospirone (SM-3997) is a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM. Tandospirone has anxiolytic and antidepressant activities. Tandospirone can be used for the research of the central nervous system disorders and the underlying mechanisms [3] .
Dimethylamine-d6 hydrochloride is a deuterium labeled Dimethylamine hydrochloride. Dimethylamine hydrochloride is the immediate precursor of dimethylnitrosamine, a known potent carcinogen in a wide variety of animal species .
Bendamustine-d8 (hydrochloride) is deuterium labeled Bendamustine (hydrochloride). Bendamustine hydrochloride (SDX-105), a purine analogue, is a DNA cross-linking agent. Bendamustine hydrochloride activats DNA-damage stress response and apoptosis. Bendamustine hydrochloride has potent alkylating, anticancer and antimetabolite properties[1].
Laquinimod-d5 (ABR-215062-d5) is deuterium labeled Laquinimod. Laquinimod (ABR-215062), an orally available carboxamide derivative, is a potent immunomodulator that prevents neurodegeneration and inflammation in the central nervous system. Laquinimod reduces astrocytic NF-κB activation to protect from Cuprizone-induced demyelination. Laquinimod has the potential for relapsing-remitting (RR) and chronic progressive (CP) forms of multiple sclerosis (MS; RRMS or CPMS) as well as neurodegenerative diseases research .
Penicillin V-d5 (potassium) is the deuterium labeled Penicillin V Potassium[1]. Penicillin V Potassium (Phenoxymethylpenicillin potassium salt) is an orally active antibiotic. Penicillin V Potassium inhibits the growth of Streptococci, C. difficile and S. aureus. Penicillin V Potassium can be used for the research of otitis, sinusitis, pharyngitis and tonsillitis[2][3][4][5].
Cariprazine-d8 is a deuterium labeled Cariprazine. Cariprazine is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
Sotorasib-d7 (AMG-510-d7) is a deuterium-labeled Sotorasib (HY-114277). Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) [3].
Carvedilol-d5 is deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker[1]. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure[2]. Carvedilol is an autophagy inducer that inhibits the NLRP3inflammasome[3].
Lopinavir-d7 is deuterated labeled Lopinavir (HY-14588). Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM [3].
Octopamine-d4 (hydrochloride) is the deuterium labeled Octopamine hydrochloride. Octopamine ((±)-p-Octopamine) hydrochloride, a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates. Octopamine hydrochloride can stimulate alpha2-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha2-ARs. Octopamine hydrochloride increased glycogenolysis, glycolysis, oxygen uptake, gluconeogenesis and the portal perfusion pressure[1][2][3].
Elacestrant-d10 is the deuterium labeled of Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also inhibits growth of ER + breast cancer cell lines in vitro and in vivo .
Chenodeoxycholic Acid-d4 is the deuterium labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
Rimonabant-d10 is deuterium labeled Rimonabant. Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
Trifloxystrobin-d6 is the deuterium labeled Trifloxystrobin. Trifloxystrobin (CGA 279202) is a fungicide, with EC50s of 23.0 μg/L and 1.7 μg/L for Daphnia magna neonate and embryos, respectively, after treatment for 48 h[1].
Loperamide-d6 (hydrochloride) is a deuterium labeled Loperamide hydrochloride. Loperamide hydrochloride is an opioid receptor agonist for the treatment of diarrhea[1].
Celecoxib-d7 is the deuterium labeled Celecoxib. Celecoxib,a selective non-steroidal anti-inflammatory drug (NSAID), is a selective COX-2 inhibitor with an IC50 of 40 nM[1][2].
Edaravone-d5 is a deuterium labeled Edaravone. Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator[1][2][3][4].
Vandetanib-d6 is the deuterium labeled Vandetanib. Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM)[1].
Pimozide-d4 is a deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5[1][2][3].
Abemaciclib-d8 is the deuterium labeled Abemaciclib. Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.
Dimethyl phthalate-d6 is the deuterium labeled Dimethyl phthalate. Dimethyl phthalate, a known endocrine disruptor and one of the phthalate esters (PAEs), is a ubiquitous pollutant. Dimethyl phthalate is commonly used as a plasticizer to impart flexibility to rigid polyvinylchloride (PVC) resins[1].
Cinacalcet-d4 (AMG-073-d4) hydrochlorideis deuterium labeled Cinacalcet (hydrochloride). Cinacalcet hydrochloride (AMG-073 hydrochloride) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment .
Remdesivir-d5 is a deuterium labeled Remdesivir. Remdesivir (GS-5734) is a nucleoside analogue, with effective antiviral activity, with EC50s of 74 nM for SARS-CoV and MERS-CoV in HAE cells, and 30 nM for murine hepatitis virus in delayed brain tumor cells. Remdesivir is highly effective in the control of 2019-nCoV (COVID-19) infection in vitro[1][2].
Lenalidomide-d5 is deuterium labeled Lenalidomide. Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells[1][2].
Capsaicin-d7 is deuterated labeled Capsaicin (HY-10448). Capsaicin ((E)-Capsaicin), an active component of chili peppers, is a TRPV1 agonist. Capsaicin has pain relief, antioxidant, anti-inflammatory, neuroprotection and anti-cancer effects .
Valproic acid-d14 (sodium) is deuterium labeled Valproic acid (sodium). Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium salt activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
N-Ethylmaleimide-d5 is the deuterium labeled N-Ethylmaleimide. N-Ethylmaleimide (NEM), a reagent that alkylates free sulfhydryl groups, is a cysteine protease inhibitor[1]. N-ethylmaleimide specific inhibits phosphate transport in mitochondria[2]. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor[3].
Atazanavir-d6 is deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration[1]. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)[2]. Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM[3].
Ubrogepant-d5 (MK-1602-d5) is deuterium labeled Ubrogepant. Ubrogepant (MK-1602) is an orally active and selective antagonist of calcitonin gene-related peptide receptor (CGRP). Ubrogepant has high affinity for CGRP receptors in human and rhesus monkeys, and can effectively block the cAMP response stimulated by α-CGRP. Ubrogepant can be used in the study of acute migraine [3].
Acipimox-d4 is the deuterium labeled Acipimox. Acipimox (K-9321), a nicotinic acid analogue, is an antilipolytic compound. Acipimox acutely inhibits lipolysis and suppresses systemic levels of free fatty acids (FFAs) and improves insulin sensitivity .
Lurasidone-d8 is deuterium labeled Lurasidone. Lurasidone (SM-13496) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (SM-13496) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.
Afatinib-d4 is the deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.
Buformin-d9 (hydrochloride) is the deuterium labeled Buformin. Buformin (1-Butylbiguanide), a potent AMPK activator, acts as an orally active biguanide antidiabetic agent. Buformin decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al)[1].
Hydroxymetronidazole-d4 is the deuterium labeled Hydroxymetronidazole. Hydroxymetronidazole (Metronidazole-OH) is a metabolite of Metronidazole belonging to the class of nitroimidazoles. Hydroxymetronidazole can be used for the research of certain bacterial and protozoal diseases in poultry, swine dysentery and genital trichomoniasis in cattle[1].
(R)-Lansoprazole-d4 is deuterium labeled (R)-Lansoprazole. (R)-Lansoprazole is the R enantiomer of Lansoprazole, Lansoprazole (AG 1749) is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[1][2].
Olmesartan-d6 (RNH-6270-d6) is the deuterium labeled Olmesartan. Olmesartan (RNH-6270) is an angiotensin II receptor (AT1R) antagonist used to treat high blood pressure[1][2].
Ramelteon-d5 is deuterium labeled Ramelteon. Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation[1][2].
Vapendavir-d5 is the deuterium labeled Vapendavir. Vapendavir (BTA798) is a potent enteroviral capsid binder (CB). Vapendavir (BTA798) possesses potent antiviral activity for enterovirus 71 (EV71) replication, with EC50 values of 0.5-1.4 μM in different EV71 strains .
Flurbiprofen-d5 is the deuterium labeled Flurbiprofen. Flurbiprofen (dl-Flurbiprofen) is a potent, orally active nonsteroidal anti-inflammatory agent (NSAIA/NSAID), with antipyretic and analgesic activities. Flurbiprofen is commonly used for the research of inflammatory diseases, including osteoarthritis and rheumatoid arthritis. Flurbiprofen is a non-selective cyclooxygenase (COX) inhibitor that can be used for the research of colorectal cancer[1][2][3].
Levamisole-d5 (hydrochloride) is the deuterium labeled Levamisole hydrochloride. Levamisole ((-)-Tetramisole) hydrochloride is an anthelmintic and immunomodulator belonging to a class of synthetic imidazothiazole derivatives. Levamisole hydrochloride has antiviral effects against HSV[1][2].
Rabeprazole-d4 potassium is deuterated labeled Rabeprazole sodium (HY-B0656A). Rabeprazole sodium (LY307640 sodium) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H +/K +-ATPase. Rabeprazole sodium induces apoptosis. Rabeprazole sodium acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole sodium can be used for the research of gastric ulcerations and gastroesophageal reflux [3].
Permethrin-d5 (NRDC-143-d5) is the deuterium labeled Permethrin. Permethrin (NRDC-143) is an insecticide, acaricide, and insect repellent; functions as a neurotoxin, affecting neuron membranes by prolonging sodium channel activation[1][2].
Gefitinib-d6 is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity[1][2].
Ketoprofen-d4 is the deuterium labeled Ketoprofen. Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC50s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively[1].
Macitentan-d4 is a deuterium labeled Sulfamethoxazole. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin) receptor antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH)[1].
Nintedanib-d8 is deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
Sarpogrelate-d4 (MCI-9042-d4) hydrochloride is deuterium labeled Sarpogrelate (hydrochloride). Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis [3] .
Rupintrivir-d7 is a deuterated labeled Rupintrivir . Rupintrivirvr (AG7088), an antiviral agent, is a potent, selective and irreversible inhibitor of human rhinovirus (HRV) 3C protease. Rupintrivirvr inhibits replication of a panel of 48 different HRV serotypes in H1-HeLA and MRC-5 cell protection assays, with a mean EC50 of 0.023 μM. Rupintrivirvr shows immune-modulatory effect [3].
Famotidine-d4 (MK-208-d4) is deuterium labeled Famotidine. Famotidine (MK-208) is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion .
Desloratadine-d9 is the deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities[1][2].
Simvastatin-d6 (MK 733-d6) is the deuterium labeled Simvastatin. Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.
Ertugliflozin-d5 is the deuterium labeled Ertugliflozin[1]. Ertugliflozin (PF-04971729) is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), with an IC50 of 0.877 nM for h-SGLT2[2]. Has the potential for the treatment of type 2 diabetes mellitus[3].
Famciclovir-d4 is the deuterium labeled Famciclovir. Famciclovir (BRL 42810) is a guanine analogue antiviral agent used for the treatment of various herpesvirus infections[1][2].
Methoprene-d7 is the deuterium labeled Methoprene[1]. Methoprene, an insect juvenile growth hormone mimic, is a growth-regulating insecticide that manifests its toxicity to target organisms by acting as a juvenile hormone agonist[2][3].
Levocetirizine-d4 (dihydrochloride) is the deuterium labeled Levocetirizine. Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria[1].
Olanzapine-d8 is a deuterated labeled Olanzapine . Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic [3].
Spironolactone-d7 is the deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC50 of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes[1][2][3].
Latanoprost-d4 is the deuterium labeled Latanoprost. Latanoprost (PHXA41) is a prostaglandin F2α analogue and an agonist for the FP prostanoid receptor, and lowers intraocular-pressure (IOP).
Terbuthylazine-desethyl-d9 is the deuterium labeled Terbuthylazine-desethyl[1]. Terbuthylazine-desethyl (Desethylterbuthylazine) is a chloro dealkylated metabolite of Terbuthylazine (a triazine herbicide)[2][3].
Probucol-d6 is deuterium labeled Probucol. Probucol (DH-581) is an anti-hyperlipidemic agent by lowering the level of cholesterol in the bloodstream by increasing the rate of LDL catabolism.
Meropenem-d6 is the deuterium labeled Meropenem. Meropenem (SM 7338) is a carbapenem antibiotic with broad-spectrum antibacterial activity. Meropenem has activity against susceptible and resistant N. gonorrhoeae (MIC value of 0.02-0.06 mg/mL), H. influenzae (MIC value of 0.03-0.12 mg/mL), and H. ducreyi (MIC value of 0.015-0.12 mg/mL)[1][2].
Brinzolamide-d5 (hydrochloride) is the deuterium labeled Brinzolamide hydrochloride[1]. Brinzolamide (AL-4862) hydrochloride is a selective carbonic anhydrase II inhibitor with an IC50 value of 3.2 nM. Brinzolamide hydrochloride reduces intraocular pressure (IOP) by inhibiting ciliary CA-II and decreasing atrial fluid secretion. Brinzolamide hydrochloride can be used in glaucoma disease research[2][3].
Ethylenediaminetetraacetic acid-d16 is the deuterium labeled Ethylenediaminetetraacetic acid[1]. Ethylenediaminetetraacetic acid (EDTA) is a metal chelators (binds to metal divalent and trivalent cations including calcium), which shows activities of anticoagulant and anti-hypercalcemic. Ethylenediaminetetraacetic acid decreases the metal ion-catalyzed oxidative damage to proteins, and allows maintenance of reducing environment during protein purification. Ethylenediaminetetraacetic acid can also decrease the formation of disulfide bonds[2][3][4].
Sitagliptin-d4 (MK-0431-d4) is deuterium labeled Sitagliptin. Sitagliptin (MK-0431) is a potent and orally active inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts .
Palbociclib-d4 (hydrochloride) is the deuterium labeled Palbociclib hydrochloride. Palbociclib (PD 0332991) is a selective CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research[1].
Sacubitril-d4 is the deuterium labeled Sacubitril. Sacubitril (AHU-377) is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril (AHU-377) is a component of the heart failure medicine LCZ696.
Azimilide-d8 (dihydrochloride) is the deuterium labeled Azimilide dihydrochloride. Azimilide Dihydrochloride (NE-10064 Dihydrochloride) is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.
Pioglitazone-d4 is a deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively[1].
Rosiglitazone-d4 is deuterated labeled Rosiglitazone (HY-17386). Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone is an TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer .
Ivacaftor-d9 is a potent CFTR modulator and exhibits an EC50 value of 255 nM for CFTR potentiation in G551D/F508del HBE Cells. Ivacaftor-D9 acts as an orally active and improved deuterated Ivacaftor analog for cystic fibrosis research[1].
Losartan-d6 hydrochloride is deuterated labeled Losartan potassium (HY-17512A). Losartan potassium (DuP-753 potassium) is an angiotensin II receptor type 1 (AT1) antagonist, competing with the binding of angiotensin II to AT1 with an IC50 of 20 nM.
Moxonidine-d7 is deuterated labeled Moxonidine (HY-B0374). Moxonidine (BDF5895) is an imidazoline type 1 receptor (I1-R) selective agonist and antihypertensive agent.
Telaprevir-d4 is the deuterium labeled Telaprevir. Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide[1][2][3]. Telaprevir inhibits SARS-CoV-2 3CLpro activity[4].
Dabigatran-d4 (hydrochloride) is deuterium labeled Dabigatran, which is a reversible and selective, direct thrombin inhibitor (DTI) with a Ki value of 4.5 nM.
Remdesivir-d4 is deuterium labeled Remdesivir. Remdesivir (GS-5734), a nucleoside analogue with effective antiviral activity, has EC50s of 74 nM for SARS-CoV and MERS-CoV in HAE cells, and 30 nM for murine hepatitis virus in delayed brain tumor cells. Remdesivir is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro[1][2].
Finasteride-d9 is deuterium labeled Finasteride. Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia[1][2][3].
Odanacatib-d4 is the deuterium labeled Odanacatib (HY-10042). Odanacatib is a potent and selective inhibitor of cathepsin K, with an IC50 of 0.2 nM for human cathepsin K .
Ledipasvir-d6 is the deuterium labeled Ledipasvir. Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.62 μM[3].
Amitraz-d6 (BTS-27419-d6) is the deuterium labeled Amitraz. Amitraz is a non-systemic acaricide and insecticide, with alpha-adrenergic agonist activity, interaction with octopamine receptors of the central nervous system and inhibition of monoamine oxidases and prostaglandin synthesis.
DL-dithiothreitol-d10 is the deuterated form of DL-dithiothreitol. DL-dithiothreitol (DTT) is a strong reductant with anti-disulfidptosis activity. When DL-dithiothreitol is oxidized, it forms a stable six-membered ring with an internal disulfide bond .
Sitagliptin-d4 (hydrochloride) is the deuterium labeled Sitagliptin[1]. Sitagliptin (MK-0431) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts[2].
Losartan-d4 is the deuterium labeled Losartan. Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.
Nicardipine-d4 hydrochloride is deuterated labeled Nicardipine hydrochloride (HY-12515A). Nicardipine hydrochloride (YC-93) is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine hydrochloride acts as an agent for chronic stable angina and for controlling blood pressure .
1-Octanol-d2 is the deuterium labeled 1-Octanol[1]. 1-Octanol (Octanol), a saturated fatty alcohol, is a T-type calcium channels (T-channels) inhibitor with an IC50 of 4 μM for native T-currents[2]. 1-Octanol is a highly attractive biofuel with diesel-like properties[3].
Enasidenib-d6 (AG-221-d6) is the deuterium labeled Enasidenib (HY-18690) . Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2 R140Q and IDH2 R172K, respectively .
Miconazole-d2 is the deuterium labeled Miconazole[1]. Miconazole (R18134) is an imidazole antifungal agent. Miconazole also has antibacterial effects[2][3].
Ribociclib-d6 is a deuterium labeled Ribociclib. Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex[1].
Hydroxymetronidazole-d2 is the deuterium labeled Hydroxymetronidazole(HY-136440).Hydroxymetronidazole (Metronidazole-OH) is a metabolite of Metronidazole belonging to the class of nitroimidazoles. Hydroxymetronidazole can be used for the research of certain bacterial and protozoal diseases in poultry, swine dysentery and genital trichomoniasis in cattle .
Debutyldronedarone-d7 is deuterium labeled Debutyldronedarone. Debutyldronedarone is a major circulating active metabolite of dronedarone (HY-A0016) in humans.Debutyldronedarone exhibits a potency that is 1/10 to 1/3 of that of the parent agent[1][2].
Dapoxetine-d6 (LY-210448-d6) hydrochloride is the deuterium labeled Dapoxetine hydrochloride. Dapoxetine hydrochloride is a short-acting selective serotonin reuptake inhibitor (SSRI)
Brexpiprazole-d8 (OPC-34712-d8) is the deuterium labeled Brexpiprazole (HY-15780). Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM) [3].
Arachidonic acid-d8 is the deuterium labeled Arachidonic acid. Arachidonic acid is an essential fatty acid and a major constituent of biomembranes[1][2].
Ivacaftor-d9 is a potent CFTR modulator and exhibits an EC50 value of 255 nM for CFTR potentiation in G551D/F508del HBE Cells. Ivacaftor-D9 acts as an orally active and improved deuterated Ivacaftor analog for cystic fibrosis research .
Atazanavir-d9 is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration[1]. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)[2]. Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM[3].
Crizotinib-d5 is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition [3].
Ivacaftor-d18 is the deuterium labeled Ivacaftor[1]. Ivacaftor (VX-770) is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively[2].
Alfuzosin-d6 (SL 77499-d6) is deuterium labeled Alfuzosin. Alfuzosin (SL 77499-10) is an orally active, selective and competitive α1-adrenoceptor antagonist. Alfuzosin relaxes the muscles of the prostate and bladder neck, aiding in urination. Alfuzosin can be used in study of benign prostatic hyperplasia (BPH) [3].
2-Iodoacetamide-d4 is the deuterium labeled 2-Iodoacetamide[1]. 2-Iodoacetamide (Iodoacetamide), an alkylating agent, is a commonly used agent for alkylation of cysteine during sample preparation for proteomics[2][3].
Rabeprazole-d4 is a deuterium labeled Rabeprazole. Rabeprazole is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H+/K+-ATPase. Rabeprazole induces apoptosis. Rabeprazole acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole can be used for the research of gastric ulcerations and gastroesophageal reflux[1][2][3].
Clozapine-d4 is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors[1][2][3][4][5].
Chenodeoxycholic acid-d5 is the deuterium labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
Ticlopidine-d4 is the deuterium labeled Ticlopidine. Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively[1]. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively[2][3].
Quetiapine-d4 (hydrochloride) (ICI204636-d4 (hydrochloride)) is deuterium labeled Quetiapine. Quetiapine (ICI204636) is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
Pirfenidone-d5 is a deuterium labeled Pirfenidone. Pirfenidone is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone has growth-inhibitory effect and reduces TGF-β2 protein levels in human glioma cell lines. Pirfenidone also has anti-inflammatory activities[1][2][3].
Ponesimod-d4 (ACT-128800-d4) is the deuterium labeled Ponesimod (HY-10569) . Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation [3] .
Sotalol-d6 is the deuterium labeled Sotalol. Sotalol is an orally active, non-selective β-adrenergic receptor blocker. Sotalol is a potent antiarrhythmic agent that can be used for the research of pediatric arrhythmias. Sotalol blocks β-receptors, and potassium KCNH2 channels. Antiepileptic Agent[1][2][3][4].
Flecainide-d4 (acetate) is the deuterium labeled Flecainide acetate. Flecainide acetate (R-818) is a class 1C antiarrhythmic agent especially used for the management of supraventricular arrhythmia; works by blocking the Nav1.5 sodium channel in the heart, causing prolongation of the cardiac action potential[1][2].
Glycochenodeoxycholic acid-d4 is the deuterium labeled Glycochenodeoxycholic acid. Glycochenodeoxycholic acid (Chenodeoxycholylglycine) is a bile acid formed in the liver from chenodeoxycholate and glycine. It acts as a detergent to solubilize fats for absorption and is itself absorbed. Glycochenodeoxycholic acid (Chenodeoxycholylglycine) induces hepatocyte apoptosis[1][2].
Prasugrel-d4 is the deuterium labeled Prasugrel[1]. Prasugrel (PCR 4099), a thienopyridine and proagent, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation[2].
Apalutamide-d7 is deuterated labeled Apalutamide (HY-16060). Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM .
Delamanid-d4 is the deuterium labeled Delamanid. Delamanid, a newer mycobacterial cell wall synthesis inhibitor, inhibits the synthesisi of mucolic acids[1].
Tylvalosin-d9 (Acetylisovaleryltylo?sin-d9) is the deuterium labeled Tylvalosin (HY-128423A) . Tylvalosin is a third-generation macrolide, with anti-inflammatory property. Tylvalosin decreases the levels of IL-8, IL-6, IL-1β, PGE2, TNF-α and NO, and reduces the inflammatory cells recruitment and activation in mouse acute lung injury model .
Ciprofloxacin-d8 (hydrochloride) is the deuterium labeled Ciprofloxacin. Ciprofloxacin (Bay-09867) hydrochloride is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
Ropinirole-d7 (hydrochloride) is the deuterium labeled Ropinirole hydrochloride[1]. Ropinirole (SKF 101468) hydrochloride is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease[2][3].
Glasdegib-d4 (PF-04449913-d4) is deuterium labeled Glasdegib. Glasdegib (PF-04449913) is a potent and orally bioavailable smoothened inhibitor. Glasdegib (PF-04449913) binds to human SMO (amino acids 181-787) with an IC50 of 4 nM .
(R)-Oxybutynin-d10 (Aroxybutynin-d10) is deuterium labeled (R)-Oxybutynin. (R)-Oxybutynin (Aroxybutynin) is the racemic isomer of Oxybutynin and an orally active muscarinic receptor antagonist. (R)-Oxybutynin has antispasmodic, antimuscarinic, and anticholinergic activities and competitively antagonizes carbachol-induced contractions. (R)-Oxybutynin can be used to study urinary incontinence caused by neurogenic bladder dysfunction [3] .
Dapoxetine-d7 (hydrochloride) is the deuterium labeled Dapoxetine hydrochloride. Dapoxetine hydrochloride is a short-acting selective serotonin reuptake inhibitor (SSRI)[1].
Bazedoxifene-d4 is deuterium labeled Bazedoxifene. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[1][2].
Lusutrombopag-d13 is deuterium labeled Lusutrombopag. Lusutrombopag is an orally bioavailable thrombopoietin (TPO) receptor agonist, used for treatment of chronic liver disease.
Biperiden-d5 (KL 373-d5) is deuterium labeled Biperiden. Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders .
Tecovirimat-d4 (ST-246-d4) is a deuterium-labelled Tecovirimat (HY-14805). Tecovirimat is an orally bioavailable and selective compound against orthopoxviruses [including vaccinia, monkeypox, camelpox, cowpox, ectromelia (mousepox), smallpox and variola viruses]. Tecovirimat is evaluated against vaccinia, cowpox virus, ectromelia virus with EC50 values of 0.01 μM, 0.48 μM and 0.05 μM, respectively. Tecovirimat targets the orthopoxvirus protein VP37 which is necessary for membrane envelopment of intracellular mature virus particles to form enveloped virus. Tecovirimat exerts antiviral activity on the target of the cowpox virus V061 gene, which is homologous to vaccinia virus F13L, encoding a major envelope protein (p37) required for production of extracellular virus. Tecovirimat could be used in the study for orthopoxvirus-induced diseases [3] .
Teneligliptin-d8 is a deuterium labeled Teneligliptin (MP-513). Teneligliptin is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor[1].
Prasugrel-d5 is deuterium labeled Prasugrel. Prasugrel (PCR 4099), a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation[1].
Eliglustat-d4 is the deuterium labeled Eliglustat. Eliglustat is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC50 of 24 nM[1][2].
Linagliptin-d4 is deuterium labeled Linagliptin. Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM. Linagliptin-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Levocetirizine-d4 ((R)-Cetirizine-d4) is the deuterium-labeled Levocetirizine (HY-B0814) . Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptorthan (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria .
Erdosteine-d4 is a deuterium labeled Erdosteine (HY-B0289). Erdosteine has muco-modulatory, anti-bacterial, anti-inflammatory and anti-oxidant effects[1].
Diclazuril-d4 is deuterium labeled Diclazuril. Diclazuril (R-64433), a benzeneacetonitrile derivative, is a potent and orally active anticoccidial agent. Diclazuril can be used for the research of certain infectious and parasitic diseases, including coccidiosis, acute toxoplasmosis, equine protozoal pyoencephalitis (EPM) et.al[1][2].
Piracetam-d6 is deuterium labeled Piracetam. Piracetam (UCB-6215) is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders.
Meclofenamic acid-d4 is the deuterium labeled Meclofenamic acid. Meclofenamic Acid (Meclofenamate), a non-steroidal, anti-inflammatory agent, is a highly selective fat mass and obesity-associated (FTO) enzyme inhibitor. Meclofenamic Acid competes with FTO binding for the m(6)A-containing nucleic acid. Meclofenamic acid is a non-selective gap-junction blocker[1][2][3].
Ruxolitinib-d9 (INCB18424-d9) is deuterium labeled Ruxolitinib. Ruxolitinib (INCB18424) is an orally active and selective JAK1/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3 . Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy[3].
Glycocyamine-d2 is the deuterium labeled Glycocyamine. Glycocyamine (Guanidinoacetic acid), a precursor of creatine, is a replacement of dietary arginine and could support overall energy homeostasis of the bird.
Butenafine-d4 (KP363-d4) is the deuterium labeled Butenafine (HY-114518). Butenafine (KP363) is a potent and broad spectrum benzylamine antifungal agent . Butenafine inhibits fungal ergosterol biosynthesis at the point of squalene epoxidation, leading to a deficiency of the fungal cell membranes. Butenafine is effective against dermatophytes infections, such as ?tinea pedis, ?tinea cruris, tinea versicolor .
Varenicline-d4 is deuterium labeled Varenicline. Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively[1]. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment[2].
Ziprasidone-d88 is deuterium labeled Ziprasidone, which is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.
Albendazole-d7 is the deuterium labeled Albendazole. Albendazole is a broad-spectrum parasiticide with high effectiveness and low host toxicity. Albendazole is used for the research gastrointestinal parasites in humans and animals[1][2].
Elacestrant-d6 (RAD1901-d6) is a deuterated labeled Elacestrant (HY-19822). Elacestrant is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER + breast cancer cell lines both in vitro and in vivo.
Dexpanthenol-d6 is deuterium labeled D-Panthenol. D-Panthenol is the biologically-active alcohol of pantothenic acid, which leads to an elevation in the amount of coenzyme A in the cell.
Emodin-d4 is the deuterium labeled Emodin. Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction[1]. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects[2]. Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice[3].
Valsartan-d9 is deuterium labeled valsartan. Valsartan is an angiotensin II receptor antagonist and has the potential for high blood pressure and heart failure research[1].
Elacestrant-d4 (RAD1901-d4) is a deuterated labeled Elacestrant (HY-19822). Elacestrant (RAD1901) is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER + breast cancer cell lines both in vitro and in vivo.
Biperiden-d5 (hydrochloride) is the deuterium labeled Biperiden hydrochloride. Biperiden (KL 373) hydrochloride is an antiparkinsonian agent, which is the selective central M1 cholinoreceptors blocker.
Methylprednisolone-d4 is deuterium labeled Methylprednisolone. Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels[3].
Tulobuterol-d9 (hydrochloride) is the deuterium labeled Tulobuterol. Tulobuterol (C-78 free base) is a long-acting β2-adrenoceptor agonist, which reduces the frequency of exacerbations of chronic obstructive pulmonary disease and bronchial asthma. Tulobuterol is also a sympathomimetic agent used as a transdermal patch, and increases normal diaphragm muscle strength[1].
Dasatinib-d4 (BMS-354825-d4) is deuterium labeled Dasatinib. Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib also induces apoptosis and autophagy.
Methazolamide-d6 is the deuterium labeled Methazolamide. Methazolamide (L584601) is a sulfonamide derivative used as a carbonic anhydrase inhibitor with a Ki of 14 nM for human carbonic anhydrase II. Methazolamide, an intraocular pressure-lowering agent, reduces intraocular pressure elevations associated with glaucoma and other ocular disorders[1][2].
Promethazine-d6 (hydrochloride) is the deuterium labeled Promethazine hydrochloride. Promethazine hydrochloride is an orally active histamine receptor antagonist[1][2].
Licofelone-d6 is the deuterium labeled Licofelone[1]. Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC50=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins[2][3][4].
Ribociclib-d6 (hydrochloride) is a deuterium labeled Ribociclib. Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex[1].
Sildenafil-d8 is the deuterium labeled Sildenafil. Sildenafil (UK-92480) is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM[1][2].
Guaiacol-d4 is the deuterium labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
(±)-Darifenacin-d4 is deuterium labeled (±)-Darifenacin. (±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist[1].
Pemigatinib-d6 (INCB054828-d6) is deuterium labeled Pemigatinib. Pemigatinib (INCB054828) is an orally active, selective FGFR inhibitor with IC50s of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma [3].
Teneligliptin-d4 is deuterium labeled Teneligliptin. Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM[1].
Pomalidomide-d5 is deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.
Palbociclib-d4 is deuterium labeled Palbociclib. Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma [3] .
Donepezil-d4 (hydrochloride) is the deuterium labeled Donepezil hydrochloride. Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE[1]. Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity[2].
Aprocitentan-d4 is a deuterium labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is an orally active dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively. Aprocitentan is an antihypertensive agent .
Apremilast-d5 is a deuterium labeled Apremilast. Apremilast is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM[1].
Ribociclib-d8 is the deuterium labeled Ribociclib[1]. Ribociclib (LEE01) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex[2].
Itraconazole-d9 is the deuterium labeled Itraconazole[1]. Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor[2][3][4][5].
Cilnidipine-d7 is deuterium labeled Cilnidipine. Cilnidipine is a long-acting, second-generation dihydropyridine Ca2+-channel blocker on L and N-type Ca2+ channel[1][2][3][4]. Antihypertensive effects[5].
Ciprofloxacin-d8 (hydrochloride monohydrate) is the deuterium labeled Ciprofloxacin (hydrochloride monohydrate). Ciprofloxacin hydrochloride is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
Cabergoline-d6 is deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).
Ciprofloxacin-d8 is the deuterium labeled Ciprofloxacin. Ciprofloxacin (Bay-09867) is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
Fluconazole-d4 is the deuterium labeled Fluconazole. Fluconazole (UK-49858) is a triazole antifungal agent with excellent activities against a broad range of fungi, especially against Candida albicans. Fluconazole inhibits C. albicans and Candida kefyr with IC99s range from 0.20 μg/mL to 0.39 μg/mL[1].
Nemonoxacin-d4 is the deuterium labeled Nemonoxacin. Nemonoxacin (TG-873870) is an orally active and potent broad-spectrum antibiotic. Nemonoxacin shows good inhibitory activity against different species of staphylococci, streptococci, and enterococci, Neisseria gonorrhoeae, and Haemophilus influenza. Nemonoxacin can be used in the study of bacterial infections and community-acquired pneumonia[1][2][3].
Piroxicam-d4 is the deuterium labeled Piroxicam. Piroxicam (CP-16171) is a non-steroidal anti-inflammatory drugs, acts as a COX inhibitor, with IC50s of 47, 25 μM for human monocyte COX-1 and COX-2, respectively.
Debutyldronedarone-d6 (hydrochloride) is deuterium labeled Debutyldronedarone. Debutyldronedarone is a major circulating active metabolite of dronedarone (HY-A0016) in humans. Debutyldronedarone exhibits a potency that is 1/10 to 1/3 of that of the parent agent[1][2].
Didesethyl chloroquine-d4 is the deuterium labeled Didesethyl chloroquine. Didesethyl chloroquine (Bisdesethylchloroquine) is a major metabolite of the antimalarial agent Chloroquine. Didesethyl chloroquine is a potent myocardial depressant[1][2].
Valsartan-d8 is the deuterium labeled Valsartan. Valsartan (CGP 48933) is an angiotensin II receptor antagonist and has the potential for high blood pressure and heart failure research[1].
Methylprednisolone-d7 is deuterium labeled Methylprednisolone. Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels[3].
Relugolix-d6 is deuterium labeled Relugolix. Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209)[1]. Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al[2].
Bazedoxifene-d4 (acetate) is the deuterium labeled Bazedoxifene[1]. Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer[2][3].
Gilteritinib-d8 is deuterium labeled Gilteritinib. Gilteritinib (ASP2215) is a potent and ATP-competitive FLT3/AXL inhibitor with IC50s of 0.29 nM/0.73 nM, respectively.
Sarafloxacin-d8 (A-56620-d8) hydrochloride is the deuterium labeled Sarafloxacin hydrochloride. Sarafloxacin hydrochloride (A-56620 hydrochloride) is a quinolone antibiotic drug.
Moclobemide-d4 is deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A[1].Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
Terbinafine-d7 is the deuterium labeled Terbinafine. Terbinafine (TDT 067) is an antifungal medication used to treat fungal infections. It is a potent non-competitive inhibitor of squalene epoxidase from Candida with a Ki of 30 nM[1][2]. Terbinafine also antibacterial activity against certain Gram-positive and Gram-negative bacteria[3].
Clozapine-d8 is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors[1][2][3][4].
Moclobemide-d8 (Ro111163-d8) is the deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A .Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
Oxprenolol-d7 (hydrochloride) is the deuterium labeled Oxprenolol hydrochloride. Oxprenolol hydrochloride (Ba 39089) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle[1].
Carteolol-d9 (hydrochloride) is the deuterium labeled Carteolol hydrochloride. Carteolol hydrochloride (OPC-1085 hydrochloride) is a non-selective beta blocker used to treat glaucoma[1][2].
Mavatrep-d6 (JNJ-39439335-d6) is a deuterated labeled Mavatrep (HY-16935). Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with high affinity for hTRPV1 channels (Ki=6.5 nM). Mavatrep antagonizes capsaicin-induced Ca 2+ influx with an IC50 value of 4.6 nM. Mavatrep can be used in some studies of neuropathic pain .
Lisinopril-d5 is the deuterium labeled Lisinopril. Lisinopril (MK-521) is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks.
Pazopanib-d6 is the deuterium labeled Pazopanib. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
Atenolol-d7 is the deuterium labeled Atenolol. Atenolol ((RS)-Atenolol) is a cardioselective β1-adrenergic receptor blocker, with a Ki of 697 nM atβ1-adrenoceptor in guine pig left ventricle membrane. Atenolol can be used for the research of hypertension and angina pectoris[1][2].
Tazarotene-d8 is the deuterium labeled Tazarotene. Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris[1][2].
Filgotinib-d4 is the deuterium labeled Filgotinib. Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.
Empagliflozin-d4 is deuterium labeled Empagliflozin. Empagliflozin (BI 107730 is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor with an IC50 of 3.1 nM for human SGLT-2[1].
Tranylcypromine-d5 (hydrochloride) is a deuterium labeled (rel)-Tranylcypromine hydrochloride. Tranylcypromine hydrochloride is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. Tranylcypromine hydrochloride is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis[1][2].
Edoxaban-d6 is deuterium labeled Edoxaban. Edoxaban (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and can be used for stroke prevention. Edoxaban is also a weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10000-fold selectivity for FXa. Edoxaban has antithrombotic properties and has potential for thromboembolic diseases treatment [3].
Donepezil-d7 (hydrochloride) is the deuterium labeled Donepezil. Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively[1].
Venlafaxine-d6 (hydrochloride) is the deuterium labeled Venlafaxine hydrochloride. Venlafaxine hydrochloride (Wy 45030 hydrochloride) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant[1].
Bimatoprost-d4 is the deuterium labeled Bimatoprost. Bimatoprost is a prostaglandin analog used topically (as eye drops) to control the progression of glaucoma and in the management of ocular hypertension.
Docetaxel-d9 is the deuterium labeled Docetaxel. Docetaxel (RP-56976) is a microtubule depolymerization inhibitor, with an IC50 of 0.2 μM. Docetaxel attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel arrests the cell cycle at G2/M and leads to cell apoptosis. Docetaxel has anti-cancer activity[1][3].
Adinazolam-d5 is a deuterium labeled Adinazolam (HY-A0198). Adinazolam, a triazolobenzodiazepine, has dual anxiolytic and antidepressant activities[1].
Tezacaftor-d4 (VX-661-d4) is the deuterium-labeled Tezacaftor (HY-15448), a F508del CFTR corrector. Tezacaftor helps CFTR protein reach the cell surface .
Betaxolol-d7 (hydrochloride) is the deuterium labeled Betaxolol hydrochloride. Betaxolol Hydrochloride is a selective beta1 adrenergic receptor blocker that can be used for the research of hypertension and glaucoma.
EDTA-d12 is the deuterium labeled Ethylenediaminetetraacetic acid[1]. Ethylenediaminetetraacetic acid (EDTA) is a metal chelators (binds to metal divalent and trivalent cations including calcium), which shows activities of anticoagulant and anti-hypercalcemic. Ethylenediaminetetraacetic acid decreases the metal ion-catalyzed oxidative damage to proteins, and allows maintenance of reducing environment during protein purification. Ethylenediaminetetraacetic acid can also decrease the formation of disulfide bonds[2][3][4].
Hyodeoxycholic acid-d5 is the deuterium labeled Hyodeoxycholic acid. Hyodeoxycholic acid is a secondary bile acid formed in the small intestine by the gut flora, and acts as a TGR5 (GPCR19) agonist, with an EC50 of 31.6 µM in CHO cells.
Doxazosin-d8 is a deuterium labeled Doxazosin (UK 33274). Doxazosin is a quinazoline-derivative that selectively antagonizes postsynaptic α1 adrenergic receptors[1].
Sunitinib-d10 is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
Cobicistat-d8 (GS-9350-d8) is a deuterated version of Cobicistat (HY-10493). Cobicistat is a potent and selective inhibitor of cytochrome P450 3A (CYP3A) with IC50 values of 30-285 nM. Cobicistat is a pharmacokinetic enhancer that enhances the absorption of anti-HIV active molecules [3].
Cabergoline-d5 is the deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively)[1][2].
Itopride-d6 (hydrochloride) is deuterium labeled Itopride (hydrochloride). Itopride hydrochloride (HSR803), a gastroprokinetic Benzamide (HY-Z0283) derivative, is an inhibitor of acetylcholinesterase (AChE) and dopamine D2 receptor[1][2].
Chenodeoxycholic Acid-d9 is the deuterium labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
Dacarbazine-d6 is the deuterium labeled Dacarbazine. Dacarbazine(DTIC-Dome; DTIC) is an antineoplastic agent. It has significant activity against melanomas.
Telmisartan-d7 (BIBR 277-d7) is a deuterium labeled Telmisartan (HY-13955). Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
Ponatinib-d8 is a deuterium labeled Ponatinib. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
Flurbiprofen-d4 is deuterated labeled Flurbiprofen (HY-10582). Flurbiprofen (dl-Flurbiprofen) is a potent, orally active nonsteroidal anti-inflammatory agent (NSAIA/NSAID), with antipyretic and analgesic activities. Flurbiprofen is commonly used for the research of inflammatory diseases, including osteoarthritis and rheumatoid arthritis. Flurbiprofen is a non-selective cyclooxygenase (COX) inhibitor that can be used for the research of colorectal cancer [3].
Pranlukast-d4 is deuterium labeled Pranlukast. Pranlukast is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [3H]LTE4, [3H]LTD4, and [3H]LTC4 bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.
Imiquimod-d9 is deuterium labeled Imiquimod. Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19[1][2].
Adenosine- 15N5 (Adenine riboside- 15N5; D-Adenosine- 15N5) is the 15N labled Adenosine (HY-B0228). Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation .
L-Theanine-d5 is the deuterium labeled L-Theanine. L-Theanine (L-Glutamic Acid γ-ethyl amide）is a non-protein amino acid contained in green tea leaves, which blocks the binding of L-glutamic acid to glutamate receptors in the brain, and with neuroprotective and anti-oxidative activities. L-Theanine causes anti-stress effects via the inhibition of cortical neuron excitation by oral intake[1][2][3].
Promethazine-d4 is a deuterated-labeled promethazine (HY-B0781). Promethazine is an orally active H1 receptor and mAChR antagonist with antihistamine (H1), sedative, antiemetic, anticholinergic, and anti-motion sickness properties [3] .
Artemisinin- 13C,d4 is 13C and deuterated labeled Artemisinin (HY-B0094). Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants . Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects .
Vitamin D3- 13C5 is the deuterium labeled Vitamin D3 (HY-15398). Vitamin D3 (Cholecalciferol) is a naturally occuring form of vitamin D. Vitamin D3 induces cell differentiation and prevents proliferation of cancer cells[1][2].
L-Glutamine- 15N2,d5 is the deuterium and 15N-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells[1][2].
Resveratrol- 13C6 is the 13C-labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].
Vitamin K1- 13C6 is the 13C-labeled Vitamin K1. Vitamin K1 a naturally occurring vitamin required for blood coagulation and bone and vascular metabolism.
Adenosine- 13C10 (Adenine riboside- 13C10; D-Adenosine- 13C10) is 13C-labeled Adenosine (HY-B0228). Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation.
17(R)-Resolvin D1-d5 (17(R)-RvD1-d5) is deuterium labeled 17(R)-Resolvin D1. 17R-Resolvin D1 (17R-RvD1; AT-RvD1) is an aspirin-triggered epimer of Resolvin D1, which exhibits anti-inflammatory activity in mice and human PMNs cells . 17R-Resolvin D1 specificially inhibits TRPV3 with an IC50 of 398 nM and exhibits peripheral anti-nociceptive efficacy .
Dihomo-γ-linolenic acid-d6 (DGLA-d6) is the deuterium labeled Dihomo-γ-linolenic acid. Dihomo-γ-linolenic acid (all-cis-8,11,14-Eicosatrienoic acid) is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid attenuates atherosclerosis in the apolipoprotein E deficient mouse model system[1][2][3].
Procainamide- 13C2 hydrochloride is 13C labeled Procainamide. Procainamide hydrochloride is an antiarrhythmic agent used in the study of cardiac arrhythmias.
Dutasteride- 13C6 is the 13C labeled Dutasteride[1]. Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT[2].
D-Sorbitol- 13C6 is the 13C labeled D-Sorbitol[1]. D-Sorbitol (Sorbitol) is a six-carbon sugar alcohol and can used as a sugar substitute. D-Sorbitol can be used as a stabilizing excipient and/or isotonicity agent, sweetener, humectant, thickener and dietary supplement[2].
Adenosine- 13C5 is the 13C labeled Adenosine[1]. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation[2][3].
Pantethine- 15N2 is the 15N2 labeled Pantethine. Pantethine is an orally active lipid-lowering agent. Pantethine has anti-tumor, anti-inflammatory and anti-SARS-COV virus activities. Pantethine is also a neuroprotective agent. Pantethine can be used in the study of Alzheimer's disease, Parkinson's disease, major depression, systemic sclerosis and pantothenate kinase-related neurodegeneration [3] .
Hypoxanthine- 15N4 is the 15N labeled Hypoxanthine[1]. Hypoxanthine, a purine derivative, is a potential free radical generator and could be used as an indicator of hypoxia[2].
Deoxythymidine-5'-triphosphate- 15N2,d15 (dTTP- 15N2,d15) dilithium is deuterium and 15N labeled Deoxythymidine-5'-triphosphate (HY-138615). Deoxythymidine-5'-triphosphate (dTTP) is one of the four nucleoside triphosphates. Deoxythymidine-5'-triphosphate (dTTP) is used in the synthesis of DNA.
Pyridoxine- 13C4 (hydrochloride) is the 13C-labeled Pyridoxine (hydrochloride). Pyridoxine hydrochloride (Pyridoxol; Vitamin B6) is a pyridine derivative. Pyridoxine (Pyridoxol; Vitamin B6) exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
Topiramate-13C6 (McN 4853-13C6) is the 13C labeled isotope of Topiramate (HY-B0122). Topiramate (McN 4853) is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase[3].
Thyroxine hydrochloride- 13C6 is the 13C-labeled L-Thyroxine. L-Thyroxine (Levothyroxine; T4) is a synthetic hormone for the research of hypothyroidism. DIO enzymes convert biologically active thyroid hormone (Triiodothyronine,T3) from L-Thyroxine (T4)[1].
ATP- 15N5,d14 (Adenosine 5'-triphosphate- 15N5,d14) dilithium is deuterium and 15N labeled ATP (HY-B2176). ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation.
Vanillin- 13C6 is the 13C labeled Vanillin[1]. Vanillin (p-Vanillin) is a single molecule extracted from vanilla beans and also a popular odor used widely in perfume, food and medicine[2][3].
Rufinamide- 15N,d2 is the deuterium and 15N labeled Rufinamide[1]. Rufinamide is a new antiepileptic agent that differs structurally from other antiepileptic agents and is approved as adjunctive therapy for Lennox-Gastaut syndrome (LGS)[2][3].
2-Methoxybenzoic acid- 13C6 is the 13C-labeled 2-Methoxybenzoic acid. 2-Methoxybenzoic acid (NSC 3778) is used as an internal standard of salicylic acid and its putative biosynthetic precursors in cucumber leaves. Another known use is in the synthesis of Benextramine.
dGTP- 15N5 (2'-Deoxyguanosine-5'-triphosphate- 15N5) dilithium is 15N labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
1-PalMitoyl-2-arachidoyllecithin-d9-1 (1-Palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine-d9-1) is deuterium labeled 1-PalMitoyl-2-arachidoyllecithin. 1-Palmitoyl-2-arachidonoyl-sn-glycero-3-PC (PAPC) is a phospholipid containing palmitic acid (16:0) and arachidonic acid (20:4) at the sn-1 and sn-2 positions, respectively, that is found in biological membranes. PAPC is oxidized in vivo, and its oxidation products are involved in chronic inflammation and vascular disease. PAPC has been used to study signaling of oxidized phospholipids. Levels of PAPC are decreased in isolated human multiple myeloma cells .
NAD+- 13C5-1 is the 13C labeled NAD+[1]. NAD+ is a coenzyme composed of ribosylnicotinamide 5'-diphosphate coupled to adenosine 5'-phosphate by pyrophosphate linkage.
Ethynyl Estradiol- 13C2 is the 13C-labeled Ethynyl Estradiol. Ethynyl Estradiol-13C2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Allantoin- 13C2, 15N4 is the 13C and 15N labeled Allantoin[1]. Allantoin is a skin conditioning agent that promotes healthy skin, stimulates new and healthy tissue growth[2].
(Rac)-Rivastigmine-d6 is a labelled racemic Rivastigmine. Rivastigmine (ENA 713 free base) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease[1][2].
DL-α-Tocopherol acetate- 13C4,d6 is the deuterium and 13C labeled DL-α-Tocopherol acetate[1]. DL-α-Tocopherol acetate is a vitamin E derivative which is often included in the formulations of enteral nutrition[2][3].
Adenine- 15N5 (6-Aminopurine- 15N5; Vitamin B4- 15N5) is 15N labeled Adenine (HY-B0152). Adenine (6-Aminopurine), a purine, is one of the four nucleobases in the nucleic acid of DNA.
Adenine acts as a chemical component of DNA and RNA. Adenine also plays an important role in biochemistry involved in cellular respiration, the form of both ATP and the cofactors (NAD and FAD), and protein synthesis.
Levoglucosan-d7 is the deuterium labeled Levoglucosan. Levoglucosan (1,6-Anhydro-β-D-glucopyranose) is an anhydrosugar produced through glucan pyrolysis and is widely found in nature[1][2].
Nε,Nε,Nε-Trimethyllysine-d9 (chloride) is the deuterium labeled Nε,Nε,Nε-Trimethyllysine (chloride)[1]. Nε,Nε,Nε-Trimethyllysine chloride serves as a precursor for gut flora-dependent formation of N,N,N-trimethyl-5-aminovaleric acid (TMAVA)[2].
2'-Deoxyadenosine-5'-triphosphate- 15N5,d14 (dATP- 15N5,d14) dilithium is deuterium and 15N labeled 2'-Deoxyadenosine-5'-triphosphate (HY-136648). 2'-Deoxyadenosine-5'-triphosphate (dATP) is a nucleotide used in cells for DNA synthesis (or replication), as a substrate of DNA polymerase.
Adenine-15N5 hydrochloride hydrate (6-Aminopurine-15N5 hydrochloride hydrate) is the deuterium labeled Adenine (HY-B0152). Adenine (6-Aminopurine), a purine, is one of the four nucleobases in the nucleic acid of DNA. Adenine acts as a chemical component of DNA and RNA. Adenine also plays an important role in biochemistry involved in cellular respiration, the form of both ATP and the cofactors (NAD and FAD), and protein synthesis [3].
Adenine- 13C5 (6-Aminopurine- 13C5; Vitamin B4- 13C5) is 13C-labeled Adenine (HY-B0152). Adenine (6-Aminopurine), a purine, is one of the four nucleobases in the nucleic acid of DNA.
Adenine acts as a chemical component of DNA and RNA. Adenine also plays an important role in biochemistry involved in cellular respiration, the form of both ATP and the cofactors (NAD and FAD), and protein synthesis.
(Rac)-1,2-Dimyristoyl-sn-glycero-3-phosphocholine-d72 is deuterium labeled (Rac)-1,2-Dimyristoyl-sn-glycero-3-phosphocholine. 1,2-Dimyristoyl-sn-glycero-3-phosphocholine (DMPC) is a synthetic phospholipid used in liposomes. 1,2-Dimyristoyl-sn-glycero-3-ph
Dapsone- 13C12 is the 13C12 labeled Dapsone (HY-B0688). Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al [3] .
Cobimetinib- 13C6 (GDC-0973- 13C6; XL518- 13C6) racemate is the deuterium labeled Cobimetinib (racemate) (HY-13078) . Cobimetinib racemate (GDC-0973 racemate; XL518 racemate) is the racemate of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor .
Ethyl linoleate- 13C18 is the 13C labeled Ethyl linoleate. Ethyl linoleate inhibit the development of atherosclerotic lesions and the expression of inflammatory mediators[1].
Dabigatran- 13C6 is the 13C labeled Dabigatran[1]. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[2][3].
Riboflavin- 13C5 is the 13C-labeled Riboflavin. Riboflavin is an easily absorbed micronutrient with a key role in maintaining health in humans and other animals.
Neopterin- 13C5 (D-(+)-Neopterin- 13C5; D-erythro-Neopterin- 13C5) is the deuterium labeled Neopterin (HY-W040055) . Neopterin (D-(+)-Neopterin), a catabolic product of guanosine triphosphate (GTM), serves as a marker of cellular immune system activation .
dGTP- 15N5,d14 (2'-Deoxyguanosine-5'-triphosphate- 15N5,d14) dilithium is deuterium and 15N labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
N-Acetyl-D-glucosamine- 13C3, 15N is the 13C and 15N labeled N-Acetyl-D-glucosamine. N-Acetyl-D-Glucosamine (N-Acetyl-2-amino-2-deoxy-D-glucose) is a monosaccharide derivative of gluc[1][2].
Menaquinone-7- 13C6 is the 13C-labeled Menaquinone-7. Menaquinone-7 (Vitamin K2-7), belongs to a class of K2-vitamin homologs, is originally discovered as the anti-hemorrhagic factors[1]. Menaquinone-7 (Vitamin K2-7) is identified as the most bioactive cofactor for the carboxylation reaction of Gla-proteins [2]. Supplementation with Menaquinone-7 (Vitamin K2-7) is a pharmacological option for activating matrix Gla protein and intervening in the progression of calcific aortic valve stenosis (CAVS)[3].
Tenofovir alafenamide-d6 (GS-7340-d6) is deuterium labeled Tenofovir alafenamide. Tenofovir alafenamide (GS-7340) is an investigational oral proagent of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor .
Lansoprazole sulfone-d4 (AG-1813-d4) is the deuterium labeled Lansoprazole sulfone. Lansoprazole sulfone-d4 is an orally active and selective inhibitor of H +, K +-ATPase. Lansoprazole sulfone-d4 can significantly stimulates gastric acid secretion by inhibiting H +, K +-ATPase. Lansoprazole sulfone-d4 has potential applications in duodenal ulcer, gastric ulcer, gastroesophageal reflux disease and Zolinger Ellison disease [3].
Etiocholanolone-d2 is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2][3].
Myrcene-d6 is the deuterium labeled Myrcene. Myrcene (β-Myrcene) is a type of aromatic compound that inhibits TNFα and NF-κB activity. Myrcene has anti-invasive action, inhibits cell cycle, and leads to cancer cell apoptosis. Myrcene has strong blood protection effect, anti-inflammation, and anti-inflammatory activity [3] .
Tiludronate-d5 (sodium)mis the deuterium labeled Tiludronate disodium. Tiludronate (Tiludronic Acid) disodium, an orally active bisphosphonate, can act an osteoregulator. Tiludronate is used for the research of the metabolic bone disorders. Tiludronate is a potent inhibitor of the osteoclast vacuolar H(+)-ATPase. Antiresorptive and anti-inflammatory properties[1][2][3][4].
Sorafenib-d4 is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
Cromoglicic acid-d5 is the deuterium labeled Cromolyn[1]. Cromolyn is a mast cell stabilizer. Cromolyn has the potential for the research of bronchial asthma, allergic rhinitis, and certain allergic eye conditions such as vernal conjunctivitis, keratitis, and keratoconjunctivitis[2].
25-Hydroxycholesterol-d6 (25-OHC-d6) is the deuterium labeled 25-Hydroxycholesterol. 25-Hydroxycholesterol is a metabolite of cholesterol that is produced and secreted by macrophages in response to Toll-like receptor (TLR) activation. 25-hydroxycholesterol is a potent (EC50≈65 nM) and selective suppressor of IgA production by B cells[1][2].
5-Fluorouracil-d is the deuterium labeled 5-Fluorouracil. 5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer[1][2]. 5-Fluorouracil also inhibits HIV[3].
DPPC-d62 is the deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers[1]. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in mice[2].
Diethyl succinate-d4 is the deuterium labeled Diethyl succinate[1]. Diethyl succinate (Diethyl Butanedioate) is used at physiological pH and crosses biological membranes, incorporates into cells in tissue culture and is metabolized by the TCA cycle. Diethyl succinate is known to be non-toxic and used in fragrances and flavoring[2].
Octanoic acid-d15 is the deuterium labeled Octanoic acid. Octanoic acid (Caprylic acid) is an oily liquid with a slightly unpleasant rancid taste and used commercially in the production of esters used in perfumery and also in the manufacture of dyes.
Piperonyl butoxide-d9 is the deuterium labeled Piperonyl butoxide.Piperonyl butoxide (ENT-14250) is a pesticide synergist and food additive. Piperonyl butoxide has adverse effects on reproduction, development and behavior in mice. Piperonyl butoxide can activate c-Jun and ATF-2 in mouse hepatocytes. Piperonyl butoxide is a liver cancer carcinogen in rats and mice [3] .
Kynurenic acid-d5 is the deuterium labeled Kynurenic acid. Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8 .
CX516-d10 is the deuterium labeled CX516. CX516 (BDP 12) is an ampakine and acts as an AMPA receptor positive allosteric modulator for the research of Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI)[1].
Dolutegravir-d5 is deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2].
Deruxtecan-d5 is deuterium labeled Deruxtecan (HY-13631E). Deruxtecan is an ADC drug-linker conjugate composed of an DX-8951 derivative (DXd) and a maleimide-GGFG peptide linker, used for synthesizing DS-8201 and U3-1402.
DPPC-d66 is deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in
Alfuzosin-d7 (hydrochloride) is the deuterium labeled Alfuzosin hydrochloride. Alfuzosin hydrochloride is an α1 adrenergic receptor antagonist used to treat benign prostatic hyperplasia (BPH).
Aztreonam-d6 is deuterium labeled Aztreonam. Aztreonam (SQ-26,776) is a synthetic monocyclic beta-lactam antibiotic, which has a very high affinity for penicillin-binding protein 3 (PBP-3).
cis-Atovaquone-d4 is deuterium labeled Atovaquone. Atovaquone (Atavaquone) is a potent, selective and orally active inhibitor of the parasite’s mitochondrial cytochrome bc1 complex. Atovaquone is against human and P. falciparum cytochrome bc1 activity with IC50 values of 460 nM and 2.0 nM, respectively. Atovaquone is an antimalarial agent and has the potential for the investigation of neumocystis pneumonia, toxoplasmosis, malaria, and babesia[1][2].
Daurisoline-d2 is the deuterium labeled Daurisoline (HY-N0221). Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on hERG and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer .
Nonanoic acid-d4 is the deuterium labeled Nonanoic acid. Nonanoic acid is a naturally-occurring saturated fatty acid with nine carbon atoms. Nonanoic acid significantly reduces bacterial translocation, enhances antibacterial activity, and remarkably increases the secretion of porcine β-defensins 1 (pBD-1) and pBD-2[1].
Minodronic acid-d4 is deuterium labeled Minodronic acid. Minodronic acid (YM-529) is a third-generation bisphosphonate that directly and indirectly prevents proliferation, induces apoptosis, and inhibits metastasis of various types of cancer cells. Minodronic acid (YM-529) is an antagonist of purinergic P2X2/3 receptors involved in pain[1][2].
Ulipristal acetate-d6 is deuterium labeled Ulipristal acetate. Ulipristal acetate (CDB-2914) is an orally active, selective progesterone receptor modulator (SPRM). Ulipristal acetate stimulates the autophagic response selectively in leiomyoma cells. Ulipristal acetate has the potential for benign gynecological conditions treatment, such as uterine myoma[1][2].
Metformin-d6 hydrochloride is a deuterium labeled Metformin hydrochloride. Metformin hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin hydrochloride also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, metformin hydrochloride regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo .
Stigmasterol-d5-1 is deuterium labeled Stigmasterol. Stigmasterol is a plant sterol which has been focused on the cholesterol-lowering activity and is valued as an anti-stiffness factor in the therapy of rheumatic diseases[1].
DPPC-d75 is deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in
Suberic acid-d4 is the deuterium labeled Suberic acid[1]. Suberic acid (Octanedioic acid) is found to be associated with carnitine-acylcarnitine translocase deficiency, malonyl-Coa decarboxylase deficiency[2].
Cyfluthrin-d6 (β-Cyfluthi-d6) is deuterium labeled Cyfluthrin. Cyfluthrin is a type II pyrethroid and has effects on various insects. Cyfluthrin is a modulator of Nav1.8 sodium channels by repetitive stimulation. Cyfluthrin can be applied in agriculture,veterinary, insecticide,pyrethroid and stored product .
4-Methylanisole-d4 is the deuterium labeled 4-Methylanisole[1]. 4-Methylanisole (4-Methoxytoluene) is food flavoring agent and can be naturally found in Ylang Ylang fragrance oil[2].
Solifenacin-d5 (succinate) is deuterium labeled Solifenacin (Succinate). Solifenacin Succinate (YM905) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
Taurine-d4 is the deuterium labeled Taurine. Taurine, a sulphur-containing amino acid and an organic osmolyte involved in cell volume regulation, provides a substrate for the formation of bile salts, and plays a role in the modulation of intracellular free calcium concentration. Taurine has the ability to activate autophagy in adipocytes[1][2][3].
trans-Stilbene-d10 is the deuterium labeled trans-Stilbene[1]. trans-Stilbene ((E)-Stilbene) is used in the manufacturing of dye lasers, optical brighteners, non-steroidal synthetic estrogens[2].
D-Leucine-d10 is the deuterium labeled D-Leucine. D-Leucine is a more potent anti-seizure agent than L-leucine. D-leucine potently terminates seizures even after the onset of seizure activity. D-leucine, but not L-leucine, reduces long-term potentiation but had no effect on basal synaptic transmission in vitro[1].
Arachidic acid-d2 is the deuterium labeled Arachidic acid. Arachidonic acid (Icosanoic acid), a long-chain fatty acid, is present in all mammalian cells, typically esterified to membrane phospholipids, and is one of the most abundant polyunsaturated fatty acids present in human tissue[1][2].
Daurisoline-d11 is the deuterium labeled Daurisoline (HY-N0221). Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on hERG and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer .
4-Vinylphenol-d4 is deuterated labeled Losartan (potassium) (HY-17512A). Losartan potassium (DuP-753 potassium) is an angiotensin II receptor type 1 (AT1) antagonist, competing with the binding of angiotensin II to AT1 with an IC50 of 20 nM.
Parecoxib-d5 (sodium) is the deuterium labeled Parecoxib sodium. Parecoxib Sodium (SC 69124A) is a highly selective and orally active COX-2 inhibitor, the proagent of Valdecoxib (HY-15762). Parecoxib Sodium is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits prostaglandin (PG) synthesis. Parecoxib Sodium can be used for the relief of acute postoperative pain and symptoms of chronic inflammatory conditions such as osteoarthritis and rheumatoid arthritis in vivo[1][2].
Levocarnitine propionate-d9 (hydrochloride) (L-Propionylcarnitine-d9 (chloride)) is deuterium labeled Levocarnitine propionate (hydrochloride). Levocarnitine propionate hydrochloride (L-Propionylcarnitine chloride) is used to study diseases such as renal function deterioration, congestive heart failure, and intermittent claudication .
Homovanillic acid-d5 is the deuterium labeled Homovanillic acid. Homovanillic acid is a dopamine metabolite found to be associated with aromatic L-amino acid decarboxylase deficiency, celiac disease, growth hormone deficiency, and sepiapterin reductase deficiency.
Montelukast-d6 is the deuterium labeled Montelukast (sodium). Montelukast sodium is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (Cysltr1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage[1].
N-Arachidonylglycine-d8 is a deuterated labeled N-Arachidonylglycine . N-Arachidonylglycine (NA-Gly), a carboxylic analog of the endocannabinoid anandamide (AEA), is a GPR18 agonist (EC50 = 44.5 nM). Unlike AEA, N-Arachidonylglycine has no activity at either CB1 or CB2 receptors. N-Arachidonylglycine inhibits GLYT2 (IC50 = 5.1 μM). N-Arachidonylglycine also is an effective activator of endometrial cell migration [3].
Banoxantrone-d12 is the deuterium labeled banoxantrone. Banoxantrone is a novel bioreductive agent that can be reduced to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor.
Isobutylparaben-d4 is the deuterium labeled Isobutylparaben[1]. Isobutylparaben (Isobutyl 4-hydroxybenzoate) is a constitutive androstane receptor (CAR) activator. Isobutylparaben has a broad-spectrum antimicrobial activity and widely used in personal care products and cosmetics[2].
Moxifloxacin-d4 hydrochloride (BAY 12-8039-d4) is the hydrochloride salt form of deuterium labeled Moxifloxacin (Moxifloxacin). Moxifloxacin is an orally active antimicrobial, that can be used in the research of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia [3].
Tetrabenazine-d6 (Deutetrabenazine) is a deuterium-labled Tetrabenazine (HY-B0590), is the first deuterium approved worldwide for the research of Huntington's disease, or other hyperkinetic movement disorders .
Fosetyl-aluminum-d15 (Fosetyl-Al-d15) is the deuterium labeled Fosetyl-aluminum. Fosetyl-aluminum (Fosetyl-Al) is an active ingredient in many fungicides against downy mildew. Fosetyl-aluminum is used to control many diseases caused by Phytophthora spp. on agricultural and horticultural crops .
Climbazole-d4 is the deuterium labeled Climbazole. Climbazole (BAY-e 6975) is a potent antifungal agent. Climbazole also is a potent inducer of rat hepatic cytochrome P450[2].
Prednisolone acetate-d8 is the deuterium labeled Prednisolone acetate. Prednisolone acetate (Prednisolone 21-acetate) is an adrenal cortico hormones, with anti-inflammatory, anti-allergic and immune suppressive effects.
Docosanoic acid-d2 (Behenic acid-d2) is deuterium labeled Docosanoic acid (HY-W013049).
Docosanoic acid (Behenic acid) is a long-chain saturated fatty acid. Docosanoic acid inhibits the double-stranded DNA (dsDNA) binding activity of p53 DNA binding domain, with a Kd of 12 nM. Docosanoic acid has low bioavailability and can increase cholesterol in humans [3].
Taurocholic acid-d4 (sodium) is the deuterium labeled Taurocholic acid. Taurocholic acid (N-Choloyltaurine) is a bile acid involved in the emulsification of fats.
Lignoceric acid-d47 is the deuterium labeled Lignoceric acid. Lignoceric acid (Tetracosanoic acid) is a 24-carbon saturated (24:0) fatty acid, which is synthesized in the developing brain. Lignoceric acid is also a by-product of lignin production. Lignoceric acid can be used for Zellweger cerebro‐hepato‐renal syndrome and adrenoleukodystrophy research[1][2].
Abiraterone acetate-d4 is the deuterium labeled Abiraterone acetate. Abiraterone acetate (CB7630) is an oral, potent, selective, and irreversible inhibitor of CYP17A1 with antiandrogen activity. Abiraterone acetate is a proagent form of Abiraterone (CB7598).
SAH-d4 is the deuterium labeled SAH. SAH (S-Adenosylhomocysteine) is an amino acid derivative and a modulartor in several metabolic pathways. It is an intermediate in the synthesis of cysteine and adenosine[1]. SAH is an inhibitor for METTL3-METTL14 heterodimer complex (METTL3-14) with an IC50 of 0.9 µM[2].
Ospemifene-d4 is a deuterium labeled Ospemifene. Ospemifene is a selective and orally active estrogen receptor modulator for the prevention of osteoporosis with IC50 values of 827 nM and 1633 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene has bone-sparing, antitumor, and cholesterol-lowering effects[1][2].
Cefadroxil-d4 (hydrate) is the deuterium labeled Cefadroxil. Cefadroxil is a broad-spectrum antibiotic of the cephalosporin type, effective in Gram-positive and Gram-negative bacterial infections.
Azelaic acid-d14 is the deuterium labeled Azelaic acid[1]. Azelaic acid is an organic compound produced by the ozonolysis of oleic acid;component of a number of hair and skin conditioners[2][3].
4-Methylanisole-d7 is the deuterium labeled 4-Methylanisole[1]. 4-Methylanisole (4-Methoxytoluene) is food flavoring agent and can be naturally found in Ylang Ylang fragrance oil[2].
Tricaine-d5 (methanesulfonate) is the deuterium labeled Tricaine-d5 methanesulfonate. Tricaine methanesulfonate (MS-222) is a commonly used agent that can suppress or relieve pain. agent for immobilization of aquatic species. Tricaine methanesulfonate, the most widely used agent that can suppress or relieve pain. in fish, has been shown to induce embryotoxic effects in zebrafish .
Phenylglyoxylic acid-d5 (Benzoylformic acid-d5) is a deuterium labeled Phenylglyoxylic acid (HY-W010255). Phenylglyoxylic acid (Benzoylformic acid) is a metabolite of ethylbenzene and styrene (EB/S) and can be used as a biomarker of exposure to EB/S in human .
Rivaroxaban-d4 is a deuterium labeled Rivaroxaban. Rivaroxaban is a highly potent，selective and direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM)[1][2].
Theobromine-d6 is the deuterium labeled Theobromine. Theobromine is a methylxanthine found in cacao beans which can inhibit adenosine receptor A1 (AR1) signaling.
1-Phenylpyrrole-d9 (N-Phenylpyrrole-d9) is the deuterium labeled 1-Phenylpyrrole (HY-124891). 1-Phenylpyrrole (N-Phenylpyrrole) has dual fluorescent properties. 1-Phenylpyrrole displays a single band in nonpolar solvents and a second red-shifted fluorescent band in polar solvents .
1-Eicosanol-d41 is the deuterium labeled 1-Eicosanol[1]. 1-Eicosanol is a natural compound with antioxidant activity isolated from Hypericum carinatum[2].
Octanoic acid-d2 is the deuterium labeled Octanoic acid. Octanoic acid (Caprylic acid) is an oily liquid with a slightly unpleasant rancid taste and used commercially in the production of esters used in perfumery and also in the manufacture of dyes.
Oxcarbazepine-d8-1 is a deuterium of Oxcarbazepine. Oxcarbazepine is a sodium channel blocker . Oxcarbazepine significantly inhibits glioblastoma cell growth and induces apoptosis or G2/M arrest in glioblastoma cell lines . Oxcarbazepine-d8-1 has anti-cancer and anticonvulsant effects .
(S)-Verapamil-d7 (hydrochloride) is a deuterium labeled (S)-Verapamil hydrochloride. (S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells[1][2].
Ethyl acetoacetate-d5 is the deuterium labeled Ethyl acetoacetate[1]. Ethyl acetoacetate (Ethyl acetylacetate) is an ester widely used as an intermediate in the synthesis of many varieties of compounds[2][3][4]. Ethyl acetoacetate is an inhibitor of bacterial biofilm[5].
L-Arginine-d7 (hydrochloride) is the deuterium labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
Arbutin-d4 is deuterium labeled Arbutin. Arbutin (β-Arbutin) is a competitive inhibitor of tyrosinase in melanocytes, with Kiapp values of 1.42 mM for monophenolase; 0.9 mM for diphenolase. Arbutin is also used as depigmenting agents[1]. Arbutin is a natural polyphenol isolated from the bearberry plant Arctostaphylos uvaursi, possesses with anti-oxidant, anti-inflammatory and anti-tumor properties[2][3].
Octanoic acid-d5 is the deuterium labeled Octanoic acid[1]. Octanoic acid (Caprylic acid) is an oily liquid with a slightly unpleasant rancid taste and used commercially in the production of esters used in perfumery and also in the manufacture of dyes.
Uridine-d12 (β-Uridine-d12) is the deuterium labeled Uridine (HY-B1449). Uridine is a glycosylated pyrimidine-analog containing uracil attached to a ribose ring (or more specifically, aribofuranose) via a β-N1-glycosidic bond .
Tolcapone-d4 is the deuterium labeled Tolcapone. Tolcapone (Ro 40-7592) is a selective, orally active and powerful mixed (peripheral and central) COMT inhibitor with an IC50 of 773 nM in the liver[1]. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis[2]. Tolcapone induces oxidative stress leading to apoptosis and inhibition of tumor growth in neuroblastoma[3].
Nifedipine-d4 is the deuterium labeled Nifedipine. Nifedipine (BAY-a-1040) is a potent calcium channel blocker and agent of choice for cardiac insufficiencies.
Docosanoic acid-d43 (Behenic acid-d43) is the deuterium labeled Docosanoic acid (HY-W013049). Docosanoic acid (Behenic acid) is a long-chain saturated fatty acid. Docosanoic acid inhibits the double-stranded DNA (dsDNA) binding activity of p53 DNA binding domain, with a Kd of 12 nM. Docosanoic acid has low bioavailability and can increase cholesterol in humans [3].
Taurochenodeoxycholic acid-d5 (sodium) is the deuterium labeled Taurochenodeoxycholic acid sodium. Taurochenodeoxycholic acid sodium salt (12-Deoxycholyltaurine sodium salt) is one of the main bioactive substances of animals' bile acid. Taurochenodeoxycholic acid induces apoptosis and shows obvious anti-inflammatory and immune regulation properties[1][2].
DSG Crosslinker-d4 is the deuterium labeled DSG Crosslinker. Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Methyl Salicylate-d4 is the deuterium labeled Methyl Salicylate[1]. Methyl Salicylate (Wintergreen oil) is a topical analgesic and anti-inflammatory agent. Also used as a pesticide, a denaturant, a fragrance ingredient, and a flavoring agent in food and tobacco products[2]. A systemic acquired resistance (SAR) signal in tobacco[3]. A topical nonsteroidal anti-inflammatory agent (NSAID). Methyl salicylate lactoside is a COX inhibitor[5].
Isradipine-d6 is the deuterium labeled Isradipine[1]. Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease[2][3][4].
Homovanillic acid-d2 is the deuterium labeled Homovanillic acid. Homovanillic acid is a dopamine metabolite found to be associated with aromatic L-amino acid decarboxylase deficiency, celiac disease, growth hormone deficiency, and sepiapterin reductase deficiency.
Ethyl palmitate-d31 is the deuterium labeled Ethyl palmitate. Ethyl palmitate, a fatty acid ethyl ester (FAEE), shows a marked preference for the synthesis of ethyl palmitate and ethyl oleate over other FAEEs in human subjects after ethanol consumption. Ethyl palmitate is used as a hair- and skin-conditioning agent[1].
Succinic acid-d6 is the deuterium labeled Succinic acid. Succinic acid is an intermediate product of the tricarboxylic acid cycle, as well as one of fermentation products of anaerobic metabolism.
N,N-Dimethylacetamide-d6 is the deuterium labeled N,N-Dimethylacetamide[1]. N,N-Dimethylacetamide (DMAc) is an inexpensive, common aprotic organic solvent[2].
5-Methoxytryptamine-d4 (O-Methylserotonin-d4) is the deuterium labeled 5-Methoxytryptamine (HY-W015169). 5-Methoxytryptamine, a metabolite of Melatonin, is a nonselective 5-HT receptor agonist. 5-Methoxytryptamine has no affinity for the 5-HT3 receptor. 5-Methoxytryptamine is also a potent antioxidant and has radioprotective action [3].
trans-Stilbene-d12 is the deuterium labeled trans-Stilbene[1]. trans-Stilbene ((E)-Stilbene) is used in the manufacturing of dye lasers, optical brighteners, non-steroidal synthetic estrogens[2].
Mefatinib-d6 free base (Mifanertinib-d6) is the deuterium labeled Mefatinib. Mefatinib is a potent tyrosine kinase inhibitor with antineoplastic activity .
Vortioxetine-d4 (Lu AA 21004-d4) is the deuterium labeled Vortioxetine (HY-15414). Vortioxetine is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial agonist of 5-HT1B (Ki: 15 nM, 33 nM) .
Daurisoline-d5 is the deuterium labeled Daurisoline (HY-N0221). Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on hERG and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer .
Sitafloxacin-d4 (DU6859a-d4) is deuterium labeled Sitafloxacin. Sitafloxacin (DU6859a) is a potent, orally active fluoroquinolone antibiotic. Sitafloxacin shows antichlamydial activity and antibacterial activities against a broad range of gram-positive and gram-negative bacteria, including anaerobic bacteria, as well as against atypical pathogens. Sitafloxacin can be used for the research of respiratory tract infection and urinary tract infection .
Taurochenodeoxycholic acid-d4 (sodium) is the deuterium labeled Taurochenodeoxycholic acid. Taurochenodeoxycholic acid (12-Deoxycholyltaurine) is one of the main bioactive substances of animals' bile acid. Taurochenodeoxycholic acid induces apoptosis and shows obvious anti-inflammatory and immune regulation properties[1][2].
Cletoquine-d4-1 is the deuterium labeled Cletoquine. Cletoquine (Desethylhydroxychloroquine) is a major active metabolite of Hydroxychloroquine. Cletoquine is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune diseases treatment[1][2].
Taurochenodeoxycholic acid-d9 (sodium) is the deuterium labeled Taurochenodeoxycholic acid sodium. Taurochenodeoxycholic acid sodium salt (12-Deoxycholyltaurine sodium salt) is one of the main bioactive substances of animals' bile acid. Taurochenodeoxycholic acid induces apoptosis and shows obvious anti-inflammatory and immune regulation properties[1][2].
Prosulfocarb-d7 (S-Benzyl dipropylthiocarbamate-d7) is deuterium labeled Prosulfocarb. Prosulfocarb is a herbicide with a rapidly growing use trend. Prosulfocarb is used in winter cereals to help address the problem of increasing biotic resistance of weeds to certain pesticides. Environmental and food effects of prosulfocarb have been observed, and its transfer pattern from target crops to non-target areas has been studied. The volatility effect of prosulfocarb is an important factor explaining the inefficiency of isolated area contamination and marginal protection against residue spread .
Tolcapone-d7 is a deuterium labeled Tolcapone. Tolcapone is a selective, potent and orally active COMT inhibitor. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis and protect against extracellular toxicity induced by the aggregation of both proteins in PC12 cells[1][2].
Ramatroban-d4 is deuterium labeled Ramatroban. Ramatroban is a selective thromboxane A2 (TxA2, IC50=14 nM) antagonist, which also antagonizes CRTH2 (IC50=113 nM) by inhibiting PGD2 binding.
Fluvastatin-d6 (sodium) is deuterium labeled Fluvastatin sodium. Fluvastatin sodium (XU 62320) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM.
DPPC-d71 is deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in
Butamben-d9 is the deuterium labeled Butamben. Butamben (Butyl 4-aminobenzoate) results in long-lasting relief from pain, without impairing motor function or other sensory functions[1][2].
Trihydroxycholestanoic acid-d5 (Coprocholic acid-d5) is deuterium labeled Trihydroxycholestanoic acid. Trihydroxycholestanoic acid is an endogenous metabolite present in Blood that can be used for the research of Zellweger Syndrome, Refsum Disease, D Bifunctional Protein Deficiency and Infantile Refsum Disease [3][3] .
Arachidic acid-d4 is the deuterium labeled Arachidic acid. Arachidonic acid (Icosanoic acid), a long-chain fatty acid, is present in all mammalian cells, typically esterified to membrane phospholipids, and is one of the most abundant polyunsaturated fatty acids present in human tissue[1][2].
Tazarotenic acid-d6 is deuterium labeled Tazarotenic acid. Tazarotenic acid is the metabolite of Tazarotene. Tazarotenic acid binding to retinoic acid receptors (RARs) is the probable molecular target of retinoid action. Tazarotenic acid has the potential for the research of warty dyskeratoma [3].
Docosanoic acid-d4 (Behenic acid-4) is deuterium labeled Docosanoic acid (HY-W013049). Docosanoic acid (Behenic acid) is a long-chain saturated fatty acid. Docosanoic acid inhibits the double-stranded DNA (dsDNA) binding activity of p53 DNA binding domain, with a Kd of 12 nM. Docosanoic acid has low bioavailability and can increase cholesterol in humans [3].
Suberic acid-d12 is the deuterium labeled Suberic acid[1]. Suberic acid (Octanedioic acid) is found to be associated with carnitine-acylcarnitine translocase deficiency, malonyl-Coa decarboxylase deficiency[2].
Banoxantrone-d12 (dihydrochloride) is the deuterium labeled Banoxantrone dihydrochloride. Banoxantrone is a novel bioreductive agent that can be reduced to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor.
Nisoldipine-d6 is the deuterium labeled Nisoldipine. Nisoldipine(BAY-k 5552; Sular) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with an IC50 of 10 nM.
Finerenone-d5 (BAY 94-8862-d5) is deuterium labeled Finerenone. Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
Lansoprazole sulfide-d4 is a deuterium labeled Lansoprazole Sulfide. Lansoprazole Sulfide is an active metabolite of the proton pump inhibitor Lansoprazole. Lansoprazole Sulfide is an orally active anti-TB (Mycobacterium tuberculosis) agent with IC50 values of 0.59 µM intracellularly and 0.46 µM in broth[1].
Mexiletine-d6 (hydrochloride) is a deuterium labeled Mexiletine hydrochloride (KOE-1173 hydrochloride). Mexiletine hydrochloride, a Class IB antianhythmic, is a non-selective voltage-gated sodium channel blocker[1].
Gliquidone-d6 is deuterium labeled Gliquidone. Gliquidone (AR-DF 26) is an anti-diabetic agent in the sulfonylurea class, used in the treatment of diabetes mellitus type 2.
Benazepril-d5 hydrochloride is deuterium labeled Benazepril hydrochloride. Benazepril hydrochloride is an orally active angiotensin-converting enzyme (ACE) inhibitor to reduce angiotensin-II production. Benazepril hydrochloride inhibits oxidative stress and inhibits apoptosis by the PI3K/Akt signaling pathway. In addition, Benazepril hydrochloride improves diabetic nephropathy and decreases proteinuria. Benazepril hydrochloride can be used in the study of hypertension, heart failure and diabetic nephropathy [3].
Tempol-d17 is the deuterium labeled Tempol[1]. Tempol is a general superoxide dismutase (SOD)-mimetic agent that efficiently neutralizes reactive oxygen species (ROS)[2][3].
Tetrahydrocurcumin-d6 is a deuterium labeled Tetrahydrocurcumin. Tetrahydrocurcumin is a Curcuminoid which displays inhibitory activity for CYP2C9 and CYP3A4[1].
Phenytoin-d10 is the deuterium labeled Phenytoin. Phenytoin (5,5-Diphenylhydantoin) is a potent Voltage-gated Na+ channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice[1][2].
(±)-Carnitine-d9 (chloride) is the deuterium labeled (±)-Carnitine chloride. (±)-Carnitine chloride exists in two isomers, known as D and L. L-carnitine plays an essential role in the β-oxidation of fatty acids and also shows antioxidant, and anti-inflammatory activities.
Clofibric acid-d4 is the deuterium labeled Clofibric acid. Clofibric acid (Chlorofibrinic acid), the pharmaceutically active metabolite of lipid regulators Clofibrate, Etofibrate and Etofyllinclofibrate, is a PPARα agonist which exhibits hypolipidemic effects. Clofibric acid also is an herbicide[1][2][3].
Arachidic acid-d39 is the deuterium labeled Arachidic acid. Arachidonic acid (Icosanoic acid), a long-chain fatty acid, is present in all mammalian cells, typically esterified to membrane phospholipids, and is one of the most abundant polyunsaturated fatty acids present in human tissue[1][2].
Nitrendipine-d5 is the deuterium labeled Nitrendipine. Nitrendipine (BAY-E-5009), an analogue of Nifedipine (HY-B0284), is a dihydropyridine calcium channel blocker with vasodilator action. Nitrendipine has antihypertensive effect[1][2][3][4].
(Rac)-Rotigotine-d7 (hydrochloride) is deuterium labeled (Rac)-Rotigotine (hydrochloride). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
Asoxime-d4 (dichloride) is the deuterium labeled Asoxime dichloride. Asoxime dichloride (HI-6) is an antagonist to acetylcholine receptors (AChRs) including the nicotinic receptor, α7 nAChR. Asoxime dichloride involves in modulating immunity response. Asoxime dichloride (HI-6) can be used as an antigen and improves vaccination efficacy in the nervous system[1].
trans-Stilbene-d2 is the deuterium labeled trans-Stilbene[1]. trans-Stilbene ((E)-Stilbene) is used in the manufacturing of dye lasers, optical brighteners, non-steroidal synthetic estrogens[2].
Hydroxy Itraconazole-d8 is the deuterium labeled Hydroxy Itraconazole. Hydroxy Itraconazole is an active metabolite of Itraconazole (ITZ), which is a triazole antifungal agent.
Salmeterol-d5 is a deuterated labeled Salmeterol . Salmeterol (GR33343X) is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively .
Deuruxolitinib, a deuterated Ruxolitinib (HY-50856), is an orally active JAK1 and JAK2 inhibitor. Deuruxolitinib demonstrates significant hair regrowth effects. Deuruxolitinib can be used for the research of alopecia areata .
N4-Acetylsulfamethoxazole-d4 is the deuterium labeled N4-Acetylsulfamethoxazole. N4-Acetylsulfamethoxazole (Acetylsulfamethoxazole) is a metabolite of Sulfamethoxazole (HY-B0322). Sulfamethoxazole is a sulfonamide bacteriostatic antibiotic, used for bacterial infections[1].
(-)-Huperzine A-d4 hydrochloride is deuterated labeled (-)-Huperzine A (HY-17387). (-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease [3] .
SAR405838-d10 (MI-77301-d10) is the deuterium labeled SAR405838 (HY-18986). SAR405838 (MI-77301), an analog of MI-773, is a highly potent and selective MDM2-p53 interaction inhibitor. SAR405838 binds to MDM2 with a Ki of 0.88 nM. SAR405838 induces apoptosis and has potent antitumor activity [3].
Berberine-d6 (chloride) is the deuterium labeled Berberine chloride. Berberine chloride is an alkaloid that acts as an antibiotic. Berberine chloride induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Antineoplastic properties[1].
Muscarine-d9 (iodide) is the deuterium labeled Muscarine iodide. Muscarine ((+)-Muscarine) iodide is a toxin that can stimulate the parasympathetic nervous system. Muscarine iodide is a prototype muscarinic acetylcholine receptor agonist[1][2].
Tazarotenic acid-d8 (AGN 190299-d8) is the deuterium labeled Tazarotenic acid (HY-101108). Tazarotenic acid is the metabolite of Tazarotene (HY-15388) .
Vortioxetine-d6 (Lu AA 21004-d6) is the deuterium labeled Vortioxetine (HY-B1490A). Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial agonist of 5-HT1B (Ki: 15 nM, 33 nM) .
DPPC-d13 is deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in
N,N-Dimethylacetamide-d9 is the deuterium labeled N,N-Dimethylacetamide[1]. N,N-Dimethylacetamide (DMAc) is an inexpensive, common aprotic organic solvent[2].
N6-Benzyladenosine-d5 (Benzyladenosine-d5) is deuterium labeled N6-Benzyladenosine. N6-Benzyladenosine is an adenosine receptor agonist, has a cytoactive activity. N6-Benzyladenosine arrests cell cycle at G0/G1 phase and induces cell apoptosis. N6-Benzyladenosine also exerts inhibitory effect on T. gondii adenosine kinase and glioma [3] .
Isradipine-d7 is deuterated labeled Isradipine (HY-B0233). Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease [3].
Genistein-d4 is the deuterium labeled Genistein. Genistein, a soy isoflavone, is a multiple tyrosine kinases (e.g., EGFR) inhibitor which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis[1][2].
Deruxtecan-d4 is deuterium labeled Deruxtecan (HY-13631E). Deruxtecan is an ADC drug-linker conjugate composed of an DX-8951 derivative (DXd) and a maleimide-GGFG peptide linker, used for synthesizing DS-8201 and U3-1402.
Dihydrodiol-Ibrutinib-d5 is the deuterium labeled Dihydrodiol-Ibrutinib (HY-100659). Dihydrodiol-Ibrutinib is a dihydrodiol active metabolite of Ibrutinib (HY-10997), has inhibitory activity towards BTK approximately 15 times lower than that of ibrutinib .
DPPC-d4 is deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in m
Nonanoic acid-d17 is the deuterium labeled Nonanoic acid. Nonanoic acid is a naturally-occurring saturated fatty acid with nine carbon atoms. Nonanoic acid significantly reduces bacterial translocation, enhances antibacterial activity, and remarkably increases the secretion of porcine β-defensins 1 (pBD-1) and pBD-2[1].
DPPC-d9 is the deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers[1]. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in mice[2].
Rimsulfuron-d6 is deuterium labeled Rimsulfuron. Rimsulfuron (DPX-E9636) is a sulfonylurea herbicide for postemergence use in maize to control grasses and some broadleaf weeds[1][2].
DL-Dipalmitoylphosphatidylcholine-d62 is deuterium labeled DL-Dipalmitoylphosphatidylcholine. DL-Dipalmitoylphosphatidylcholine (DL-DPPC) is a biochemical reagent .
(R)-Verapamil-d7 (hydrochloride) is a deuterium labeled (R)-Verapamil hydrochloride. (R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer agents[1][2].
Ciclopirox-d11 is the deuterium labeled Ciclopirox. Ciclopirox (HOE296b) is a synthetic antifungal agent that can be used for superficial mycoses reseaech. Ciclopirox olamine has a very broad spectrum of activity and inhibits dermatophytes, yeasts, molds, and many Gram-positive and Gram-negative species pathogenic[1].
N6-Methyladenosine- 13C4 (6-Methyladenosine- 13C4; N-Methyladenosine- 13C4) is 13C-labeled N6-Methyladenosine (HY-N0086). N6-Methyladenosine is the most prevalent internal (non-cap) modification present in the messenger RNA (mRNA) of all higher eukaryotes. N6-Methyladenosine can modifies viral RNAs and has antiviral activities.
Pregnenolone- 13C2,d2 is the deuterium and 13C labeled Pregnenolone (HY-B0151). Pregnenolone is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[1][2][3][4].
Dihydrouracil- 13C4, 15N2 is the 13C and 15N labeled Dihydrouracil[1]. Dihydrouracil (5,6-Dihydrouracil), a metabolite of Uracil, can be used as a marker for identification of dihydropyrimidine dehydrogenase (DPD)-deficient[2][3].
Exemestane- 13C,d2 is 13C and deuterated labeled Exemestane (HY-13632). Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research .
ATP- 13C10, 15N5 is the 13C and 15N labeled ATP[1]. ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation[2][3].
Mitotane- 13C6 is the 13C labeled Mitotane . Mitotane (2,4′-DDD), an isomer of DDD and derivative of dichlorodiphenyltrichloroethane (DDT), is an antineoplastic agent, can be used to research adrenocortical carcinoma. Mitotane exert its adrenocorticolytic effect at least in part through lipotoxicity induced by intracellular free cholesterol (FC) accumulation. Mitotane can have direct pituitary effects on corticotroph cells. Mitotane can induce CYP3A4 gene expression via steroid and xenobiotic receptor (SXR) activation, and has agent-agent interactions [3] .
Uridine-13C9,15N2 (β-Uridine-13C9,15N2) is 13C and 15N labeled Uridine (HY-B1449). Uridine is a glycosylated pyrimidine-analog containing uracil attached to a ribose ring (or more specifically, aribofuranose) via a β-N1-glycosidic bond .
5-Fluorouracil- 13C4, 15N2 is the 13C and 15N labeled 5-Fluorouracil[1]. 5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer[2][3]. 5-Fluorouracil also inhibits HIV[4].
Cytidine-d2-1 is the deuterium labeled Cytidine. Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catech
Ethyl Paraben- 13C6 (Ethyl parahydroxybenzoate- 13C6) is 13C labeled Ethylparaben. Ethylparaben is the ethyl ester of paraben and is used as an antifungal preservative and food additive .
Folic acid-13C6 is a deuterated labeled Folic acid . Folic acid (Vitamin B9) is a orally active essential nutrient from the B complex group of vitamins. Folic acid shows antidepressant-like effect. Folic acid sodium reduces the risk of neonatal neural tube defects. Folic acid can be used to the research of megaloblastic and macrocytic anemias due to folic deficiency [3] .
L-Ascorbic acid- 13C6 is the 13C-labeled L-Ascorbic acid. L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor[1][2][3]. L-Ascorbic acid exhibits anti-cancer effects through the generation of reactive oxygen species (ROS) and selective damage to cancer cells[4].
Hydrochlorothiazide- 15N2, 13C,d2 is 15N and deuterated labeled Hydrochlorothiazide (HY-B0252). Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect [3].
rU Phosphoramidite- 13C2,d1 (DMT-2'O-TBDMS-rU phosphoramidite- 13C2,d1) is deuterium and 13C-labeled rU Phosphoramidite (HY-W048482). rU Phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
Folic acid- 13C5 is the 13C-labeled Folic acid. Folic acid (Vitamin M; Vitamin B9) is a B vitamin; is necessary for the production and maintenance of new cells, for DNA synthesis and RNA synthesis.
Ornidazole- 13C2, 15N2 is the 13C, 15N labeled Ornidazole. Ornidazole(Ro 7-0207) is a 5-nitroimidazole derivative with antiprotozoal and antibacterial properties against anaerobic bacteria.
Zearalenone- 13C18 (Mycotoxin F2- 13C18; Toxin F2- 13C18) is the 13C labeled Zearalenone (HY-103447) . Zearalenone is a mycotoxin produced mainly by fungi belonging to the genus Fusarium in foods and feeds. Possess oestrogenic activity in pigs, cattle and sheep, with low acute toxicity. Causes precocious development of mammae and other estrogenic effects in young gilts [3].
L-Arginine- 13C6, 15N4 (hydrochloride) is the 13C- and 15N-labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
Uridine 5'-monophosphate- 15N2,d11 (5'-?Uridylic acid- 15N2,d11) dilithium is deuterium and 15N labeled Uridine 5'-monophosphate (HY-101981). Uridine 5'-monophosphate (5'-?Uridylic acid), a monophosphate form of UTP, can be acquired either from a de novo pathway or degradation products of nucleotides and nucleic acids in vivo and is a major nucleotide analogue in mammalian milk.
2-Methoxyestradiol- 13C6 is the 13C-labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa[1][2][3][4][5][6].
Mitotane- 13C12 (2,4′-DDD- 13C12) is 13C labeled Mitotane. Mitotane (2,4′-DDD), an isomer of DDD and derivative of dichlorodiphenyltrichloroethane (DDT), is an antineoplastic agent, can be used to research adrenocortical carcinoma. Mitotane exert its adrenocorticolytic effect at least in part through lipotoxicity induced by intracellular free cholesterol (FC) accumulation. Mitotane can have direct pituitary effects on corticotroph cells. Mitotane can induce CYP3A4 gene expression via steroid and xenobiotic receptor (SXR) activation, and has agent-agent interactions [3][3] .
Propyl paraben- 13C6 (Propyl parahydroxybenzoate- 13C6) is 13C labeled Propylparaben. Propylparaben (Propyl parahydroxybenzoate) is an antibacterial preservative that can be produced by plants and bacteria. Propylparaben is commonly used in cosmetics, pharmaceuticals and foods. Propylparaben disrupts follicular growth and steroidogenic function by altering cell cycle, apoptosis and steroidogenic pathways. Propylparaben also reduced sperm count and motility in rats [3] .
β-Caryophyllene- 13C,d2 is 13C and deuterated labeled trans,trans-2,4-Decadienal (HY-W013627). trans,trans-2,4-Decadienal is a lipid peroxidation product of linolieic acid .
2-Deoxy-D-glucose- 13C6 (2-DG- 13C6) is 13C labeled 2-Deoxy-D-glucose. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase .
13,14-Dihydro-15-keto prostaglandin D2-d4 (DK-PGD2-d4) is deuterium labeled 13,14-Dihydro-15-keto prostaglandin D2. 13, 14-Dihydro-15-keto prostaglandin D2 (DK-PGD2) is a PGD2 metabolite formed by the 15-hydroxyl PGDH pathway. 13, 14-Dihydro-15-keto prostaglandin D2 is a selective agonist for the DP2 receptor. 13, 14-Dihydro-15-keto prostaglandin D2 can inhibit ion flux in canine colonic mucosa preparation .
α-Hydroxyglutaric acid- 13C5 (sodium) is the 13C labeled α-Hydroxyglutaric acid sodium[1]. α-Hydroxyglutaric acid (2-Hydroxyglutarate) sodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid sodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases[2].
13,14-Dihydro-15-keto prostaglandin D2-d9 (DK-PGD2-d9) is deuterium labeled 13,14-Dihydro-15-keto prostaglandin D2. 13, 14-Dihydro-15-keto prostaglandin D2 (DK-PGD2) is a PGD2 metabolite formed by the 15-hydroxyl PGDH pathway. 13, 14-Dihydro-15-keto prostaglandin D2 is a selective agonist for the DP2 receptor. 13, 14-Dihydro-15-keto prostaglandin D2 can inhibit ion flux in canine colonic mucosa preparation .
1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d4 is deuterium labeled 1,2-Distearoyl-sn-glycero-3-phosphorylcholine. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine (1,2-Distearoyl-sn-glycero-3-PC; DSPC) is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-glyc
1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d9 is deuterium labeled 1,2-Distearoyl-sn-glycero-3-phosphorylcholine. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine (1,2-Distearoyl-sn-glycero-3-PC; DSPC) is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-glyc
L-Valine- 13C5, 15N,d8 is the deuterium, 13C-, and 15-labeled L-Valine. L-Valine is one of 20 proteinogenic amino acids. L-Valine is an essential amino acid[1].
D-(+)-Trehalose-13C12 is a 13C isotope labeled version of D-(+)-Trehalose (HY-N1132). D-(+)-Trehalose,which is widespread, can be used as a food ingredient and pharmaceutical excipient .
1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d74 is deuterium labeled 1,2-Distearoyl-sn-glycero-3-phosphorylcholine. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine (1,2-Distearoyl-sn-glycero-3-PC; DSPC) is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-gly
Guanosine triphosphate- 13C10, 15N5 (tetraammonium) is the 13C and 15N labeled Guanosine triphosphate tetraammonium[1]. Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19[2].
1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d70 is the deuterium labeled 1,2-Distearoyl-sn-glycero-3-phosphorylcholine. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine (1,2-Distearoyl-sn-glycero-3-PC; DSPC) is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine is used to synthesize liposomes, and is the lipid component in the lipid nanoparticle (LNP) system[1][2].
Adenosine monophosphate- 13C10, 15N5 (AMP- 13C10, 15N5) disodium is 13C and 15N-labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction [3].
1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d13 is deuterium labeled 1,2-Distearoyl-sn-glycero-3-phosphorylcholine. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine (1,2-Distearoyl-sn-glycero-3-PC; DSPC) is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-gly
1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d79 is deuterium labeled 1,2-Distearoyl-sn-glycero-3-phosphorylcholine. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine (1,2-Distearoyl-sn-glycero-3-PC; DSPC) is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-gly
L-Thyroxine- 13C6-1 (Levothyroxine- 13C6-1; T4- 13C6-1) is a 13C labeled L-Thyroxine (HY-18341). L-Thyroxine (Levothyroxine; T4) is a synthetic hormone for the research of hypothyroidism. DIO enzymes convert biologically active thyroid hormone (Triiodothyronine,T3) from L-Thyroxine (T4) .
p-Anisic acid- 13C6 is the 13C-labeled p-Anisic acid. p-Anisic acid (4-Methoxybenzoic acid) is one of the isomers of anisic acid, with anti-bacterial and antiseptic properties[1].
L-Valine- 13C5, 15N,d2 is the deuterium, 13C-, and 15-labeled L-Valine. L-Valine is one of 20 proteinogenic amino acids. L-Valine is an essential amino acid[1].
Imidazole- 15N2 (Glyoxaline- 15N2) is 15N labeled Imidazole. Imidazole (Glyoxaline; 1,3-Diaza-2,4-cyclopentadiene) is a heterocyclic aromatic compound. Imidazole bearing molecules have been used as corrosion, acetylcholinesterase (AChEI) and xanthine oxidase (XO) inhibitors, performing biological activities such as antifungal, antituberculosis, anti-inflammatory, antioxidant, and analgesic, amongst many others. Imidazole inhibits the enzymatic conversion of the endoperoxides (PGG2 and PGH2) to thromboxane A2 by platelet microsomes. Imidazole derivatives exhibits inhibition on SARS-CoV-2 3CL Pro enzyme, which is promising for research in the field of Alzheimer’s disease, gout, COVID-19 and thrombo-embolic disease [3] .
1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d83 is deuterium labeled 1,2-Distearoyl-sn-glycero-3-phosphorylcholine. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine (1,2-Distearoyl-sn-glycero-3-PC; DSPC) is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine is used to synthesize liposomes, and is the lipid component in the lipid nanoparticle (LNP) system[1][2].
LysoPC(14:0/0:0)-d7 (14:0 Lyso PC-d7) is deuterium labeled LysoPC(14:0/0:0). LysoPC(14:0/0:0) is a lysophospholipid (LyP). It is a monoglycerophospholipid in which a phosphorylcholine moiety occupies a glycerol substitution site. LysoPC(14:0/0:0) has potent antispasmodic effect .
Lamivudine-13C,15N2,d2 (BCH-189-13C,15N2,d2) is a 13C, 15N, and deuterium labeled Lamivudine (HY-B0250). Lamivudine is an orally active and blood-brain barrier permeable nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine inhibits HIV reverse transcriptase 1 and 2 and hepatitis B virus (HBV) reverse transcriptase [3] .
Adenosine monophosphate- 13C10, 15N5(AMP- 13C10, 15N5) is the 13C-labeled and 15N-labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction [3].
Talazoparib- 13C,d4 is 13C and deuterated labeled Talazoparib (HY-16106). Talazoparib is an orally active PARP 1/2 inhibitor with Ki values of 1.2 nM and 0.87 nM for inhibiting PARP1 and PARP2 enzymatic activities, respectively. Has anti-tumor activity.
Thymidine-5'-monophosphate- 13C10, 15N2 (disodium) is the 13C and 15N labeled Thymidine-5'-monophosphate disodium salt[1]. Thymidine-5'-monophosphate disodium salt is an endogenous metabolite.
Mirogabalin-13C2,d1 (Mixture of Diastereomers) is a C13 and deuterium labeled Mirogabalin. Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS .
5'-Methylthioadenosine- 13C6 is the 13C-labeled 5'-Methylthioadenosine. 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis[1]. 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis[2].
Eliglustat-d15 (tartrate) is the deuterium labeled Eliglustat. Eliglustat tartrate is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC50 of 24 nM.
Vitamin D4-d5 is the deuterium labeled Vitamin D4. Vitamin D4 (22-Dihydroergocalciferol) is a Vitamin D derived from fungi. The precursor of Vitamin D4 is 22,23-dihydroergosterol[1].
(R)-Carvedilol-d4 is deuterium labeled (R)-Carvedilol. (R)-Carvedilol ((R)-BM 14190), the R-enantiomer of Carvedilol, is a non-selective β/α-1 blocker. (R)-Carvedilol exerts protection against the vascular or cardiac toxicity of Doxorubicin (DOX)[1].
Palmitoyl serinol-d5 is the deuterium labeled Palmitoyl serinol[1]. Palmitoyl serinol (N-Palmitoyl serinol) is an analog of the endocannabinoid N-palmitoyl ethanolamine (PEA). Palmitoyl serinol improves the epidermal permeability barrier in both normal and inflamed skin[2][3].
Sphingosine-1-phosphate-d7 is the deuterium labeled Sphingosine-1-phosphate. Sphingosine-1-phosphate (S1P) is an agonist of S1P1-5 receptors and a ligand of GPR3, GPR6 and GPR12. Sphingosine-1-phosphate is an intracellular second messenger and mobilizes Ca2+ as an extracellular ligand for G protein-coupled receptors[1]. Sphingosine-1-phosphate is an important lipid mediator generated from Sphingomyelin (HY-113498) or other membrane phospholipids[2].
Methyl cinnamate-d7 is deuterated labeled Cinnamyl Alcohol (HY-Y0078). Cinnamyl Alcohol is an active component from chestnut flower, inhibits increased PPARγ expression, with anti-obesity activity .
Cholestenone-d7 is deuterium labeled Cholestenone. Cholestenone (4-Cholesten-3-one), the intermediate oxidation product of cholesterol, is metabolized primarily in the liver. Cholestenone is highly mobile in membranes and influences cholesterol flip-flop
Elacestrant-d4-1 is the deuterium labeled Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively .
Sildenafil (citrate)-d8 is the deuterium labeled Sildenafil citrate[1]. Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 5.22 nM.
7-Ethoxyresorufin-d5 is deuterium labeled 7-Ethoxyresorufin. 7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase[1][2].
Oxcarbazepine-d4-1 is deuterium labeled Oxcarbazepine. Oxcarbazepine is a sodium channel blocker[1]. Oxcarbazepine significantly inhibits glioblastoma cell growth and induces apoptosis or G2/M arrest in glioblastoma cell lines[2]. Anti-cancer and anticonvulsant effects[2][3].
Resolvin D3-d5 is the deuterium labeled Resolvin D3. Resolvin D3 (RvD3) is a docosahexaenoic acid (DHA) derived mediator. Resolvin D3 is dysregulated in arthritis and reduces arthritic inflammation[1][2].
Azilsartan mepixetil-d5 (QR-01019-d5) is deuterium labeled Azilsartan mepixetil. Azilsartan mepixetil is the antagonist of angiotensin II receptor. Azilsartan mepixetil has stronger and longer blood pressure effect, more abvious and longer lasting heart rate lowering effect and high safety. Azilsartan mepixetil achieves ideal protective effect for heart and kidney functions. Azilsartan mepixetil has the potential for the research of hypertension, chronic heart failure and diabetic nephropathy (extracted from patent CN107400122A) .
Melatonin-d4 is deuterium labeled Melatonin. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Antioxidative and anti-inflammatory properties [3]. Melatonin is a selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation .
(S)-Carvedilol-d4 is deuterium labeled (S)-Carvedilol. (S)-Carvedilol, the S-enantiomer of Carvedilol, is a non-selective β/α-1 blocker. (S)-Carvedilol exerts protection against the vascular or cardiac toxicity of Doxorubicin (DOX)[1].
Guaiacol-d4-1 is the deuterium labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
Vilanterol-d4 (trifenatate) is deuterium labeled Vilanterol (trifenatate). Vilanterol trifenatate (GW642444 trifenatate) is a long-acting β2-adrenoceptor (β2-AR) agonist with inherent 24-hour activity. The pEC50s for β2-AR, β1-AR and β3-AR are 10.37, 6.98 and 7.36, respectively.
Tridecanoic acid-d25 is the deuterium labeled Tridecanoic acid. Tridecanoic acid (N-Tridecanoic acid), a 13-carbon medium-chain saturated fatty acid, can serve as an antipersister and antibiofilm agent that may be applied to research bacterial infections. Tridecanoic acid inhibits Escherichia coli persistence and biofilm formation[1].
Folinic acid-d4-1 (Leucovorin-d4-1) calcium hydrate is deuterated labeled Folinic acid (HY-17556). Folinic acid (Leucovorin) is a biological folic acid and is generally administered along with Methotrexate (MTX) (HY-14519) as a rescue agent to decrease MTX-induced toxicity.
Mono(3-carboxypropyl) phthalate-d4 (MCPP-d4) is a deuterium labeled Mono(3-carboxypropyl) phthalate (HY-133673). Mono(3-carboxypropyl) phthalate (MCPP) is a metabolite of Di-n-octyl phthalate. Di-n-octyl phthalate (DnOP) is a plasticizer used in polyvinyl chloride plastics, cellulose esters, and polystyrene resins .
Fingolimod-d4 is the deuterium labeled Fingolimod. Fingolimod (FTY720 free base) is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant[1].
Melatonin-d7 is the deuterium labeled Melatonin (HY-B0075). Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties [3]. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation . Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress .
(Rac)-Valsartan-d9 is deuterium labeled Valsartan. Valsartan (CGP 48933) is an angiotensin II receptor antagonist and has the potential for high blood pressure and heart failure research[1].
1,4-Dibromobenzene-d4 is a deuterium labeled 1,4-Dibromobenzene. 1,4-Dibromobenzene is used as a fumigant and as a chemical intermediate for pharmaceuticals. Inhalation exposure gives rise to dizziness and chokingwhereas contact with skin or eye produces inflammation and burning in humans[1].
Hippuric acid-d2 is the deuterium labeled Hippuric acid. Hippuric Acid (2-Benzamidoacetic acid), an acyl glycine produced by the conjugation of benzoic acid and glycine, is a normal component in urine as a metabolite of aromatic compounds from food.
Tridecanoic acid-d2 is the deuterium labeled Tridecanoic acid. Tridecanoic acid (N-Tridecanoic acid), a 13-carbon medium-chain saturated fatty acid, can serve as an antipersister and antibiofilm agent that may be applied to research bacterial infections. Tridecanoic acid inhibits Escherichia coli persistence and biofilm formation[1].
Brexpiprazole S-oxide-d8 is a deuterium labeled Brexpiprazole S-oxide. Brexpiprazole S-oxide is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM[1][2][3].
N-Desmethyl Selegiline-dd5 hydrochloride is the deuterium labeled N-Desmethyl Selegiline hydrochloride[1]. N-Desmethyl Selegiline-d5 hydrochloride is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Methyl paraben-d4 is the deuterium labeled Methyl Paraben[1]. Methyl Paraben, isolated from the barks of Tsuga dumosa the methyl ester of p-hydroxybenzoic acid, is a standardized chemical allergen. Methyl Paraben is a stable, non-volatile compound used as an antimicrobial preservative in foods, agents and cosmetics. The physiologic effect of Methyl Paraben is by means of increased histamine release, and cell-mediated immunity[2].
Degarelix-d7 (FE 200486-d7 free base) is deuterium labeled Degarelix. Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist.
2-Phenylglycine-d5 is the deuterium labeled 2-Phenylglycine. 2-Phenylglycine (DL-α-Phenylglycine) is a metabolite in breast milk during the W2 to W4 lactation period[1].
4-Hydroxypropranolol-d7 is the deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol. 4-Hydroxypropranolol hydrochlorid is of comparable potency to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties[1][2][3].
Leukotriene B4-d5 (LTB4-d5) is deuterium labeled Leukotriene B4. Leukotriene B4 (LTB4) is known as one of the most potent chemoattractants and activators of leukocytes and is involved in inflammatory diseases. Leukotriene B4 is also an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs [3] .
(E)-4-Hydroxytamoxifen-d5 ((E)-Afimoxifene-d5) is the deuterium labeled (E)-4-Hydroxytamoxifen. (E)-4-Hydroxytamoxifen ((E)-Afimoxifene), the less active isomer of (Z)-4-hydroxytamoxifen, is an estrogen receptor modulator.
Methyl tetradecanoate-d27 is the deuterium labeled Methyl myristate. Methyl myristate is a saturated fatty acid methyl ester obtained from the esterification of myristic acid. Methyl myristate shows a high melanin induction in B16F10 melanoma[1].
Docosahexaenoic acid ethyl ester-d5 is the deuterium labeled Docosahexaenoic acid ethyl ester. Docosahexaenoic acid ethyl ester (Ethyl docosahexaenoate) is a 90% concentrated ethyl ester of docosahexaenoic acid manufactured from the microalgal oil. Docosahexaenoic acid ethyl ester enhances 6-hydroxydopamine-induced neuronal damage by induction of lipid peroxidation in mouse striatum. Docosahexaenoic acid (DHA) is a key component of the cell membrane, and its peroxidation is inducible due to the double-bond chemical structure. Docosahexaenoic acid has neuroprotective effects[1][2].
Pimozide-d4-1 is the deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5[1][2][3][4].
Indole-3-acetyl glutamate-d4 (IAGlu-d4) is deuterium labeled Indole-3-acetyl glutamate. Indole-3-acetyl glutamate (IAGlu) is a derivative of the plant hormone indole-3-acetic acid (IAA). As a conjugated form of IAA, Indole-3-acetyl glutamate involves in the transport, storage, and homeostatic regulation of IAA within the plant. Indole-3-acetyl glutamate can be used for research into the effects of plant hormones on the growth and development of plants .
Simvastatin acid-d6 (ammonium)mis the deuterium labeled Simvastatin acid ammonium. Simvastatin ammonium is an active metabolite of simvastatin lactone mediated by CYP3A4/5 in the intestinal wall and liver (pKa=5.5). Simvastatin ammonium reduces indoxyl sulfate-mediated reactive oxygen species and modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene[1].
(±)-Darifenacin-d4 (hydrobromide) is deuterium labeled (±)-Darifenacin. (±)-Darifenacin is the racemate of Darifenacin. Darifenacin is a selective M3 muscarinic receptor antagonist[1].
PIPES-d18 is the deuterium labeled PIPES[1]. PIPES (1,4-Piperazinediethanesulfonic acid) is an important component of PIPES buffer agent used in biochemistry[2].
(Rac)-Mirabegron-d5 is a deuterium labeled (Rac)-Mirabegron. (Rac)-Mirabegron is the racemate of Mirabegron. Mirabegron is a selective β3-adrenoceptor agonist[1].
Lipoxin A4-d5 is the deuterium labeled Lipoxin A4. Lipoxin A4 (LXA4), an endogenous lipoxygenase-derived eicosanoid mediator, has potent dual pro-resolving and anti-inflammatory properties[1]. Lipoxin A4 inhibits proliferation and inflammatory cytokine/chemokine production of human epidermal keratinocytes (NHEKs) associated with the ERK1/2 and NF-kB pathways[2]. Lipoxin A4 inhibits serum amyloid A (SAA)-mediated IL-8 release with an IC50 value of 25.74 nM[3].
Tiotropium-d6 (bromide) is deuterium labeled Tiotropium (Bromide). Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
Resolvin D1-d5 is the deuterium labeled Resolvin D1. Resolvin D1 (RvD1), an endogenous pro-resolving mediator of inflammation, is derived from omega-3 docosahexaenoic acid during the resolution phase of acute inflammation. Resolvin D1 blocks proinflammatory neutrophil migration by regulating actin polymerization, reduces TNF-α–mediated inflammation in macrophages, and enhances phagocytosis of apoptotic cells by macrophages[1][2].
4-Hydroxypropranolol-d7 (hydrochloride) is a deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol, with potency comparable to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties[1][2][3].
Leukotriene E4-d5 is the deuterium labeled Leukotriene E4. Leukotriene E4 (LTE4) is produced by the action of dipeptidase on LTD4. Leukotriene E4 is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A). Leukotriene E4 accumulates in both plasma and urine and urinary excretion of Leukotriene E4 is most often used as an indicator of asthma.
Triclocarban-d4 is the deuterium labeled Triclocarban. Triclocarban (3,4,4′-Trichlorocarbanilide), a broad spectrum antibacterial compound, is widely used in a broad range of applications such as the production of soaps, skin creams, toothpastes and deodorants. Triclocarban is a potential endocrine-disrupting chemical with the capacity to modulate androgen and estrogen activities as well as other hormone-mediated biological processes[1][2][3].
(R)-Pioglitazone-d1 ((R)-U 72107-d1) is a stabilized and deuterated R-enantiomer of pioglitazone, exhibiting pharmacological properties that are beneficial for NASH treatment, including modulation of mitochondrial function, non-steroidal anti-inflammatory effects, and glucose-lowering capabilities.
L-Histidine-d5 (hydrochloride hydrate) is the deuterium labeled L-Histidine hydrochloride hydrate. L-Histidine hydrochloride hydrate (H-His-OH.HCl.H2O) is an endogenous metabolite.
Latanoprost ethyl amide-d4 (Lat-NEt-d4) is deuterium labeled Latanoprost ethyl amide. Latanoprost ethyl amide (Lat-NEt) is a latanoprost analog in which the C-1 carboxyl group has been modified to an N-ethyl amide. Prostaglandin esters have been shown to have ocular hypotensive activity.1 Prostaglandin N-ethyl amides were recently introduced as alternative prostaglandin ocular hypotensive prodrugs. Although it has been claimed that prostaglandin ethyl amides are not converted to the free acids in vivo, studies in our laboratories have shown that bovine and human corneal tissue converts the N-ethyl amides of various prostaglandins to the free acids with a conversion rate of about 2.5 μg/g corneal tissue/hr. Lat-NEt would be expected to show the typical intraocular effects of Latanoprost free acid, but with the much slower hydrolysis pharmacokinetics of the prostaglandin N-amides .
Mindeudesivir (JT001; VV116; GS-621763-d1) hydrobromide is a deuterated version of Remdesivir (HY-104077), a highly orally active nucleoside antiviral against SARS-CoV-2 and respiratory syncytial virus (RSV). Mindeudesivir hydrobromide retains the antiviral activity of Remdesivir against COVID-19, and is the first domestically produced deuterium targeting the COVID-19 .
Bendamustine-d4 is the deuterium labeled Bendamustine. Bendamustine is a DNA cross-linking agent that causes DNA breaks, with alkylating and antimetabolite properties.
Gemfibrozil-d6-1 (CI-719-d6-1) is the deuterium labeled Gemfibrozil (HY-B0258). Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively .
GS-621763-d1 is the deuterium labeled GS-621763 (HY-145119) . GS-621763, an orally bioavailable proagent of GS-441524, shows antiviral activity against SARS-CoV-2 pathogenesis in mice .
Resolvin D2-d5 is the deuterium labeled Resolvin D2. Resolvin D2 is a metabolite of docosahexaenoic acid (DHA), with anti-inflammatory, anti-infective activities. Resolvin D2 is a potent regulator of leukocytes and controls microbial sepsis. Resolvin D2 is a remarkably potent inhibitor of TRPV1 (IC50 = 0.1 nM) and TRPA1 (IC50 = 2 nM) in primary sensory neurons[1][2][3].
Asymmetric dimethylarginine-d7 (hydrochloride hydrate) is the deuterium labeled Asymmetric dimethylarginine. Asymmetric dimethylarginine is an endogenous inhibitor of nitric oxide synthase (NOS), and functions as a marker of endothelial dysfunction in a num
4-Methylanisole-d7-1 is the deuterium labeled 4-Methylanisole[1]. 4-Methylanisole (4-Methoxytoluene) is food flavoring agent and can be naturally found in Ylang Ylang fragrance oil[2].
Venlafaxine-d6-1 is deuterium labeled Venlafaxine. Venlafaxine (Wy 45030) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant[1].
11-Oxo etiocholanolone-d5 is the deuterium labeled 11-Oxo etiocholanolone. 11-Oxo etiocholanolone (11-Ketoetiocholanolone) is a metabolite of Etiocholanolone. Etiocholanolone is the excreted metabolite of testosterone and has anticonvulsant activity[1][2][3].
4-Methylpentanoic acid-d12 is the deuterium labeled 4-Methylpentanoic acid. 4-Methylpentanoic acid (Isocaproic Acid) is a Short chain fatty acid (SCFA)[1].
Umeclidinium-d5 (bromide) is the deuterium labeled Umeclidinium bromide. Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.
Bethanechol-d6 (chloride) is the deuterium labeled Bethanechol chloride. Bethanechol chloride (Carbamyl-β-methylcholine chloride), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system[1].
Prostaglandin D2-d4 is the deuterium labeled Prostaglandin D2. Prostaglandin D2 (PGD2) is one of the major PGs actively produced in the brain of various mammals[1]. Prostaglandin D2 is one of the most potent endogenous sleep promoting substances[2]. PGD2 plays a protective role by suppressing inflammation[3].
(rel)-Lopinavir-d8 ((rel)-ABT-378-d8) is the deuterium labeled Lopinavir (HY-14588) . Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity [3]. Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
DL-dithiothreitol-d10-1 is the deuterated form of DL-dithiothreitol. DL-dithiothreitol (DTT) is a strong reductant with anti-disulfidptosis activity. DL-dithiothreitol is oxidized to form a stable six-membered ring with an internal disulfide bond .
Ezetimibe-d4-1 is deuterium labeled Ezetimibe. Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
o-Phenanthroline-d8 is the deuterium labeled o-Phenanthroline. o-Phenanthroline (1,10-Phenanthroline), a metal chelator, prevents the induction of chromosomal aberrations in streptozotocin-treated cells. o-Phenanthroline (1,10-Phenanthroline) forms a red chelate with Fe2+ that absorbs maximally at 510 nm. o-Phenanthroline (1,10-Phenanthroline) is also a MMP inhibitor[1][2].
Brexpiprazole-d8-1 (OPC-34712-d8-1) is the deuterium labeled Brexpiprazole (HY-15780) . Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM) [3].
Meropenem-d6-1 (SM 7338-d6-1) is the deuterium labeled Meropenem. Meropenem (SM 7338) is a carbapenem antibiotic with broad-spectrum antibacterial activity. Meropenem has activity against susceptible and resistant N. gonorrhoeae (MIC value of 0.02-0.06 mg/mL), H. influenzae (MIC value of 0.03-0.12 mg/mL), and H. ducreyi (MIC value of 0.015-0.12 mg/mL) .
Delamanid-d4-1 is deuterated labeled Delamanid.Delamanid, a newer mycobacterial cell wall synthesis inhibitor, inhibits the synthesisi of mucolic acids .
Sudan I-d5 is a the deuterated Sudan I. Sudan I is a diazo-conjugate red dye and can be used as an additive to products such as oils, solvents or polishes. Sudan I inhibits growth of bacterial strains Clostridium perfringens and L. rhamnosus[1].
1-Octanol-d2-1 is deuterated labeled Cinnamyl acetate (HY-N7125). Cinnamyl acetate has a wide application in the flavor and fragrance industry . Cinnamyl acetate is a new broad spectrum antibacterial agent .
Sacubitril-d4 hemicalcium salt is the deuterium labeled Sacubitril hemicalcium salt (HY-15407A). Sacubitril hemicalcium salt is a potent NEP inhibitor with an IC50 of 5 nM [3] .
Sarafloxacin-d8 (hydrochloride trihydrate) is the deuterium labeled Sarafloxacin hydrochloride trihydrate. Sarafloxacin hydrochloride trihydrate is a quinolone antibiotic compound[1][2].
Amprenavir-d4-1 is deuterium labeled Amprenavir. Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.09 μM.
Hippuric acid-d5 is the deuterium labeled Hippuric acid. Hippuric Acid (2-Benzamidoacetic acid), an acyl glycine produced by the conjugation of benzoic acid and glycine, is a normal component in urine as a metabolite of aromatic compounds from food.
Adenosine monophosphate-d12 (AMP-d12) dilithium is deuterium labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction [3].
Hydroxy Bosentan-d6 is deuterium labeled Hydroxy bosentan. Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver. Ro 48-5033 assists BOS pharmacologically, retaining 10%-20% activities[1].
Bendamustine-d8 is the deuterium labeled Bendamustine[1]. Bendamustine (SDX-105 free base), a purine analogue, is a DNA cross-linking agent. Bendamustine activates DNA-damage stress response and apoptosis. Bendamustine has potent alkylating, anticancer and antimetabolite properties[2].
rac-Trandolapril-d5 (rac-RU44570-d5) is deuterium labeled Trandolapril. Trandolapril (RU44570) is a nonsulfhydryl proagent that is hydrolysed to the active diacid Trandolaprilat. Trandolapril is an orally administered angiotensin converting enzyme (ACE) inhibitor that has been used in the treatment of hypertension and congestive heart failure (CHF), and after myocardial infarction (MI) .
Umeclidinium-d10 (bromide) is the deuterium labeled Umeclidinium bromide. Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.
Cholestenone-d5 is the deuterium labeled Cholestenone. Cholestenone (4-Cholesten-3-one), the intermediate oxidation product of cholesterol, is metabolized primarily in the liver. Cholestenone is highly mobile in membranes and influences cholesterol flip-flop and efflux. Cholestenone may cause long-term functional defects in cells[1][2][3].
4-(Trifluoromethyl)aniline-d4 is deuterium labeled 4-(Trifluoromethyl)aniline. 4-(Trifluoromethyl)aniline is a DYRK1A and DYRK1B kinase inhibitor with IC50s of 54.84 nM and 186.40 nM, respectively[1].
Prostaglandin D2-d9 is the deuterium labeled Prostaglandin D2. Prostaglandin D2 (PGD2) is one of the major PGs actively produced in the brain of various mammals[1]. Prostaglandin D2 is one of the most potent endogenous sleep promoting substances[2]. PGD2 plays a protective role by suppressing inflammation[3].
Bimatoprost-d5 is a deuterium labeled Bimatoprost. Bimatoprost is a prostaglandin analog and is a topical hypotensive agent frequently used for treating ocular hypertension and glaucoma. Bimatoprost also has an antiadipogenic effect[1][2].
Tridecanoic acid-d9 is the deuterium labeled Tridecanoic acid. Tridecanoic acid (N-Tridecanoic acid), a 13-carbon medium-chain saturated fatty acid, can serve as an antipersister and antibiofilm agent that may be applied to research bacterial infections. Tridecanoic acid inhibits Escherichia coli persistence and biofilm formation[1].
Pemetrexed-d5 (disodium) is the deuterium labeled Pemetrexed disodium. Pemetrexed disodium (LY231514 disodium) is an antifolate, the Kis of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively[1].
Amlodipine-d4 (besylate) is the deuterium labeled Amlodipine besylate. Amlodipine besylate (Amlodipine benzenesulfonate), an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure and cancer[1][2][3].
Dxd-d5 is a deuterium labeled Dxd. Dxd is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a) [1].
Desloratadine-d4 hydrobromide is deuterated labeled Desloratadine (HY-B0539). Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities .
Sumatriptan-d6 succinate is the deuterium labeled Sumatriptan succinate. Sumatriptan succinate is an orally active 5-HT1 receptor agonist with Kis of 17 nM, 27 nM and 100 nM for 5-HT1D, 5-HT1B and 5-HT1A receptors, respectively. Sumatriptan succinate can be used for migraine headache research [3].
Simvastatin acid-d9 ammonium is deuterated labeled Simvastatin acid ammonium (HY-119695A). Simvastatin acid (Tenivastatin) ammonium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid ammonium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid ammonium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
Prostaglandin D1-d4 (PGD1-d4) is deuterium labeled Prostaglandin D1. Prostaglandin D1 is a prostanoid which causes contractile and relaxant on isolated human pial arteries, it is also an inhibitor of ADP-induced platelet aggregation with an IC50 value of 320 ng/ml. Prostaglandin D1 can be used for metabolic research .
Docetaxel-d5 (trihydrate) is the deuterium labeled Docetaxel (Trihydrate). Docetaxel Trihydrate (RP-56976 Trihydrate) is an antineoplastic agent and inhibits microtubule depolymerization with an IC50 value of 0.2 μM[1]. Docetaxel Trihydrate is a semisynthetic analog of taxol and attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel Trihydrate arrests the cell cycle at G2/M and leads to cell apoptosis[1][3].
N-Desethyl Sunitinib-d5 (hydrochloride) is a deuterated labeled N-Desethyl Sunitinib . N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively .
N-Desmethyl Pimavanserin-d9 hydrochloride (AC-279-d9 hydrochloride) is the deuterium labeled N-Desmethyl Pimavanserin (HY-135392). N-Desmethyl Pimavanserin is the active metabolite of Pimavanserin. Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC50 and pKd of 8.73 and 9.3, respectively .
Lurasidone-d8-1 (hydrochloride) is deuterium labeled Lurasidone (Hydrochloride). Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM .
Hydroxy Bosentan-d4 is deuterium labeled Hydroxy bosentan. Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver. Ro 48-5033 assists BOS pharmacologically, retaining 10%-20% activities[1].
22-Hydroxy Mifepristone-d6 is the deuterium labeled 22-Hydroxy Mifepristone[1]. 22-Hydroxy Mifepristone-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Kinetin riboside-d5 (N6-Furfuryladenosine-d5) is the deuterium labeled Kinetin riboside (HY-101055). Kinetin riboside, a cytokinin analog, can induce apoptosis in cancer cells. It inhibits the proliferation of HCT-15 cells with an IC50 of 2.5 μM .
Donepezil-d5 is deuterium labeled Donepezil. Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively[1].
Norethindrone acetate-d8 is the deuterium labeled Norethindrone acetate. Norethindrone acetate is a female hormone used for the research of endometriosis[1]. Norethindrone acetate-d8 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Miconazole-d5 (nitrate) is the deuterium labeled Miconazole. Miconazole (R18134) is an imidazole antifungal agent. Miconazole also has antibacterial effects[2].
Ipratropium-d7 (bromide)eis the deuterium labeled Ipratropium bromide. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with binding IC50 values of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma[1][2][3].
Paroxetine-d6-1 is a deuterated labeled Paroxetine . Paroxetine, a phenylpiperidine derivative, is a potent and selective serotonin reuptake inhibitor (SSRI). Paroxetine is a very weak inhibitor of norepinephrine (NE) uptake but it is still more potent at this site than the other SSRIs .
Benzyl benzoate-d12 is the deuterium labeled Benzyl benzoate[1]. Benzyl benzoate (Benzoic acid benzyl ester) is a fragrance ingredient in cosmetic products. Benzyl benzoate can be used for the research of Scabies and Demodex-associated inflammatory skin conditions[2][3][4].
L-Glutamine- 13C5, 15N2 is the 13C- and 15N-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells .
Uridine triphosphate- 15N2 (UTP- 15N2 dilithium; Uridine 5'-triphosphate- 15N2) dilithium is 15N labeled Uridine triphosphate (HY-107372). Uridine triphosphate (UTP;Uridine 5'-triphosphate) is a nucleotide that regulates the functions of the pancreas in endocrine and exocrine secretion, proliferation, channels, transporters, and intracellular signaling under normal and disease states.
5-Methyltetrahydrofolic acid- 13C5 is the 13C-labeled 5-Methyltetrahydrofolic acid. 5-Methyltetrahydrofolic acid (5-Methyl THF) is a biologically active form of folic acid. 5-Methyltetrahydrofolic acid is a methylated derivate of tetrahydrofolate. 5-Methyltetrahydrofolic acid is the predominant natural dietary folate and the principal form of folate in plasma and cerebrospinal fluid[1].
p,p'-DDE- 13C12 is 13C labeled p,p'-DDE. p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent androgen receptor antagonist, with an IC50 of 5 μM and a Ki of 3.5 μM .
Deoxythymidine-5'-triphosphate- 13C10, 15N2 (dTTP- 13C10, 15N2) dilithium is 13C and 15N-labeled Deoxythymidine-5'-triphosphate (HY-138615). Deoxythymidine-5'-triphosphate (dTTP) is one of the four nucleoside triphosphates. Deoxythymidine-5'-triphosphate (dTTP) is used in the synthesis of DNA.
DL-Lysine- 13C6, 15N2 hydrochloride ((±)-2,6-Diaminocaproic acid- 13C6, 15N2 hydrochloride) is 13C and 15N-labeled DL-Lysine (HY-B2236). DL-Lysine is a racemic mixture of the D-Lysine and L-Lysine. Lysine is an α-amino acid that is used in the biosynthesis of proteins.
Uridine triphosphate- 13C9 (UTP- 13C9 dilithium; Uridine 5'-triphosphate- 13C9) dilithium is 13C-labeled Uridine triphosphate (HY-107372). Uridine triphosphate (UTP;Uridine 5'-triphosphate) is a nucleotide that regulates the functions of the pancreas in endocrine and exocrine secretion, proliferation, channels, transporters, and intracellular signaling under normal and disease states.
Guanosine 5'-diphosphate- 13C10, 15N5 (GDP- 13C10, 15N5) dilithium is 13C and 15N-labeled Guanosine 5'-diphosphate (HY-113066). Guanosine 5'-diphosphate (GDP) is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K + channel. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Guanosine 5'-diphosphate can be used in the research of inflammation, such as anemia of inflammation (AI).
2'-Deoxyguanosine 5'-monophosphate- 13C10, 15N5 (disodium) is the 13C and 15N labeled 2'-Deoxyguanosine 5'-monophosphate disodium[1]. 2'-Deoxyguanosine 5'-monophosphate disodium (5′-dGMP disodium) is a mononucleotide having guanine as the nucleobase. 2'-Deoxyguanosine 5'-monophosphate disodium is a nucleic acid guanosine triphosphate (GTP) derivative[2].
4,4'-Sulfonyldiphenol- 13C12 (Bisphenol S- 13C12) is 13C labeled 4,4'-Sulfonyldiphenol. 4,4'-Sulfonyldiphenol (Bisphenol S; Bis(4-hydroxyphenyl) sulfone) is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Calcitonin- 13C6, 15N4 (salmon) (Salmon calcitonin- 13C6, 15N4) TFA is 13C and 15N-labeled Calcitonin (salmon) (HY-P0090). Calcitonin (salmon) , a calcium regulating hormone, is a dual-action amylin and calcitonin receptor agonist, could stimulate bone formation and inhibit bone resorption .
Trifluridine- 13C, 15N2 is the 13C and 15N labeled Trifluridine[1]. Trifluridine (Trifluorothymidine;5-Trifluorothymidine;TFT) is an irreversible thymidylate synthase inhibitor, and thereby suppresses DNA synthesis. Trifluridine is an antiviral agent for herpes simplex virus (HSV) infection. Trifluorothymidine also has anti-orthopoxvirus activity[2].
Cytidine-5'-triphosphate- 13C9 (Cytidine triphosphate- 13C9 dilithium; 5'-CTP- 13C9) dilithium is 13C-labeled Cytidine-5'-triphosphate (HY-125818). Cytidine 5′-triphosphate (Cytidine triphosphate; 5'-CTP) is a nucleoside triphosphate and serves as a building block for nucleotides and nucleic acids, lipid biosynthesis. Cytidine triphosphate synthase can catalyze the formation of cytidine 5′-triphosphate from uridine 5′-triphosphate (UTP). Cytidine 5′-triphosphate is an essential biomolecule?in the de novo?pyrimidine biosynthetic pathway in?T. gondii.
Deoxycytidine triphosphate- 13C9 (dCTP- 13C9 dilithium; 2′-Deoxycytidine-5′-triphosphate- 13C9) dilithium is 13C-labeled Deoxycytidine triphosphate (HY-101400). Deoxycytidine triphosphate (dCTP) is a nucleoside triphosphate that can be used for DNA synthesis. Deoxycytidine triphosphate has many applications, such as real-time PCR, cDNA synthesis, and DNA sequencing.
DMT-dA(bz) Phosphoramidite- 13C10, 15N5 is the 13C and 15N labeled DMT-dA(bz) Phosphoramidite[1]. DMT-dA(bz) Phosphoramidite is typically used in the synthesis of DNA[2].
Menaquinone-4- 13C6 is the 13C-labeled Menaquinone-4. Menaquinone-4 is a vitamin K, used as a hemostatic agent, and also a adjunctive therapy for the pain of osteoporosis.
Bisphenol AF- 13C12 is an isotopic label of Bisphenol AF. Bisphenol AF is used in polycarbonate plastic and epoxy resin manufacturing. Bisphenol AF can significantly increase intracellular ROS levels .
Thymine- 13C5, 15N2 (5-Methyluacil- 13C5, 15N2) is 13C and 15N labeled Thymine. Thymine is one of the four nucleobases in the nucleic acid of DNA and can be a target for actions of 5-fluorouracil (5-FU) in cancer treatment, with a Km of 2.3 μM .
dGTP- 13C10, 15N5 (2'-Deoxyguanosine-5'-triphosphate- 13C10, 15N5) dilithium is 13C and 15N-labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
2'-Deoxyadenosine-5'-triphosphate- 13C10, 15N5 (dATP- 13C10, 15N5) dilithium is 13C and 15N-labeled 2'-Deoxyadenosine-5'-triphosphate (HY-136648). 2'-Deoxyadenosine-5'-triphosphate (dATP) is a nucleotide used in cells for DNA synthesis (or replication), as a substrate of DNA polymerase.
5-Hydroxymethylfurfural- 13C6 (2-Hydroxymethyl-5-furfural- 13C6; 2-Formyl-5-hydroxymethylfuran- 13C6) is a 13C labeled 5-Hydroxymethylfurfural (HY-Y0051). 5-Hydroxymethylfurfural (2-Hydroxymethyl-5-furfural), derived from Cornus officinalis, inhibits yeast growth and fermentation as stressors.
p,p'-DDD- 13C12 is 13C labeled p,p'-DDD. p,p'-DDD is a major metabolite of p,p'-DDT. p,p'-DDD occurs in the feces and livers of rats, that are given p,p'-DDT by stomach tube, but not of rats injected intraperitoneally with p,p'-DDT [3].
Oleic acid- 13C18 is the 13C labeled Oleic acid (HY-N1446). Oleic acid (9-cis-Octadecenoic acid) is an abundant monounsaturated fatty acid . Oleic acid is a Na+/K+ ATPase activator .
3-Methoxytyramine-d4 (hydrochloride) is the deuterium labeled 3-Methoxytyramine hydrochloride. 3-Methoxytyramine hydrochloride is an inactive metabolite of dopamine which can activate trace amine associated receptor 1 (TAAR1)[1][2].
Eprosartan-d6 is deuterated labeled Eprosartan (HY-117743). Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively .
p-Toluic acid-d4 is the deuterium labeled p-Toluic acid[1]. p-Toluic acid (4-Methylbenzoic acid) is a substituted benzoic acid and can be used as an intermediate for the synthesis of para-aminomethylbenzoic acid (PAMBA), p-tolunitrile, etc.
Taurochenodeoxycholic acid-d4-1 (sodium) is the deuterium labeled Taurochenodeoxycholic acid. Taurochenodeoxycholic acid (12-Deoxycholyltaurine) sodium is one of the main bioactive substances of animals' bile acid. Taurochenodeoxycholic acid sodium induces apoptosis and shows obvious anti-inflammatory and immune regulation properties[1][2].
Sulfachloropyridazine- 13C6 is the 13C6 labeled Sulfachloropyridazine. Sulfachloropyridazine is a broad spectrum sulfonamide used against both Gram-positive and Gram-negative aerobic bacteria.
Lignoceric acid-d4-2 is the deuterium labeled Lignoceric acid. Lignoceric acid (Tetracosanoic acid) is a 24-carbon saturated (24:0) fatty acid, which is synthesized in the developing brain. Lignoceric acid is also a by-product of lignin production. Lignoceric acid can be used for Zellweger cerebro‐hepato‐renal syndrome and adrenoleukodystrophy research[1][2].
D-Glutamic acid-d5 is the deuterium labeled D-Glutamic acid. D-glutamic acid, an enantiomer of L- glutamic acid, is widely used in pharmaceuticals and foods[1].
Risperidone-d6 (R 64 766-d6) is the deuterium labeled Risperidone (HY-11018). Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively .
4-Aminohippuric acid-d4 is the deuterium labeled 4-Aminohippuric acid. 4-Aminohippuric acid is a diagnostic agent, useful in medical tests involving the kidney, used in the measurement of renal plasma flow.
5,6-Dihydro-5-methyluracil-d6 is the deuterium labeled 5,6-Dihydro-5-methyluracil. 5,6-Dihydro-5-methyluracil (Dihydrothymine), an intermediate breakdown product of thymine, comes from animal or plants. 5,6-Dihydro-5-methyluracil (Dihydrothymine) can be toxic when present at abnormally high levels[1].
Docosanoic acid-d4-1 (Behenic acid-d4-1) is the deuterium labeled Docosanoic acid (HY-W013049). Docosanoic acid (Behenic acid) is a long-chain saturated fatty acid. Docosanoic acid inhibits the double-stranded DNA (dsDNA) binding activity of p53 DNA binding domain, with a Kd of 12 nM. Docosanoic acid has low bioavailability and can increase cholesterol in humans [3].
Moxifloxacin-d4 is the deuterium labeled Moxifloxacin. Moxifloxacin is an orally active 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia[1][2].
Valerylcarnitine-d9 (C5:0 L-carnitine-d9) is the deuterium labeled Valerylcarnitine (HY-113266). Valerylcarnitine is an endogenous metabolite, belonging to the short-chain acylcarnitines .
L-Alanine-d7 is the deuterium labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
Betamethasone dipropionate-d10 is the deuterium labeled Betamethasone dipropionate. Betamethasone dipropionate is a glucocorticoid steroid with anti-inflammatory and immunosuppressive abilities.
Risperidone-d4 is the deuterium labeled Risperidone. Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
ATP-d14 (Adenosine 5'-triphosphate-d14) dilithium is deuterium labeled ATP (HY-B2176). ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation.
Vortioxetine-d8 (Lu AA 21004-d8) is a deuterated version of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM) .
L-Glutamine-d5 is the deuterium labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells[1][2].
Abemaciclib metabolite M2-d6 is the deuterium labeled Abemaciclib metabolite M2. Abemaciclib metabolite M2 (LSN2839567) is a metabolite of Abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50s in the range of 1-3 nM. Anti-cancer activity[1][2].
(2R)-Isopropyl 2-((((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)amino)propanoate-d5 is the deuterium labeled (2R)-isopropyl 2-((((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)amino)propanoate [
Indolelactic acid-d5 is the deuterium labeled Indolelactic acid. Indolelactic acid is a tryptophan (Trp) catabolite in Azotobacter vinelandii cultures.
Adenosine-d is the deuterium labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation[1][2].
O-Toluic acid-d7 is the deuterium labeled o-Toluic acid[1]. o-Toluic acid (2-Methylbenzoic acid) is a benzoic acid substituted by a methyl group at position 2. O-Toluic acid plays a role as a xenobiotic metabolite.
Tropisetron-d5 (SDZ-ICS-930-d5 (free base)) is deuterium labeled Tropisetron. Tropisetron (SDZ-ICS-930 free base) is an orally active anti-inflammatory and antiemetic agent. Tropisetron is 5-HT3R antagonists with a Ki of 5.3 nM. Tropisetron is also a partial agonist of α7 nicotinic receptor (α7 nAChR) with an EC50 of 1.3 μM. In addition, Tropisetron has antitumor and neuroprotective effects [3] .
Diethyl phosphate-d10-1 is the deuterium labeled Diethyl phosphate. Diethylphosphate (Diethyl phosphoric acid) is an orally active organophosphorus pesticides metabolite. Diethylphosphate can interfere with thyroid hormone-related mechanisms and affect intestinal microbes in rats .
L-Alanine-d4 is the deuterium labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
(±)11(12)-EET-d11 is the deuterium labeled (±)11(12)-EET. (±)11(12)-EET is a NLRP3 inflammasome inhibitor. (±)11(12)-EET can be used for the research of anti-inflammatory, angiogenic and cardioprotective[1][2][3][4][6].
Ribavirin- 13C5 is the 13C-labeled Ribavirin. Ribavirin (ICN-1229) is an antiviral agent against a broad spectrum of viruses including HCV, HIVl, and RSV.
Abemaciclib metabolite M18-d8 is the deuterium labeled Abemaciclib metabolite M18. Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader[1][2].
Glycerol- 13C2 is the 13C labeled Glycerol[1]. Glycerol is used in sample preparation and gel formation for polyacrylamide gel electrophoresis[2][3][4].
2-Hydroxy Ibuprofen-d6 is the deuterium labeled 2-Hydroxy Ibuprofen. 2-Hydroxy Ibuprofen is a metabolite of Ibuprofen. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively[1][2].
Norethindrone- 13C2 (Norethisterone- 13C2) is the 13C labeled Norethindrone (HY-B0554) . Norethindrone is a female progestin approved by FDA for the treatment of endometriosis, uterine bleeding caused by abnormal hormone levels, and secondary amenorrhea [3] .
TCEP-d12 (hydrochloride) (Tris(2-?carboxyethyl)?phosphine hydrochloride-d12) is deuterium labeled TCEP (hydrochloride). TCEP hydrochloride (Tris(2-carboxyethyl)phosphine hydrochloride) is a non-thiol reducing agent that is more stable and produces a faster S-S reductive reaction than other chemical reductants. TCEP hydrochloride is a trialkylphosphine, selectively reduces protein disuldes without altering the properties or interacting with thiol-directed agents in the reaction mixture. TCEP hydrochloride is also a commonly used reducing agent in the DNA/AuNP chemistry [3] .
Docosanoic acid-d4-2 (Behenic acid-d4-2) is the deuterium labeled Docosanoic acid (HY-W013049). Docosanoic acid (Behenic acid) is a long-chain saturated fatty acid. Docosanoic acid inhibits the double-stranded DNA (dsDNA) binding activity of p53 DNA binding domain, with a Kd of 12 nM. Docosanoic acid has low bioavailability and can increase cholesterol in humans [3].
DL-Lysine-4,4,5,5-d4 (dihydrochloride) is the deuterium labeled DL-Lysine. DL-Lysine is a racemic mixture of the D-Lysine and L-Lysine. Lysine is an α-amino acid that is used in the biosynthesis of proteins[1].
D-Threonine-d2 is the deuterium labeled D-Threonine. D-Threonine (H-D-Thr-OH) is an enantiomer of L-threonine. D-Threonine is a metabolite of Saccharomyces cerevisiae.
14(S)-HDHA-d5 (14(S)-HDoHE-d5) is deuterium labeled 14(S)-HDHA. 14(S)-HDHA (14(S)-HDoHE) is an oxygenation product of Docosahexaenoic acid (DHA). 14(S)-HDHA is a marker reflecting activation of a Docosahexaenoic acid carbon 14-lipoxygenation pathway .
p-Cresol sulfate-d4 (potassium) is deuterium labeled p-Cresyl sulfate (potassium). p-Cresyl sulfate potassium is a uremic toxin that binds to a prototype protein. p-Cresyl sulfate potassium activates the JNK and p38 MAPK signaling pathways. p-Cresyl sulfate potassium has pro-inflammatory activity [3].
1-Butynylbenzene-d5 is the deuterium labeled 1-Butynylbenzene[1]. 1-Butynylbenzene-d5 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Sulfadimethoxine- 13C6 is the 13C-labeled Sulfadimethoxine. Sulfadimethoxine (Sulphadimethoxine) is a sulfonamide antibiotic used to treat many infections[1][2].
Hydrochlorothiazide- 13C6 is the 13C labeled Hydrochlorothiazide[1]. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect[2][3][4].
Ciraparantag-d8 tetrahydrochloride diacetate (PER977-d8 tetrahydrochloride diacetate) is the deuterium labeled Ciraparantag (HY-18660). Ciraparantag is a thrombin and factor Xa inhibitor. Ciraparantag is a broad-spectrum reversal agent for anticoagulants, including low-molecular-weight heparin, unfractionated heparin, and certain direct oral anticoagulants. It is reported to antagonize the effects of all coagulants except VKAs and agratroban [3] .
(E)-β-Farnesene-d6 is deuterated labeled Nerol (HY-N7063). Nerol is a constituent of neroli oil. Nerol Nerol triggers mitochondrial dysfunction and induces apoptosis via elevation of Ca 2+ and ROS. Antifungal activity .
Afatinib-d6 (dimaleate) is the deuterium labeled Afatinib dimaleate. Afatinib dimaleate is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively[1][2].
Veratric acid-d6 is deuterium labeled Veratric acid. Veratric acid (3,4-Dimethoxybenzoic acid) is an orally active phenolic compound derived from vegetables and fruits, has antioxidant[1] and anti-inflammatory activities[3]. Veratric acid also acts as a protective agent against hypertension-associated cardiovascular remodelling[2]. Veratric acid reduces upregulated COX-2 expression, and levels of PGE2, IL-6 after UVB irradiation[3].
Abemaciclib metabolite M20-d8 is the deuterium labeled Abemaciclib metabolite M20. Abemaciclib metabolite M20 (LSN3106726), the active metabolite of Abemaciclib, is a selective CDK4/6 inhibitor[1].
Patulin- 13C7 (Terinin- 13C7) is the 13C labeled Patulin (HY-N6779) . Patulin (Terinin) is a mycotoxin produced by fungi including the Aspergillus, Penicillium, and Byssochlamys species, is suspected to be clastogenic, mutagenic, teratogenic and cytotoxic. Patulin induces autophagy-dependent apoptosis through lysosomal-mitochondrial axis, and causes DNA damage [3] .
Calcifediol-d6 monohydrate is the deuterium labeled Calcifediol monohydrate. Calcifediol monohydrate (25-hydroxy Vitamin D3 monohydrate), is an effective VDR ligand and VD supplement. Calcifediol is a prohormone of the vitamin D endocrine system (VDES) and is hydroxylated in the liver to produce the active form, calcitriol. Calcifediol can rapidly increase serum VD levels [3].
2-Hydroxypalmitic acid-d30 (2-Hydroxyhexadecanoic acid-d30) is deuterium labeled 2-Hydroxypalmitic acid. 2-Hydroxypalmitic acid is an intermediate in phytosphingosine metabolism .
H-D-Trp-OH-d5 (D-Tryptophan-d5) is the deuterium labeled H-D-Trp-OH. H-D-Trp-OH is a D-stereoisomer of tryptophan and occasionally found in naturally produced peptides such as the marine venom peptide.
Vortioxetine-d8 (Lu AA 21004-d8) hydrobromide is the deuterated form of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM) .
Perospirone-d8 (SM-9018-d8 (free base)) is deuterium labeled Perospirone. Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT2A receptor (Ki=0.6 nM) and dopamine D2 receptor (Ki=1.4 nM), and also a partial agonist of 5-HT1A receptor (Ki=2.9 nM). Perospirone is an atypical antipsychotic agent and has the potential for schizophrenic disease research [3].
DPPC-d9-1 is the deuterium labeled DPPC. DPPC (129Y83) is a zwitterionic phosphoglyceride that can be used for the preparation of liposomal monolayers[1]. DPPC-liposome serves effectively as a delivery vehicle for inducing immune responses against GSL antigen in mice[2].
4-Oxofenretinide-d4 (4-Oxo-4-HPR-d4) is deuterium labeled 4-Oxofenretinide. 4-Oxofenretinide (4-Oxo-4-HPR) is a metabolite of Fenretinide (HY-15373). 4-Oxofenretinide induces cell growth inhibition in ovarian, breast, and neuroblastoma tumor cell lines. 4-Oxofenretinide causes a marked accumulation of cells in G2-M. 4-Oxofenretinide induces cancer cell apoptosis through caspase-9 .
Ibuprofen- 13C6 ((±)-Ibuprofen- 13C6) is a 13C labeled Ibuprofen (HY-78131). Ibuprofen ((±)-Ibuprofen) is a potent, orally active, selective COX-1 inhibitor with an IC50 value of 13 μM. Ibuprofen inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen ((±)-Ibuprofen) can be used in the research of pain, swelling, inflammation, infection, immunology, cancers [3] .
Histamine- 13C5 is the 13C labeled Histamine (HY-B1204). Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter .
(Rac)-DPPC-d6 is a deuterated labeled DPPC . DPPC (129Y83) is a phosphoglyceride that can be used to prepare lipid monolayers, bilayers, and liposomes. DPPC is the main lipid component of pulmonary surfactant. Dppc-liposome can be effectively used as a delivery vector to induce an immune response against GSL antigen in mice [3] .
p-Toluic acid-d7 is the deuterium labeled p-Toluic acid[1]. p-Toluic acid (4-Methylbenzoic acid) is a substituted benzoic acid and can be used as an intermediate for the synthesis of para-aminomethylbenzoic acid (PAMBA), p-tolunitrile, etc.
Monomethyl phthalate-d4 (2-(Methoxycarbonyl)benzoic acid-d4) is the deuterium labeled Monomethyl phthalate. Monomethyl phthalate is a phthalate metabolite. Monomethyl phthalate acts as a urinary biomarker of phthalates exposure and can be used as a standard for the determination of thyroid cancer and benign nodule .
Sulfacetamide- 13C6 (Sulphacetamide 13C6) is the 13C6 labeled Sulfacetamide (HY-N7123). Sulfacetamide (Sulphacetamide) is a sulfonamide antibiotic that can be used for the study of ocular infections. Sulfacetamide has antifungal and antibacterial activities .
Monooctyl phthalate-d4 (Mono-n-octyl phthalate-d4) is a deuterium labeled Monooctyl phthalate (HY-133671). Monooctyl phthalate (Mono-n-octyl phthalate) exhibits antimycobacterial activity with a MIC of 20 μg/mL .
2-Phenylethyl isothiocyanate-d5 isothiocyanate-d5 is the deuterium labeled 2-Phenylethyl isothiocyanate[1]. 2-Phenylethyl isothiocyanate is a potent antifungal agent. 2-Phenylethyl isothiocyanate significantly inhibited spore germination and mycelial growth of Alternaria alternata, with a MIC (minimum inhibitory concentration) of 1.22 mM. The antifungal effect of 2-Phenylethyl isothiocyanate against Alternaria alternata might be via reduction in toxin content and breakdown of cell membrane integrity[2][3].
Cytidine 5′-monophosphate- 13C9 (5'-Cytidylic acid- 13C9 dilithium; 5'-CMP- 13C9) dilithium is 13C-labeled Cytidine 5'-monophosphate (HY-W009162). Cytidine 5'-monophosphate (5'-Cytidylic acid) is a nucleotide which is used as a monomer in RNA. Cytidine 5'-monophosphate consists of the nucleobase cytosine, the pentose sugar ribose, and the phosphate group.
5'-Guanylic acid- 13C10 (5'-GMP- 13C10 dilithium; 5'-guanosine monophosphate- 13C10) dilithium is 13C-labeled 5'-Guanylic acid (HY-N5134). 5'-Guanylic acid (5'-GMP) is involved in several metabolic disorders, including the AICA-ribosiduria pathway, adenosine deaminase deficiency, adenine phosphoribosyltransferase deficiency (aprt), and the 2-hydroxyglutric aciduria pathway.
N-Acetyl mesalazine-13C6 is a deuterated labeled N-Acetyl mesalazine . N-Acetyl mesalazine (N-Acetyl-5-aminosalicylic acid) is the metabolite of 5-Aminosalicylic Acid (HY-15027) with endoscopic activity. N-Acetyl mesalazine can be used for the research of ulcerative colitis .
Cytidine- 13C9 (Cytosine β-D-riboside- 13C9; Cytosine-1-β-D-ribofuranoside- 13C9) is 13C labeled Cytidine (HY-B0158). Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catecholamine synthesis, and mitochondrial function [3].
rU Phosphoramidite- 13C9, 15N2 (DMT-2'O-TBDMS-rU phosphoramidite- 13C9, 15N2) is 13C and 15N-labeled rU Phosphoramidite (HY-W048482). rU Phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
Uridine 5'-monophosphate- 13C9, 15N2 (5'- Uridylic acid- 13C9, 15N2) dilithium is 13C and 15N-labeled Uridine 5'-monophosphate (HY-101981). Uridine 5'-monophosphate (5'- Uridylic acid), a monophosphate form of UTP, can be acquired either from a de novo pathway or degradation products of nucleotides and nucleic acids in vivo and is a major nucleotide analogue in mammalian milk.
Pregnenolone monosulfate (sodium)- 13C2,d2 is the 13C- and deuterium labeled Pregnenolone monosulfate sodium. Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium salt acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium salt can protect the brain from cannabis intoxication[1][2]. Pregnenolone monosulfate sodium salt is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
Droxidopa- 13C2, 15N (hydrochloride) is deuterium labeled Droxidopa. Droxidopa(L-DOPS), the mixture of Droxidopa (w/w80%) and Pharmaceutical starch (w/w20%), acts as a proagent to the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline); Droxidopa(L-DOPS) is capable of crossing the protective blood–brain barrier[1][2].
Acetaminophen- 13C2, 15N is the 13C and 15N labeled Acetaminophen[1]. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM;is a widely used antipyretic and analgesic agent[2][3][4]. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor[5].
15-Deoxy-Δ-12,14-prostaglandin J2-d4 is the deuterium labeled 15-Deoxy-Δ-12,14-prostaglandin J2. 15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2. 15-Deoxy-Δ-12,14-prostaglandin J2 is a selective PPARγ (EC50 of 2 µM) and a covalent PPARδ agonist. 15-Deoxy-Δ-12,14-prostaglandin J2 promotes efficient differentiation of C3H10T1/2 fibroblasts to adipocytes with an EC50 of 7 μM[1][2].
(R)-3-Hydroxybutanoic acid- 13C4 sodium is a 13C labeled (R)-3-Hydroxybutanoic acid (HY-W051723). (R)-3-Hydroxybutanoic acid is a metabolite converted from acetoacetic acid catalyzed by 3-hydroxybutyrate dehydrogenase. (R)-3-Hydroxybutanoic acid can function as a nutrition source, and as a precursor for vitamins, antibiotics and pheromones .
(R)-3-Hydroxybutanoic acid- 13C2 (sodium) is the 13C labeled (R)-3-Hydroxybutanoic acid (sodium) (HY-W015851). (R)-3-Hydroxybutanoic acid (sodium) is a metabolite converted from acetoacetic acid catalyzed by 3-hydroxybutyrate dehydrogenase. (R)-3-Hydroxybutanoic acid sodium can function as a nutrition source, and as a precursor for vitamins, antibiotics and pheromones[1][2][3].
1,2-Dioleoyl-3-lauroyl-rac-glycerol- 13C3 is the 13C-labeled 1,2-Dioleoyl-3-lauroyl-rac-glycerol (HY-165089), 1,2-Dioleoyl-3-lauroyl-rac-glycerol (1,2-Olein-3-laurin) is a triglyceride identified by specific analytical methods in human milk, infant formula, other mammalian milk, and vegetable oils, with specific structural and distribution characteristics.
Fmoc-Gly-OH- 13C2, 15N is a 15N-labeled and 13C-labled Crystal Violet. Crystal violet (Basic Violet 3) is a triarylmethane dye. Crystal Violet (Gentian Violet) has antiviral effects against H1N1 and also has prominent bactericidal activities.
2-Hydroxyestrone- 13C6 is the 13C-labeled 2-Hydroxyestrone. 2-Hydroxyestrone (Catecholestrone) is a specific receptor-mediated antiestrogenic agent. 2-Hydroxyestrone is anticarcinogenic[1][2].
3-Hydroxybutyric acid-d2 (sodium) is the deuterium labeled 3-Hydroxybutyric acid sodium[1]. 3-Hydroxybutyric acid sodium (β-Hydroxybutyric acid sodium) is a metabolite that is elevated in type I diabetes. 3-Hydroxybutyric acid sodium can modulate the properties of membrane lipids[2].
Mycophenolic acid-13C17 (Mycophenolate-13C17) is the 13C labeled Mycophenolic acid (HY-B0421). Mycophenolic acid is a potent uncompetitive inosine monophosphate dehydrogenase (IMPDH) inhibitor with an EC50 of 0.24 μM. Mycophenolic acid demonstrates antiviral effects against a wide range of RNA viruses including influenza. Mycophenolic acid is an immunosuppressive agent. Antiangiogenic and antitumor effects.
γ-Aminobutyric acid-d2 is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
N-Nitrosodibutylamine-d18 is the deuterium labeled N-Nitrosodibutylamine[1]. N-Nitrosodibutylamine (N-Nitroso-di-n-butylamine) is a nitrosamine enriched in the drinking water[2].
Progesterone-d9 is the deuterium labeled Progesterone. Progesterone is a steroid hormone that regulates the menstrual cycle and is crucial for pregnancy.
trans-Cinnamic acid-d7 is the deuterium labeled trans-Cinnamic acid[1]. trans-Cinnamic acid is a natural antimicrobial, with minimal inhibitory concentration (MIC) of 250 μg/mL against fish pathogen A. sobria, SY-AS1[2].
2'-Deoxyadenosine-5'-triphosphate-d14 (dATP-d14) dilithium is deuterium labeled 2'-Deoxyadenosine-5'-triphosphate (HY-136648). 2'-Deoxyadenosine-5'-triphosphate (dATP) is a nucleotide used in cells for DNA synthesis (or replication), as a substrate of DNA polymerase.
Niclosamide- 13C6 (monohydrate) is the 13C labeled Niclosamide monohydrate[1]. Niclosamide (BAY2353) monohydrate is an orally active antihelminthic agent used in parasitic infection research[2]. Niclosamide monohydrate is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells[5]. Niclosamide monohydrate has biological activities against cancer, and inhibits DNA replication in Vero E6 cells[3][4][6].
p-Cresol sulfate-d7 (potassium) is the deuterium labeled p-Cresyl sulfate potassium. p-Methylphenyl potassium sulfate is a prototype protein-bound uremic toxin[1][2].
Sucrose-13C6 is the 13C labeled Sucrose[1]. Sucrose (D-(+)-Saccharose) is a disaccharide which is composed of two monosaccharides, glucose and fructose. Sucrose can be applied in some animal models, including metabolic disease, obesity, diet on preference, and diabetes, et al[2].
N-desmethyl Enzalutamide-d6 is a deuterium labeled N-desmethyl Enzalutamide. N-desmethyl Enzalutamide is an active metabolite of Enzalutamide. N-desmethyl Enzalutamide is the active metabolite of Enzalutamide. N-desmethyl Enzalutamide demonstrates primary and secondary pharmacodynamics of similar potency to Enzalutamide and circulates at approximately the same plasma concentrations as enzalutamide[1].
Adenosine monophosphate- 13C5 (AMP- 13C5) is 13C labeled Adenosine monophosphate. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction .
Bis(1-chloro-2-propyl) phosphate-d12 is deuterium labeled Bis(1-chloro-2-propyl) phosphate. Bis(1-chloro-2-propyl) phosphate (BCIPP) is a metabolite of organophosphate flame retardants (OPFR) that may alter energy metabolism by influencing the levels of steroid hormones, such as cortisol and cortisone. Bis(1-chloro-2-propyl) phosphate holds potential for research on metabolism-related diseases caused by environmental exposure .
N-Dodecyl-β-D-maltoside-d25 (Lauryl Maltoside-d25) is deuterium labeled N-Dodecyl-β-D-maltoside (HY-128974). N-Dodecyl-β-D-maltoside is a non-ionic detergent. N-Dodecyl-β-D-maltoside has strong adsorption on alumina, titanium dioxide and hematite. N-Dodecyl-β-D-maltoside can promote the reactivation of various proteins. N-Dodecyl-β-D-maltoside can effectively stabilize photoactive reaction center complexes (RCs) and inhibit the degradation of Rhodopseudomonas spheroides R-26 reaction center in solution. N-Dodecyl-β-D-maltoside can be used for purification and stabilization of RNA polymerase and for detection of protein-lipid interactions [3] .
N-Nitrosodibutylamine-d9 is the deuterium labeled N-Nitrosodibutylamine[1]. N-Nitrosodibutylamine (N-Nitroso-di-n-butylamine) is a nitrosamine enriched in the drinking water[2].
Erdosteine- 13C4 is a 13C-labeled Erdosteine. Erdosteine inhibits lipopolysaccharide (LPS)-induced NF-κB activation[1][2]. Erdosteine has muco-modulatory, anti-bacterial, anti-inflammatory and anti-oxidant effects[3].
Prasugrel-13C6 is a deuterated labeled Prasugrel . Prasugrel (PCR 4099), a thienopyridine and proagent, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation .
Sacubitril-13C4 (AHU-377-13C4) is a 13C-labeled version of Sacubitril (HY-15407). Sacubitril is an orally active inhibitor of neprilysin NEP (IC50=5 nM). Sacubitril is used in research on heart failure, hypertension and COVID-19 [3] .
trans-Cinnamic acid-d5 is the deuterium labeled trans-Cinnamic acid[1]. trans-Cinnamic acid is a natural antimicrobial, with minimal inhibitory concentration (MIC) of 250 μg/mL against fish pathogen A. sobria, SY-AS1[2].
2-Ketoglutaric acid-d4 is the deuterium labeled 2-Ketoglutaric acid[1]. 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM)[2].
8-Isoprostaglandin E2-d4 (iPE2-III-d4) is deuterium labeled 8-Isoprostaglandin E2. 8-Isoprostaglandin E2 (iPE2-III) is a member of the isoprostane class of prostanoids. 8-Isoprostaglandin E2 acts at the receptor for thromboxane A2 (the TP) in vivo to induce vasoconstriction and platelet aggregation. 8-Isoprostaglandin E2 enhances receptor-activated NFkappa B ligand (RANKL)-dependent osteoclastic potential of marrow hematopoietic precursors via the cAMP pathway .
N-Palmitoyl-D-sphingomyelin-d9 (Sphingomyelin 16:0-d9) is deuterium labeled N-Palmitoyl-D-sphingomyelin. N-Palmitoyl-D-sphingomyelin (Sphingomyelin 16:0) (Compound SM-03) can be used for the synthesis of lipid nanoparticles .
9-Aminoacridine-13C6 is the 13C-labeled 9-Aminoacridine(HY-B1422). 9-Aminoacridine, a fluorescent probe, acts as an indicator of pH for quantitative determination of transmembrane pH gradients (inside acidic). 9-Aminoacridine is an antimicrobial. 9-Aminoacridine exerts its antimicrobial activity by interacting with specific bacterial DNA and disrupting the proton motive force in K. pneumoniae. 9-Aminoacridine is a HIV-1 inhibitor and inhibits HIV LTR transcription highly dependent on the presence and location of the amino moiety. 9-Aminoacridine inhibits virus replication in HIV-1 infected cell lines. 9-Aminoacridine is used as a Rifampin (RIF; HY-B0272) adjuvant for the multidrug-resistant K. pneumoniae infections [3].
Arachidonic acid- 13C4 (Immunocytophyt- 13C4) is 13C labeled Arachidonic acid. Arachidonic acid (Immunocytophyt) is a polyunsaturated omega-6 fatty acid and a major constituent of biomembranes. Arachidonic acid also acts as the substrate for various lipid mediators, such as prostaglandins (PGs). Arachidonic acid improves cognitive response and cardiovascular function .
Estradiol valerianate-d4 is the deuterium labeled Estradiol valerianate. Estradiol valerianate (β-estradiol 17-valerate) is a synthetic estrogen widely used in combination with other steroid hormones in hormone replacement therapy agents.
Diclofenac- 13C6 (Sodium) is the 13C6 labeled Diclofenac (Sodium). Diclofenac Sodium (GP 45840) is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac Sodium induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
Lactate-d4 sodium (60% in water) is the deuterium labeled Lactate sodium (60% in water). Lactate sodium (60% in water) is the product of glycogenolysis and glycolysis. Lactate sodium (60% in water) functions in a variety of biochemical processes .
Resolvin E1-d4-1 is the deuterium labeled Resolvin E1. Resolvin E1 (RvE1), a potent endogenous pro-resolving mediator of inflammation, is derived from omega-3 fatty acid eicosapentaenoic acid (EPA). Resolvin E1 is endogenously biosynthesized from EPA in the presence of Aspirin during the spontaneous resolution phase of acute inflammation, where specific cell-cell interactions occur. Resolvin E1 possesses unique counterregulatory actions that inhibit polymorphonuclear leukocyte (PMN) transendothelial migration. Resolvin E1 also acts as a potent inhibitor of leukocyte infiltration, dendritic cell migration, and IL-12 production[1][2].
Penicillin V- 13C6 (potassium) is the 13C6 labeled Penicillin V (potassium). Penicillin V Potassium (Phenoxymethylpenicillin potassium salt) is an orally active antibiotic. Penicillin V Potassium inhibits the growth of Streptococci, C. difficile and S. aureus. Penicillin V Potassium can be used for the research of otitis, sinusitis, pharyngitis and tonsillitis.
Odevixibat- 13C6 is 13C labeled Odevixibat (HY-109120). Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis .
Docosahexaenoic acid ethyl ester-d5-1 is the deuterium labeled Docosahexaenoic acid ethyl ester. Docosahexaenoic acid ethyl ester (Ethyl docosahexaenoate) is a 90% concentrated ethyl ester of docosahexaenoic acid manufactured from the microalgal oil. Docosahexaenoic acid ethyl ester enhances 6-hydroxydopamine-induced neuronal damage by induction of lipid peroxidation in mouse striatum. Docosahexaenoic acid (DHA) is a key component of the cell membrane, and its peroxidation is inducible due to the double-bond chemical structure. Docosahexaenoic acid has neuroprotective effects[1][2][3].
Methyl(E)-cinnamate-d7 is the deuterium labeled Methyl (E)-cinnamate[1]. Methyl (E)-cinnamate (EMC), a phytochemical constituent isolated from Alpinia katsumadai Hayata, is a natural flavor compound with anti-inflammatory properties. Methyl (E)-cinnamate is widely used in the food and commodity industry[2].
Guaiacol- 13C6 is the 13C labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
dGTP-d14 (2'-Deoxyguanosine-5'-triphosphate-d14) dilithium is deuterium labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
Vandetanib-13C6 is a deuterated labeled Vandetanib . Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) .
p-Coumaric acid-d6 is the deuterium labeled p-Coumaric acid (HY-N0351). p-Coumaric acid is the abundant isomer of cinnamic acid which has antitumor and anti-mutagenic activities[1][2].
Anthracene-9-carboxylic acid-d9 is the deuterium labeled Anthracene-9-carboxylic acid[1]. Anthracene-9-carboxylic acid (9-Anthracenecarboxylic acid) is an anthracene derivative traditionally used to block and identify Ca2+-activated Cl- currents (CaCCs) in various cell types, like diverse smooth muscle cells, epithelial cells and salivary gland cells[2].
Mead acid-d6 is the deuterium labeled Mead acid. Mead acid (5,8,11-Eicosatrienoic acid), an unsaturated (Omega-9) fatty acid, is an indicator of essential fatty acid deficiency[1].
Niclosamide- 13C6 is the 13C6 labeled Niclosamide. Niclosamide (BAY2353) is an orally bioavailable chlorinated salicylanilide, with anthelmintic and potential antineoplastic activity. Niclosamide (BAY2353) inhibits STAT3 with IC50 of 0.25 μM in HeLa cells and inhibits DNA replication in a cell-free assay.
Gallic acid-d2 is the deuterium labeled Gallic acid[1]. Gallic acid (3,4,5-Trihydroxybenzoic acid) is a natural polyhydroxyphenolic compound and an free radical scavenger to inhibit cyclooxygenase-2 (COX-2)[2]. Gallic acid has various activities, such as antimicrobial, antioxidant, antimicrobial, anti-inflammatory, and anticance activities[3].
Pragliflozin- 13C6 (ASP1941- 13C6) is 13C labeled Ipragliflozin. Ipragliflozin (ASP1941) is an orally active and selective SGLT2 inhibitor with IC50s of 7.38 and 1876 nM, 6.73 and 1166 nM, 5.64 and 1380 nM for human SGLT2 and SGLT1, rat SGLT2 and SGLT1, mouse SGLT2 and SGLT1, respectively. Antidiabetic agent .
Mono(5-carboxy-2-ethylpentyl) phthalate-d4 (MECPP-d4) is a deuterium labeled Mono(5-carboxy-2-ethylpentyl) phthalate (HY-133675). Mono(5-carboxy-2-ethylpentyl) phthalate (MECPP) is a metabolite of Di-(2-ethylhexyl) phthalate (DEHP). Di(2-ethylhexyl) phthalate is the predominant plasticizer added to rigid polyvinyl chloride (PVC) to impart flexibility, temperature tolerance, optical clarity, strength and resistance to kinking [3].
DMT-dA(bz) Phosphoramidite-d9 (DA-CE phosphoramidite-d9) is deuterium labeled DMT-dA(bz) Phosphoramidite (HY-W013059). DMT-dA(bz) Phosphoramidite is typically used in the synthesis of DNA.
Enzalutamide carboxylic acid-d6 is the deuterium labeled Enzalutamide carboxylic acid (MDV3100 carboxylic acid). Enzalutamide carboxylic acid is an inactive metabolite of Enzalutamide[1].
c is deuterium labeled Exatecan mesylate (HY-13631A). Exatecan mesylate is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL). Exatecan mesylate can be used in cancer research .
Eltrombopag- 13C4 (SB-497115- 13C4) is 13 sup>C-labeled Z-Eltrombopag. Z-Eltrombopag is an orally active thrombopoietin-receptor non-peptide agonist with platelet-stimulating activity for the study of chronic immune thrombocytopenia. Eltrombopag also has strong inhibitory effects on multidrug-resistant Staphylococcus aureus (Staphylococcus aureus) and can induce apoptosis (apoptosis) in liver cancer cells [3] .
Sumatriptan-d5 is deuterated labeled Sumatriptan (HY-B0121B). Sumatriptan (GR 43175) is an orally active 5-HT1 receptor agonist with IC50s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT1D, 5-HT1B and 5-HT1F receptors, respectively. Sumatriptan can be used for migraine headache research [3] .
Meclofenamic acid- 13C6 is the 13C6 labeled Meclofenamic acid. Meclofenamic Acid (Meclofenamate), a non-steroidal, anti-inflammatory agent, is a highly selective fat mass and obesity-associated (FTO) enzyme inhibitor. Meclofenamic Acid competes with FTO binding for the m(6)A-containing nucleic acid. Meclofenamic acid is a non-selective gap-junction blocker.
Methyl (E)-cinnamate-d5 is the deuterium labeled Methyl (E)-cinnamate[1]. Methyl (E)-cinnamate (EMC), a phytochemical constituent isolated from Alpinia katsumadai Hayata, is a natural flavor compound with anti-inflammatory properties. Methyl (E)-cinnamate is widely used in the food and commodity industry[2].
Mono(2-ethyl-5-hydroxyhexyl) phthalate-d4 (MEHHP-d4) is a deuterium labeled Mono(2-ethyl-5-hydroxyhexyl) phthalate (HY-133677). Mono(2-ethyl-5-hydroxyhexyl) phthalate (MEHHP) is an oxidative metabolite of Di(2-ethylhexyl) phthalate (DEHP). Mono(2-ethyl-5-hydroxyhexyl) phthalate may protective sperm DNA damage. Di(2-ethylhexyl) phthalate is the predominant plasticizer added to rigid polyvinyl chloride (PVC) to impart flexibility, temperature tolerance, optical clarity, strength and resistance to kinking [3].
DL-Phenylalanine-d5 (hydrochloride) is the deuterium labeled DL-Phenylalanine hydrochloride. L-Phenylalanine hydrochloride is an essential amino acid isolated from Escherichia coli. L-Phenylalanine hydrochloride is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine hydrochloride is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine hydrochloride is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
(R)-Bromoenol lactone-d7 ((R,E)-Bromoenol lactone-d7) is deuterium labeled (R)-Bromoenol lactone. (R)-Bromoenol lactone ((R)-BEL) is an irreversible, chiral, mechanism-based inhibitor of calcium-independent phospholipase γ (iPLA2γ). (R)-BEL inhibits human recombinant iPLA2γ with an IC50 of approximately 0.6 μM .
γ-Aminobutyric acid-d6 is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
Isosorbide dinitrate- 13C6 is the 13C labeled Isosorbide dinitrate[1]. Isosorbide dinitrate (ISDN) is an NO donor that prevents LV remodeling and degradation of cardiac function following myocardial infarction (MI)[2].
trans-2-Decenal-d2 is deuterated labeled Coumarin (HY-N0709). Coumarin is a potent and orally active anti-inflammatory agent. Coumarin shows an antinociceptive effect. Coumarin shows antibacterial, antifungal and anticancer activity .
Monobenzyl phthalate-d4 is the deuterium labeled Monobenzyl phthalate. Monobenzyl phthalate (2-((Benzyloxy)carbonyl)benzoic acid) is the urinary metabolite exposuring to phthalates, such as, diethylhexyl phthalate (DEHP)[1].
L-Phenylalanine- 13C9, 15N,d8 is the deuterium, 13C-, and 15-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
Levoglucosan- 13C6 is the 13C labeled Levoglucosan[1]. Levoglucosan (1,6-Anhydro-β-D-glucopyranose) is an anhydrosugar produced through glucan pyrolysis and is widely found in nature[2].
Angiotensin II human- 13C6, 15N TFA (Ang II- 13C6, 15N TFA) is 13C- and 15N-labeled Angiotensin II human (TFA) (HY-13948B). Angiotensin II human (Angiotensin II) TFA is a vasoconstrictor and a major bioactive peptide of the renin/angiotensin system. Angiotensin II human TFA plays a central role in regulating human blood pressure, which is mainly mediated by interactions between Angiotensin II and the G-protein-coupled receptors (GPCRs) Angiotensin II type 1 receptor (AT1R) and Angiotensin II type 2 receptor (AT2R). Angiotensin II human TFA stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions [3].
Liothyronine- 13C9, 15N is the 13C and 15N labeled Liothyronine[1]. Liothyronine is an active form of thyroid hormone. Liothyronine is a potent thyroid hormone receptors TRα and TRβ agonist with Kis of 2.33 nM for hTRα and hTRβ, respectively[2][3][4].
AICAR- 13C2, 15N (Acadesine- 13C2, 15N; AICA Riboside- 13C2, 15N) is the 13C and 15N labeled AICAR (HY-13417) . AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor [3].
Glucosamine- 13C6, 15N (hydrochloride) is the 13C and 15N labeled Glucosamine hydrochloride. Glucosamine hydrochloride (D-Glucosamine hydrochloride) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids,
Avibactam sodium salt- 13C5 (NXL-104- 13C5) is 13C labeled Avibactam (sodium). Avibactam sodium (NXL-104) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively .
1,2-Distearoyl-sn-glycero-3-phosphorylethanolamine-d70 is deuterium labeled 1,2-Distearoyl-sn-glycero-3-phosphorylethanolamine. 1,2-Distearoyl-sn-glycero-3-phosphorylethanolamine (DSPE) is a phosphoethanolamine (PE) lipid that can be used in the synthesis
Oxiran-2-ylmethyl hexadecanoate-d31 is deuterium labeled Glycidyl palmitate. Glycidyl Palmitate is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Taurine- 13C2 is the 13C-labeled Taurine. Taurine, a sulphur-containing amino acid and an organic osmolyte involved in cell volume regulation, provides a substrate for the formation of bile salts, and plays a role in the modulation of intracellular free calcium concentration. Taurine has the ability to activate autophagy in adipocytes[1][2][3].
Uridine 5'-monophosphate-d11 (5'-?Uridylic acid-d11) dilithium is deuterium labeled Uridine 5'-monophosphate (HY-101981). Uridine 5'-monophosphate (5'-?Uridylic acid), a monophosphate form of UTP, can be acquired either from a de novo pathway or degradation products of nucleotides and nucleic acids in vivo and is a major nucleotide analogue in mammalian milk.
L-Phenylalanine-d is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
L-Phenylalanine-d2 is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
3-Hydroxybutyric acid-d4 (sodium) is the deuterium labeled 3-Hydroxybutyric acid. 3-Hydroxybutyric acid (β-Hydroxybutyric acid) is a metabolite that is elevated in type I diabetes. 3-Hydroxybutyric acid can modulate the properties of membrane lipids[1].
Butyric acid-13C4 sodium (Butanoic acid-13C4 sodium) is a stable isotope labeled compound with the activity of promoting cell proliferation and regulating gene expression. Butyric acid-13C4 sodium can be used in metabolic research and compound development to help scientists gain a deeper understanding of the role of short-chain fatty acids in organisms. Butyric acid-13C4 sodium also plays an important role in nutrition and intestinal health research, especially in the regulation of probiotic function and intestinal microbiota.
Pregnenolone-d4 is the deuterium labeled Pregnenolone. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication[1][2]. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
(S)-2-Aminohexanedioic acid-d4 is the deuterium labeled (S)-2-Aminohexanedioic acid. (S)-2-Aminohexanedioic acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
L-Arginine- 13C6 (hydrochloride) is the 13C-labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
Norverapamil-d7 (hydrochloride) is a deuterium labeled Norverapamil. Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor[1][2].
SAH- 13C5 is the 13C-labeled SAH. SAH (S-Adenosylhomocysteine) is an amino acid derivative and a modulartor in several metabolic pathways. It is an intermediate in the synthesis of cysteine and adenosine[1]. SAH is an inhibitor for METTL3-METTL14 heterodimer complex (METTL3-14) with an IC50 of 0.9 µM[2].
trans-2-Nonenal-d2 is deuterated labeled Acetylpyrazine (HY-W007692). Acetylpyrazine (2-Acetylpyrazine) is used to form many polycyclic compounds, as useful structures in pharmaceuticals and perfumes. Acetylpyrazine is a component of the folates (vitamin B compounds) .
Phosphoenolpyruvic acid (potassium)- 13C2 is the 13C labeled Phosphoenolpyruvic acid potassium (HY-W008807) . Phosphoenolpyruvic acid (Phosphoenolpyruvate) potassium is a glycolysis metabolite with a high-energy phosphate group. Phosphoenolpyruvic acid potassium is involved in glycolysis and gluconeogenesis, and used as energy source to produce ATP, under the energy-limited conditions. Phosphoenolpyruvic acid potassium also exhibits cytoprotective and anti-oxidative properties .
L-Arginine- 15N2 (hydrochloride) is the 15N-labeled L-Arginine (hydrochloride). L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
Pseudane IX-d4 (2-Nonylquinolin-4(1H)-one-d4) is deuterium labeled Pseudane IX. Pseudane IX, a compound isolated from the leaves of Ruta angustifolia, has strong anti-HCV activity with an IC50 value of 1.4 μg/mL. Pseudane IX reduces HCV RNA replication and viral protein synthesis levels .
7α,25-Dihydroxycholesterol-d6 is deuterium labeled 7α,25-Dihydroxycholesterol. 7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly
Risperidone-d4-1 (R 64 766-d4-1) is the deuterium labeled Risperidone (HY-11018). Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
L-Arginine- 15N4 (hydrochloride) is the 15N-labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis[1].
(Rac)-Moxifloxacin-d4 ((Rac)-BAY 12-8039-d4 (free base)) is deuterium labeled (Rac)-Moxifloxacin. (Rac)-Moxifloxacin ((Rac)-BAY 12-8039 free base) is the isoform of Moxifloxacin Hydrochloride (HY-66011), which is an oral 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia .
L-Phenylalanine-d7 is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
Nifedipine-13C8 is a deuterated labeled Nifedipine . Nifedipine (BAY-a-1040) is a potent calcium channel blocker and agent of choice for cardiac insufficiencies.
L-Phenylalanine-d8 is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
1,2-Dioleoyl-sn-glycero-3-phosphocholine-d9 is deuterium labeled 1,2-Dioleoyl-sn-glycero-3-phosphocholine. 1,2-Dioleoyl-sn-glycero-3-phosphocholine (DOPC) is a phospholipid and is commonly used alone, or with other components, in the generation of micelle
Diethylene glycol-d8(2,2'-Oxybis(ethan-1-ol)-d8) is the deuterium labeled Diethylene glycol (HY-B1952). Diethylene glycol has excellent solubility and reactivity in certain chemical reactions and can help accelerate the activation of certain reactants.
Tolfenamic acid- 13C6 is the 13C6 labeled Tolfenamic acid. Tolfenamic Acid (GEA 6414) is a non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1.
Octanoic acid- 13C4 is the 13C labeled Octanoic acid. Octanoic acid (Caprylic acid) is an oily liquid with a slightly unpleasant rancid taste and used commercially in the production of esters used in perfumery and also in the manufacture of dyes.
N-(Phenylacetyl-d5)glycine is the deuterium labeled Phenylacetylglycine. Phenylacetylglycine is a gut microbial metabolite that can activate β2AR. Phenylacetylglycine protects against cardiac injury caused by ischemia/reperfusion[1][2].
rac cis-Moxifloxacin-d4 (hydrochloride) is the deuterium labeled Moxifloxacin hydrochloride. Moxifloxacin Hydrochloride (BAY 12-8039) is an oral 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia[1][2].
DPPC-13C2 is a deuterated labeled DPPC . DPPC (129Y83) is a phosphoglyceride that can be used to prepare lipid monolayers, bilayers, and liposomes. DPPC is the main lipid component of pulmonary surfactant. Dppc-liposome can be effectively used as a delivery vector to induce an immune response against GSL antigen in mice [3] .
Hydrochlorothiazid- 13C,d2 is the 13C- and deuterium labeled Hydrochlorothiazide. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect[1][2][3].
Glycolic acid- 13C2 is the 13C-labeled Glycolic acid (HY-W015967). Glycolic acid- 13C2 is an inhibitor of tyrosinase, suppressing melanin formation and lead to a lightening of skin colour.
Secalciferol-d6 is the deuterium labeled Secalciferol. Secalciferol is a metabolite of Vitamin D, a possibly anti-inflammatory steroid which is involved in bone ossification[1][2].
Triacetonamine-d17 (2,2,6,6-Tetramethyl-4-piperidone-d17) is the deuterium labeled Triacetonamine. Triacetonamine has oral activity and can induce acute liver failure (ALF) in rats [3].
Diphenyl ether- 13C12 is 13C labeled Diphenyl ether. Oxydibenzene is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
Methyl arachidonate- 13C4 (Arachidonic acid methyl ester- 13C4) is 13C labeled Methyl arachidonate. Methyl arachidonate (Arachidonic acid methyl ester) is a fatty acid methyl ester resulting from the formal condensation of the carboxy group of arachidonic acid with methanol. Methyl arachidonate has activity of human blood serum metabolite .
Uridine- 13C5 (β-Uridine- 13C5) is a 13C labeled Uridine (HY-B1449). Uridine (β-Uridine) is a nucleoside compound consisting of uracil and a ribose ring, which are linked by a β-N1- glycosyl bond.
Octachlorodibenzo-p-dioxin- 13C12 is Octachlorodibenzo-p-dioxin- 13 C-labeled octachlorodibenzo-p-dioxin- 13C. Octachlorodibenzo-p-dioxin is a widespread environmental pollutant .
6-Mercaptopurine- 13C2, 15N is the 13C- and 15N-labeled 6-Mercaptopurine. 6-Mercaptopurine is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive agent.
Entecavir- 13C2, 15N (BMS200475- 13C2, 15N; SQ34676- 13C2, 15N) is a 13C- and 15N-labeled Entecavir (HY-13623). Entecavir (SQ 34676; BMS 200475) is a potent and selective inhibitor of HBV, with an EC50 of 3.75 nM in HepG2 cell.
4-(4-Fluorobenzylamino)-1-methylpiperidine-d2(N-[(4-Fluorophenyl)methyl]-1-methyl-4-piperidinamine-d2) is the deuterium labeled 4-(4-Fluorobenzylamino)-1-methylpiperidine.
Mandelic acid-2,3,4,5,6-d5 is the deuterium labeled Mandelic acid. Mandelic acid ((±)-Mandelic acid), an alpha-hydroxycarboxylic acid, has been widely used as an intermediate of pharmaceutical and fine chemicals. Mandelic acid shows antimicrobial activity and has been used for the research of urinary tract infections and vaginal trichomoniasis. Mandelic acid exhibits high sperm-immobilizing activity and low vaginal irritation[1][2].
Hypoxanthine- 13C, 15N2 is a 15N-labeled and 13C-labled Furaltadone. Furaltadone, a nitrofuran agent, has the potential for the study in infections of chickens with salmonella enteritidis. Furaltadone is inhibitory and bactericidal in vitro for staphylococci
Cefdinir- 13C, 15N2 (FK-482- 13C, 15N2) is 13C and 15N labeled Cefdinir. Cefdinir (FK-482) is a semi-synthetic, broad-spectrum antibiotic in the third generation of the cephalosporin class, which is proved to be effective for infections caused by several Gram-negative and Gram-positive bacteria. Cefdinir can be used for the research of common bacterial infections of the ear, sinus, throat, and skin .
Zileuton- 13C2, 15N is 15N and 13C labeled Zileuton (HY-14164). Zileuton is a potent and selective inhibitor of 5-lipoxygenase with antiasthmatic properties.
Vildagliptin- 13C5, 15N (LAF237- 13C5, 15N; NVP-LAF 237- 13C5, 15N) is a 13C- and 15N-labeled Vildagliptin (HY-14291). Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity .
4-Trifluoromethylsalicylic acid- 13C6 is the 13C labeled 4-Trifluoromethylsalicylic acid[1]. 4-Trifluoromethylsalicylic acid is a platelet aggregation inhibitor[2].
4-Methyl-2-oxopentanoic acid-d7 (α-Ketoisocaproic acid-d7) sodium is the deuterium labeled 4-Methyl-2-oxopentanoic acid (HY-W012722).4-Methyl-2-oxopentanoic acid is a metabolite of L-leucine and is involved in energy metabolism. 4-Methyl-2-oxopentanoic acid increases endoplasmic reticulum stress, promotes lipid accumulation in preadipocytes and insulin resistance by impairing mTOR and autophagy signaling pathways .
Oxaloacetic acid- 13C4 is the 13C-labeled Oxaloacetic acid. Oxaloacetic acid (2-Oxosuccinic acid) is a metabolic intermediate involved in several ways, such as citric acid cycle, gluconeogenesis, the urea cycle, the glyoxylate cycle, amino acid synthesis, and fatty acid synthesis[1][2][3].
N-Lactoyl-Phenylalanine- 13C6 (Lac-Phe- 13C6) is 13C labeled N-Lactoyl-Phenylalanine. N-Lactoyl-Phenylalanine is a blood-derived signaling metabolite that can be induced by exercise. N-Lactoyl-Phenylalanine can reduce obesity and improve glucose tolerance .
Isoallolithocholic acid-d4 (3β-Hydroxy-5α-cholanic acid-d4) is deuterium labeled Isoallolithocholic acid. Isoallolithocholic acid (3β-Hydroxy-5α-cholanic acid), a derivative of Lithocholic acid (HY-10219), is a T cell regulator. Isoallolithocholic acid enhances regulatory T cells (Tregs) differentiation .
Tauro-α-muricholic acid-d4-1 (sodium) is deuterium labeled Tauro-α-muricholic acid (sodium). Tauro-α-muricholic acid (T-α-MCA) sodium is a FXR (Farnesoid X receptor) antagonist (IC50=28μM). Tauro-α-muricholic acid sodium is also a endogenous metabolite that can be found in cecal [3].
Zafirlukast- 13C,d6 is the 13C- and deuterium labeled Zafirlukast. Zafirlukast (ICI 204219) is a potent orally active leukotriene D4 (LTD4) receptor antagonist. Zafirlukast shows anti-asthmatic, anti-inflammatory and anti-bacterial effects.
Sucrose- 13C6-1 is 13C labeled Sucrose. Sucrose (D-(+)-Saccharose) is a disaccharide which is composed of two monosaccharides, glucose and fructose. Sucrose?can be applied in some animal models, including metabolic disease, obesity,?diet on preference,?and diabetes, et al .
Adenosine-d-2 is the deuterium labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular phys
Upadacitinib- 15N,d2 (ABT-494- 15N,d2) is the deuterium-labeled Upadacitinib (HY-19569). Upadacitinib- 15N,d2 (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib- 15N,d2 (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib- 15N,d2 (ABT-494) can be used for several autoimmune disorders research .
Emtricitabine- 15N,d2 is a 15N-labeled and deuterium labeled Emtricitabine. Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with an EC50 of 0.01 μM in PBMC cell. It is an antiviral agent for the treatment of HIV infection.
NH2-C2-NH-Boc-d4 is the deuterium labeled NH2-C2-NH-Boc[1]. NH2-C2-NH-Boc (PROTAC Linker 22) is a alkyl chain-based PROTAC linker can be used in the synthesis of PROTACs[2].
Adenosine-d-1 is the deuterium labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular phys
Guanosine triphosphate- 15N5 (GTP- 15N5) dilithium is 15N labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19.
1-Palmitoyl-2-oleoyl-sn-glycero-3-PC-d31 is deuterium labeled 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC (POPC), a phospholipid, is a major component of biological membranes. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC is used for
Levomefolic acid- 13C5 is the 13C labeled Levomefolic acid[1]. Levomefolic acid (L-5-MTHF) is an orally active, brain-penetrant natural active form of folic acid and is one of the most widely used folic acid food supplements[2][3].
Isoallolithocholic acid-d2 is the deuterium labeled Isoallolithocholic acid (HY-B0172A). Isoallolithocholic acid is a T cell regulator and enhances regulatory T cells (Tregs) differentiation[1][2].
Apatinib-d8 (free base) is the deuterium labeled Apatinib free base[1]. Apatinib free base (YN968D1 free base) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 (IC50=1 nM). Apatinib free base (YN968D1 free base) is an anti-angiogenic drug for the research of advanced or metastatic gastric cancer. Apatinib free base (YN968D1 free base) potently inhibits Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. It also inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ[2][3][4].
Saxagliptin-15N,d2 Hydrochloride (BMS-477118-15N,d2 Hydrochloride) is the 15N and deuterium labeled isotope of Saxagliptin (HY-10285). Saxagliptin (BMS-477118) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin has the peotential for type 2 diabetes mellitus research [3].
Guanosine triphosphate- 13C10 (GTP- 13C10) dilithium is 13C-labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate is a native nucleotide. The derivatives of GTP may be used as specific inhibitors against COVID-19.
Cholestenone- 13C2 is the 13C labeled Cholestenone. Cholestenone (4-Cholesten-3-one), the intermediate oxidation product of cholesterol, is metabolized primarily in the liver. Cholestenone is highly mobile in membranes and influences cholesterol flip-flop and efflux. Cholestenone may cause long-term functional defects in cells[1][2][3].
rac-1-Linoleoyl-3-chloropropanediol-d5 is deuterium labeled 1-Linoleoyl-3-chloropropanediolte. 1-Linoleoyl-3-chloropropanediolte (3-Chloro-2-hydroxypropyl (9Z,12Z)-octadeca-9,12-dienoate) is an ester product .
1-Palmitoyl-2-oleoyl-sn-glycero-3-PC-d82 is deuterium labeled 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC (POPC), a phospholipid, is a major component of biological membranes. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC is used for
Thiabendazole- 13C6 is the 13C6 labeled Thiabendazole. Thiabendazole inhibites the mitochondrial helminth-specific enzyme, fumarate reductase, with anthelminthic property.
Riociguat- 13C,d6 is the 13C and deuterium labeled Riociguat (HY-14779). Riociguat is an oral stimulator of soluble guanylate cyclase (sGC) used in the treatment of pulmonary hypertension.
Salicylic acid- 13C6 is the 13C-labeled Salicylic acid (HY-B0167). Salicylic acid is a precursor to and a metabolite of Aspirin (HY-14654), can inhibit cyclo-oxygenase-2 (COX-2) activity .
17β-Estradiol sulfate-d4 (sodium) is the deuterium labeled 17β-Estradiol sulfate 17β-Estradiol sulfate (sodium), also known as β-Estradiol 3-sulfate sodium salt, is a neuroactive steroid[1][2].
2-Nonyl-3-hydroxy-4-quinolone-d4 (C9-PQS-d4) is deuterium labeled 2-Nonyl-3-hydroxy-4-quinolone. 2-nonyl-3-hydroxy-4-Quinolone (C9-PQS) is a quinolone compound produced by P. aeruginosa and other related bacterias. 2-nonyl-3-hydroxy-4-Quinolone is a quorum sensing (QS) signal molecule that controls the expression of many virulence genes as a function of cell population density .
5-Methylcytidine 5'-triphosphate-d8 trisodium is the deuterium-labeled form of 5-Methylcytidine 5'-triphosphate trisodium (HY-147338A). 5-Methylcytidine 5'-triphosphate (5-Methyl-CTP) trisodium is a modified nucleoside triphosphate. 5-Methylcytidine 5'-triphosphate trisodium can be used to replace unmodified mRNA, resulting in the increase of translational properties and stability, as well as the reduction of innate immune responses in human and other mammalian cells .
Lamivudine- 15N,d2 is 15N and deuterated labeled Lamivudine (HY-B0250). Lamivudine (BCH-189) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS .
Methyl arachidonate- 13C5 (Arachidonic acid methyl ester- 13C5) is 13C labeled Methyl arachidonate. Methyl arachidonate (Arachidonic acid methyl ester) is a fatty acid methyl ester resulting from the formal condensation of the carboxy group of arachidonic acid with methanol. Methyl arachidonate has activity of human blood serum metabolite .
Triclocarban- 13C13 (3,4,4'-Trichlorocarbanilide- 13C13) is 13C labeled Triclocarban. Triclocarban (3,4,4′-Trichlorocarbanilide), a broad spectrum antibacterial compound, is widely used in a broad range of applications such as the production of soaps, skin creams, toothpastes and deodorants. Triclocarban is a potential endocrine-disrupting chemical with the capacity to modulate androgen and estrogen activities as well as other hormone-mediated biological processes [3][3] .
Adenosine monophosphate- 13C10 (AMP- 13C10) dilithium is 13C-labeled Adenosine monophosphate (HY-A0181). Adenosine monophosphate is an adenosine A1 receptor agonist. Adenosine monophosphate has significant antiviral activity against HSV-1 and HSV-2. Adenosine monophosphate is a key cellular metabolite regulating energy homeostasis and signal transduction [3].
Sumatriptan-d6 (formate) (GR 43175 free base-d6 (formate)) is deuterium labeled Sumatriptan. Sumatriptan (GR 43175) is an orally active 5-HT1 receptor agonist with IC50s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT1D, 5-HT1B and 5-HT1F receptors, respectively. Sumatriptan can be used for migraine headache research [3] .
Sacubitril- 13C4 (hemicalcium salt) is a 13C-labeled and deuterium labeled Sacubitril hemicalcium salt. Sacubitril (AHU-377) hemicalcium salt is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril hemicalcium salt is a component of the heart failure medicine LCZ696[1].
L-Histidine- 13C6 (hydrochloride hydrate) is the 13C-labeled L-Histidine hydrochloride hydrate. L-Histidine hydrochloride hydrate (H-His-OH.HCl.H2O) is an endogenous metabolite.
Methyl Paraben- 13C6 (Methyl 4-hydroxybenzoate- 13C6) is a 13C labeled Methyl Paraben (HY-N0349) . Methyl Paraben, isolated from the barks of Tsuga dumosa the methyl ester of p-hydroxybenzoic acid, is a standardized chemical allergen. Methyl Paraben is a stable, non-volatile compound used as an antimicrobial preservative in foods, agents and cosmetics. The physiologic effect of Methyl Paraben is by means of increased histamine release, and cell-mediated immunity .
4-Hydroxyestrone- 13C6 is a 13C-labeled Hypoxanthine. Hypoxanthine, a purine derivative, is a potential free radical generator and could be used as an indicator of hypoxia.
Orotic acid- 13C, 15N2 (monohydrate) is the 13C and 15N labeled Orotic acid[1]. Orotic acid (6-Carboxyuracil), a precursor in biosynthesis of pyrimidine nucleotides and RNA, is released from the mitochondrial dihydroorotate dehydrogenase (DHODH) for conversion to UMP by the cytoplasmic UMP synthase enzyme. Orotic acid is a marker for measurement in routine newborn screening for urea cycle disorders. Orotic acid can induce hepatic steatosis and hepatomegaly in rats[2][3][4].
Pregnenolone monosulfate-d4 (sodium) is the deuterium labeled Pregnenolone monosulfate. Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium can protect the brain from cannabis intoxication[1][2]. Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
(2R)-Octyl-α-hydroxyglutarate-d17 ((2R)-Octyl-2-HG-d17) is deuterium labeled (2S)-Octyl-α-hydroxyglutarate. (2S)-Octyl-α-hydroxyglutarate ((2S)-Octyl-2-HG) is a modified form of S-isomer 2-Hydroxyglutarate .
Indole-3-carboxaldehyde- 13C8 (3-Formylindole- 13C8) is the 13C-labeled Indole-3-carboxaldehyde (HY-W007376). Indole-3-carboxaldehyde, a banlangen extract, is the product of the oxidative degradation of indole-3-acetic acid (IAA) by crude enzyme preparations from etiolated pea seedlings. Indole-3-carboxaldehyde is a biochemical used to prepare analogs of the indole phytoalexin cyclobrassinin. Indole-3-carboxaldehyde also enhances the epithelial barrier and anti-inflammatory activity in the intestinal tract .
L-Glutamine- 13C5 is the 13C-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells[1][2].
(Z)-Aconitic acid- 13C6 is the 13C-labeled (Z)-Aconitic acid (HY-W016814). (Z)-Aconitic acid- 13C6 (cis-Aconitic acid) is the cis-isomer of Aconitic acid. (Z)-Aconitic acid- 13C6 (cis-Aconitic acid) is an intermediate in the tricarboxylic acid cycle produced by the dehydration of citric acid.
Calcifediol- 13C5 monohydrate is the 13C-labeled Calcifediol monohydrate. Calcifediol monohydrate (25-hydroxy Vitamin D3 monohydrate), is an effective VDR ligand and VD supplement. Calcifediol is a prohormone of the vitamin D endocrine system (VDES) and is hydroxylated in the liver to produce the active form, calcitriol. Calcifediol can rapidly increase serum VD levels [3].
Deoxythymidine-5'-triphosphate- 15N2 (dTTP- 15N2) dilithium is 15N labeled Deoxythymidine-5'-triphosphate (HY-138615). Deoxythymidine-5'-triphosphate (dTTP) is one of the four nucleoside triphosphates. Deoxythymidine-5'-triphosphate (dTTP) is used in the synthesis of DNA.
ATP- 13C10 (Adenosine 5'-triphosphate- 13C10) dilithium is 13C-labeled ATP (HY-B2176). ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation.
Benzisothiazolinone-13C5 (1,2-Benzothiazol-3-one-13C5) is a 13C-labeled Benzisothiazolinone. Benzisothiazolinone is widely used as an antiseptic and antibacterial agent .
MCPA- 13C8 is the 13C-labeled MCPA. MCPA is a phenoxy herbicide, and widely used to control annual and perennial broad leaved weeds, including poppy, thistles and docks, in crops such as cereals, rice, linseed, flax, grassland and turf[1][2].
Pyruvic acid- 13C,d4 is the deuterium and 13C labeled Pyruvic acid[1]. Pyruvic acid is an intermediate metabolite in the metabolism of carbohydrates, proteins, and fats[2].
Flavin adenine dinucleotide- 13C5 (FAD- 13C5) ammonium is 13C labeled Flavin adenine dinucleotide (HY-B1654). Flavin adenine dinucleotide (FAD) is a redox cofactor, more specifically a prosthetic group of a protein, involved in several important enzymatic reactions in metabolism.
SN-38 glucuronide- 13C6 is the 13C labeled SN-38 glucuronide (HY-126373) . SN-38 glucuronide is an inactive metabolite of the cancer agent Irinotecan. Irinotecan is a topoisomerase I inhibitor which can be used for researching colon and rectal cancer .
Guanosine 5'-diphosphate- 13C10 (GDP- 13C10) dilithium is 13C-labeled Guanosine 5'-diphosphate (HY-113066). Guanosine 5'-diphosphate (GDP) is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K + channel. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Guanosine 5'-diphosphate can be used in the research of inflammation, such as anemia of inflammation (AI).
DL-Lysine- 15N2 hydrochloride ((±)-2,6-Diaminocaproic acid- 15N2 hydrochloride) is 15N labeled DL-Lysine (HY-B2236). DL-Lysine is a racemic mixture of the D-Lysine and L-Lysine. Lysine is an α-amino acid that is used in the biosynthesis of proteins.
Pyridinium bisretinoid A2E-d4 TFA is the deuterium-labeled Pyridinium bisretinoid A2E (HY-134928). Pyridinium bisretinoid A2E (A2E)is an initiator of blue-light-induced apoptosis. Photoactivation of Pyridinium bisretinoid A2E mediates autophagy and the production of reactive oxygen species [3] .
Uridine 5'-monophosphate-15N2 is the 15N labeled Uridine 5'-monophosphate[1]. Uridine 5'-monophosphate (5'- Uridylic acid), a monophosphate form of UTP, can be acquired either from a de novo pathway or degradation products of nucleotides and nucleic acids in vivo and is a major nucleotide analogue in mammalian milk[2].
6-(γ,γ-Dimethylallylamino)purine-d6 is the deuterium labeled 6-(γ,γ-Dimethylallylamino)purine (HY-112103). 6-(γ,γ-Dimethylallylamino)purine is a plant growth substance[1][2].
L-Alanine- 13C2 is the 13C-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
DL-Lysine- 13C6 hydrochloride ((±)-2,6-Diaminocaproic acid- 13C6 hydrochloride) is 13C-labeled DL-Lysine (HY-B2236). DL-Lysine is a racemic mixture of the D-Lysine and L-Lysine. Lysine is an α-amino acid that is used in the biosynthesis of proteins.
L-Glutamine- 15N2 is the 15N-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells .
Salmeterol- 13C6 (xinafoate) is the 13C6 labeled Salmeterol (xinafoate). Salmeterol (GR 33343X) xinafoate is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively.
Pregnenolone-d4-1 is the deuterium labeled Pregnenolone. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication[1][2]. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
ATP- 15N5 (Adenosine 5'-triphosphate- 15N5) dilithium is 15N labeled ATP (HY-B2176). ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation.
Tempol-d17, 15N is the deuterium labeled Tempol[1]. Tempol is a general superoxide dismutase (SOD)-mimetic agent that efficiently neutralizes reactive oxygen species (ROS)[2][3].
Deoxythymidine-5'-triphosphate- 13C10 (dTTP- 13C10) dilithium is 13C-labeled Deoxythymidine-5'-triphosphate (HY-138615). Deoxythymidine-5'-triphosphate (dTTP) is one of the four nucleoside triphosphates. Deoxythymidine-5'-triphosphate (dTTP) is used in the synthesis of DNA.
2′,2′-Difluorodeoxyuridine- 13C, 15N2 (dFdU- 13C, 15N2; 2',2'-Difluoro-2'-deoxyuridine- 13C, 15N2) is a 13C- and 15N-labeled compound. 2’,2’-Difluorodeoxyuridine (dFdU; 2',2'-Difluoro-2'-deoxyuridine) is the main metabolite of Gemcitabine (HY-17026). 2’,2’-Difluorodeoxyuridine causes a concentration- and schedule- dependent radiosensitising effect in vitro. 2’,2’-Difluorodeoxyuridine arrests cell cycle at the early S phase and induces apoptosis in cancer cells [3] .
(Rac)-Folic acid- 13C5, 15N is the 13C-labeled and 15N-labeled Folic acid. Folic acid (Vitamin M; Vitamin B9) is a B vitamin; is necessary for the production and maintenance of new cells, for DNA synthesis and RNA synthesis.
Lysophosphatidylcholine 18:2-d9 is deuterium labeled Lysophosphatidylcholine 18:2. Lysophosphatidylcholine 18:2 (1-Linoleoyl-2-Hydroxy-sn-glycero-3-PC), a lysophospholipid, is a potential biomarker identified from insulin resistance (IR) polycystic ovary
(1S,2R)-Tranylcypromine-d5 (hydrochloride) is the deuterium labeled Tranylcypromine hydrochloride[1]. Tranylcypromine hydrochloride (SKF 385 hydrochloride) is an irreversible inhibitor of lysine-specific demethylase 1 (LSD1/BHC110) and monoamine oxidase (MAO). Tranylcypromine hydrochloride inhibits LSD1, MAO A and MAO B with IC50s of 20.7, 2.3 and 0.95 μM, respectively. Tranylcypromine hydrochloride can be used for the research of depression[2][3][4].
11-Beta-hydroxyandrostenedione-d7 is the deuterium labeled 11-Beta-hydroxyandrostenedione. 11-Beta-hydroxyandrostenedione (4-Androsten-11β-ol-3,17-dione) is a steroid mainly found in the the adrenal origin (11β-hydroxylase is present in adrenal tissue, but absent in ovarian tissue). 11-Beta-hydroxyandrostenedione is a 11β-hydroxysteroid dehydrogenase (11βHSD) isozymes inhibitor [1][2]
Histamine-α,α,β,β-d4 (dihydrochloride) is the deuterium labeled Histamine. Histamine is an organic nitrogenous compound involved in local immune responses as well as regulating physiological function in the gut and acting as a neurotransmitter.
2'-Deoxyadenosine-5'-triphosphate- 13C10 (dATP- 13C10) dilithium is 13C-labeled 2'-Deoxyadenosine-5'-triphosphate (HY-136648). 2'-Deoxyadenosine-5'-triphosphate (dATP) is a nucleotide used in cells for DNA synthesis (or replication), as a substrate of DNA polymerase.
DMT-dA(bz) Phosphoramidite- 15N5 is the 15N labeled DMT-dA(bz) Phosphoramidite[1]. DMT-dA(bz) Phosphoramidite is typically used in the synthesis of DNA[2].
(Rac)-Nebivolol-d2, 15N is 15N and deuterated labeled (Rac)-Nebivolol (HY-B0203B). (Rac)-Nebivolol ((Rac)-R 065824) is a racemic isomer of Nebivolol. Nebivolol is a selective β1-adrenergic receptor antagonist with an IC50 value of 0.8 nM. Nebivolol can prevent up-regulation of Nox2/NADPH oxidase and lipoperoxidation in the early stages of ethanol-induced cardiac toxicity. Vasodilatory activity .
Vigabatrin- 13C,d2 (hydrochloride) is the 13C- and deuterium labeled Vigabatrin (hydrochloride). Vigabatrin hydrochloride (γ-Vinyl-GABA hydrochloride), a inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin hydrochloride is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase[1][2][3].
γ-Aminobutyric acid-4,4-d2 is the deuterium labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
9(S)-HODE- 13C18 ((+)-α-Dimophecolic acid- 13C18) is 13C labeled 9S-HODE. 9S-HODE (Alpha-dimorphecolic acid) is an octadecadienoic acid and the main active derivative of linoleic acid, which can reduce the viability of HL-60 cells and induce apoptosis. 9S-HODE is rich in lipid peroxidation (LPO) products and is almost an ideal marker for LPO .
3-Hydroxybutyric acid- 13C4 (sodium) is the 13C labeled 3-Hydroxybutyric acid sodium (HY-W010452). 3-Hydroxybutyric acid sodium is a metabolite that is elevated in type I diabetes, and can modulate the properties of membrane lipids[1].
3-Hydroxybutyric acid- 13C2 (sodium) is the 13C labeled 3-Hydroxybutyric acid sodium (HY-W010452). 3-Hydroxybutyric acid sodium is a metabolite that is elevated in type I diabetes, and can modulate the properties of membrane lipids[1].
2,4-D- 13C6 is the 13C-labeled 2,4-D. 2,4-D (2,4-Dichlorophenoxyacetic acid) is a selective systemic herbicide for the control of broad-leaved weeds. 2,4-D acts as a plant hormone, causing uncontrolled growth in the meristematic tissues. 2,4-D inhibits DNA and protein synthesis and thereby prevents normal plant growth and development[1].
γ-Aminobutyric acid- 13C4 is the 13C-labeled γ-Aminobutyric acid. γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
Acetyl coenzyme A- 13C2 lithium is the 13C-labeled Acetyl coenzyme A (HY-114293). Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
Ethyl maltol-d5 is the deuterium labeled Ethyl maltol. Ethyl maltol (2-Ethyl-3-hydroxy-4H-pyran-4-one) is an orally active and important food additive and flavor enhancer. Ethyl maltol is less toxic to rats and dogs. Ethyl maltol can enhance copper-mediated cytotoxicity and induce apoptosis in lung epithelial cells [3].
2-Ketoglutaric acid-13C2 is a deuterated labeled 2-Ketoglutaric acid . 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM) .
dGTP- 13C10 (2'-Deoxyguanosine-5'-triphosphate- 13C10) dilithium is 13C-labeled dGTP (HY-138616). dGTP (2'-Deoxyguanosine-5'-triphosphate), a guanosine nucleotide, can be used in deoxyribonucleic acid synthesis. Guanosine nucleotides (GDP, GTP, dGDP, and dGTP) are highly susceptible to oxidative damage to 8-oxo-GDP (8-O-GDP), 8-O-dGTP, 8-O-GTP, and 8-O-dGTP.
2'-Deoxyadenosine-5'-triphosphate- 15N5 (dATP- 15N5) dilithium is 15N labeled 2'-Deoxyadenosine-5'-triphosphate (HY-136648). 2'-Deoxyadenosine-5'-triphosphate (dATP) is a nucleotide used in cells for DNA synthesis (or replication), as a substrate of DNA polymerase.
Prostaglandin E2-1-glyceryl ester-d5 (PGE2-1-glyceyl ester-d5) is deuterium labeled Prostaglandin E2-1-glyceryl ester. Prostaglandin E2-1-glyceryl ester, a Prostaglandin Glycerol Ester, is an endocannabinoid ligand for the CB1 receptor. Prostaglandin E2-1-glyceryl ester induces rapid, transient elevation of intracellular free Ca 2+ .
L-Hydroxyproline-d4 is deuterium labeled L-Hydroxyproline. L-Hydroxyproline, one of the hydroxyproline (Hyp) isomers, is a useful chiral building block in the production of many pharmaceuticals .
1,2-Dioctanoyl-3-chloropropanediol-d5 is deuterium labeled 1,2-Dioctanoyl-3-chloropropanediol. 1,2-Dioctanoyl-3-chloropropanediol (3-Chloropropane-1,2-diyl dioctanoate) is an ester product .
11-Beta-hydroxyandrostenedione-d4 is the deuterium labeled 11-Beta-hydroxyandrostenedione. 11-Beta-hydroxyandrostenedione (4-Androsten-11β-ol-3,17-dione) is a steroid mainly found in the the adrenal origin (11β-hydroxylase is present in adrenal tissue, but absent in ovarian tissue). 11-Beta-hydroxyandrostenedione is a 11β-hydroxysteroid dehydrogenase (11βHSD) isozymes inhibitor[1][2].
VD3-d6 (Vitamin D3-26,26,26,27,27,27-d6) is deuterated VD3. Compounds labeled with stable or radioactive isotopes can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified .
L-Glutathione reduced- 13C2, 15N is the 13C- and 15N-labeled L-Glutathione reduced. L-Glutathione reduced (GSH) is an endogenous antioxidant and is capable of scavenging oxygen-derived free radicals.
1-Stearoyl-2-15(S)-HETE-sn-glycero-3-PE-d11 (15(S)-HETE-SAPE-d11) is deuterium labeled 1-Stearoyl-2-15(S)-HETE-sn-glycero-3-PE. 1-Stearoyl-2-15(S)-HETE-sn-glycero-3-PE is a phospholipid that contains stearic acid (HY-B2219) at the sn-1 position and 15(S)-HETE at the sn-2 position. It is formed in human peripheral monocytes activated by the calcium ionophore A23187 (HY-N6687) by direct oxidation of 1-stearoyl-2-arachidonoyl-sn-glycero-3-PE (SAPE) by 15-LO. Phosphoethanolamine (PE) HETEs (PE-HETEs), including 1-stearoyl-2-15(S)-HETE-sn-glycero-3-PE, are the main source of esterified HETE in ionophore-activated monocytes .
Uridine 5'-monophosphate- 13C9 (5'- Uridylic acid- 13C9) dilithium is 13C-labeled Uridine 5'-monophosphate (HY-101981). Uridine 5'-monophosphate (5'- Uridylic acid), a monophosphate form of UTP, can be acquired either from a de novo pathway or degradation products of nucleotides and nucleic acids in vivo and is a major nucleotide analogue in mammalian milk.
L-Valine-d8 is a deuterated form of L-Valine. L-Valine-d8 can be used in the labelled synthesis of L-valineamide-d8 intermediate[1]. L-Valine is one of 20 proteinogenic amino acids. L-Valine is an essential amino acid[2].
Cefazolin- 13C2, 15N (Cephazolin- 13C2, 15N) is 13C and 15N labeled Cefazolin. Cefazolin (Cephazolin) is a first-generation cephalosporin antibiotic and can be used in varieties of bacterial infections research . Cefazolin has anti-inflammatory effect and can attenuate post-operative cognitive dysfunction (POCD) .
Emtricitabine- 13C, 15N2 (BW1592- 13C, 15N2) is a 13C- and 15N-labeled Emtricitabine (HY-17427). Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with an EC50 of 0.01 μM in PBMC cell. It is an antiviral agent for the treatment of HIV infection.
Uridine 5'-monophosphate- 15N2 (5'-?Uridylic acid- 15N2) dilithium is 15N labeled Uridine 5'-monophosphate (HY-101981). Uridine 5'-monophosphate (5'-?Uridylic acid), a monophosphate form of UTP, can be acquired either from a de novo pathway or degradation products of nucleotides and nucleic acids in vivo and is a major nucleotide analogue in mammalian milk.
rU Phosphoramidite- 13C9 (DMT-2'O-TBDMS-rU phosphoramidite- 13C9) is 13C-labeled rU Phosphoramidite (HY-W048482). rU Phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
Nitrofurazone- 13C, 15N2 (Nitrofural- 13C, 15N2) is the 13C and 15N labled Nitrofurazone (HY-B0226) . Nitrofurazone is a potential antibiotic that can be used topically to treat wounds, burns, ulcers and skin infections to combat various microorganisms and to prepare surfactants . Nitrofurazone may affect the ecosystem function in Marine environment and affect the functional processes of epiphytic fauna [3].
L-Arginine-1,2- 13C2 (hydrochloride) is the 13C-labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
[1,1'-Biphenyl]-3-amine-13C6 hydrochloride (Biphenyl-3-amine-13C6 hydrochloride) is the 13C labeled isotope of [1,1'-Biphenyl]-3-amine hydrochloride (HY-W106014) .
Uridine 5′-diphosphoglucose- 13C6 (disodium) is the 13C labeled Uridine 5′-diphosphoglucose disodium salt[1]. Uridine 5′-diphosphoglucose disodium salt (UDP-D-Glucose disodium salt) is the precursor of glucose-containing oligosaccharides, polysaccharides, glycoproteins, and glycolipids in animal tissues and in some microorganisms. Uridine-5′-diphosphoglucose is an agonist of the P2Y14 receptor, a neuroimmune system GPCR[2].
L-Alanine- 13C,d is the 13C- and deuterium labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
L-Phenylalanine- 13C6 is the 13C-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
L-Phenylalanine- 13C9 is the 13C-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
L-Alanine- 15N,d4 is the deuterium and 15N-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
rU Phosphoramidite- 15N2 (DMT-2'O-TBDMS-rU phosphoramidite- 15N2) is 15N labeled rU Phosphoramidite (HY-W048482). rU Phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
trans-2,cis-6-Nonadienal- 13C2 is 13C labeled 4-Ethylphenol (HY-W012836). 4-Ethylphenol is a volatile phenolic compound associated with off-odour in wine.
Riluzole- 13C, 15N2 is the 13C and 15N labeled Riluzole[1]. Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM[2][3].
(E)-3-Methyl-2-hexenoic acid-d5 ((2E)-3-Methyl-2-hexenoic acid-d5) is a deuterium labeled (E)-3-Methyl-2-hexenoic acid. (E)-3-Methyl-2-hexenoic acid is an axillary odor-related compound .
2-Thiouracil- 13C, 15N2 is the 13C, 15N labeled 2-Thiouracil. 2-Thiouracil (Thiouracil) is an antithyroid compound. 2-Thiouracil can function as a highly specific melanoma seeker. 2-Thiouracil is a selective inhibitor of neuronal nitric oxide synthase (nNOS) with a Ki of 20 μM.
Lenalidomide- 13C5, 15N is 15N and 13C labeled Lenalidomide (HY-A0003). Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
Ethyl linoleate-d5 (Linoleic Acid ethyl ester-d5) is deuterium labeled Ethyl linoleate. Ethyl linoleate (Linoleic Acid ethyl ester) inhibit the development of atherosclerotic lesions and the expression of inflammatory mediators . .
Fluconazole-13C2,15N (UK-49858-13C2,15N) is the 13C and 15N labeled isotope of Fluconazole (HY-B0101). Fluconazole (UK-49858) is a triazole antifungal agent with excellent activities against a broad range of fungi, especially against Candida albicans. Fluconazole inhibits C. albicans and Candida kefyr with IC99s range from 0.20 μg/mL to 0.39 μg/mL .
Gemcitabine- 13C, 15N2 (hydrochloride) is the 13C and 15N labeled Gemcitabine hydrochloride[1]. Gemcitabine Hydrochloride (LY 188011 Hydrochloride) is a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent. Gemcitabine Hydrochloride inhibits DNA synthesis and repair, resulting in autophagyand apoptosis[2][3].
Tranexamic acid- 13C2, 15N (Cyclocapron- 13C2, 15N) is the 13C2 and 15N labeled Tranexamic acid. Tranexamic acid is an antifibrinolytic agent that alleviates liver damage and fibrosis in mouse models of chronic bile duct injury .
(3S,5R)-Fluvastatin-d6 is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway[1].
Allolithocholic Acid-d4 (3α-hydoxy-5α-Cholaoic Acid-d4, allo-LCA-d4) is deuterium labeled Allolithocholic acid. Allolithocholic acid is a steroid acid could found in normal serum and feces. Allolithocholic acid facilitates excretion, absorption, and transport of fats and sterols in the intestine and liver .
Pomalidomide- 15N, 13C5 is 15N and 13C labeled Pomalidomide (HY-10984). Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.
(9S,13R)-12-OPDA-d5 is an isotopic label of (9S,13R)-12-oxyphytodienoic acid. (9S,13R)-12-Oxophytodienoic acid is an isomer of 12-oxoPDA (HY-118828). (9S,13R)-12-Oxo phytodienoic Acid is a lipoxygenase metabolite in green plant leaves .
Nonanoic acid-d2 is the deuterium labeled Nonanoic acid[1]. Nonanoic acid is a naturally-occurring saturated fatty acid with nine carbon atoms. Nonanoic acid significantly reduces bacterial translocation, enhances antibacterial activity, and remarkably increases the secretion of porcine β-defensins 1 (pBD-1) and pBD-2[2].
L-Glutamine-1,2- 13C2 is the 13C-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells .
Diethyl succinate- 13C4 is the 13C labeled Diethyl succinate[1]. Diethyl succinate (Diethyl Butanedioate) is used at physiological pH and crosses biological membranes, incorporates into cells in tissue culture and is metabolized by the TCA cycle. Diethyl succinate is known to be non-toxic and used in fragrances and flavoring[2].
L-Ascorbic acid- 13C6-1 (L-Ascorbate-1; Vitamin C- 13C6-1) is a 13C labeled L-Ascorbic acid (HY-B0166) . L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor [3] . L-Ascorbic acid exhibits anti-cancer effects through the generation of reactive oxygen species (ROS) and selective damage to cancer cells .
5-Fluorouracil- 13C, 15N2 is the 13C and 15N labeled 5-Fluorouracil[1]. 5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer[2][3]. 5-Fluorouracil also inhibits HIV[4].
L-Phenylalanine- 15N,d8 is the deuterium and 15N-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca2+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
Taurine- 13C2, 15N is the 13C- and 15N- labeled Taurine. Taurine, a sulphur-containing amino acid and an organic osmolyte involved in cell volume regulation, provides a substrate for the formation of bile salts, and plays a role in the modulation of intracellular free calcium concentration. Taurine has the ability to activate autophagy in adipocytes[1][2][3].
Oxypurinol- 13C, 15N2-1 (Oxipurinol- 13C, 15N2-1) is 15N and 13C labeled Oxypurinol (HY-19657). Oxipurinol, the major active metabolite of Allopurinoll (HY-B0219), is an inhibitor of xanthine oxidase. Oxipurinol can be used to regulate blood urate levels and treat gout .
PSI-6206-d1, 13C, 15N2 is 15N and 13C labeled PSI-6206 (HY-15236). PSI-6206 (RO 2433) is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase. PSI-6206 low potently inhibits HCV replicon with EC90 of >100 μM.
Dienogest-13C,15N,d4 (STS 557-13C,15N,d4) is the 13C, 15N and deuterium labeled isotope of Dienogest (HY-B0084). Dienogest (STS-557) is an orally active and selective progesterone receptor agonist that effectively reduces the gene expression of COX-2, mPGES-1 and aromatase. Dienogest also inhibits the mRNA and protein expression of PGE2 synthase and the activation of NF-κB. Dienogest can be used in studies of endometriosis, menopause and menorrhagia .
Benzyl alcohol-α- 13C-α,α-d2 is the 13C-labeled Benzyl alcohol. Benzyl alcohol is an aromatic alcohol; a colorless liquid with a mild pleasant aromatic odor.
L-Alanine- 13C2, 15N is the 13C- and 15N-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
N-Acetyl-D-glucosamine- 13C6 (N-Acetyl-2-amino-2-deoxy-D-glucose- 13C6) is the 13C labled N-Acetyl-D-glucosamine (HY-A0132) . N-Acetyl-D-Glucosamine (N-Acetyl-2-amino-2-deoxy-D-glucose) is a monosaccharide derivative of glucose.
Dinoprost- 13C5 is 13C labeled Dinoprost (HY-12956). Dinoprost (Prostaglandin F2α) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost plays a key role in the onset and progression of labour .
γ-Glu-(Phe- 13C9, 15N) is the 13C and 15N labeled isotope of γ-Glu-Phe(HY-101399).γ-Glu-Phe or the postenzymatic reaction mixture enhanced the umami intensity of commercial soy sauce and model chicken soup.
13,14-Dihydro-15-keto Prostaglandin F2α-d4 (13,14-Dihydro-15-keto-PGF2α-d4) is a deuterated labeled 13,14-Dihydro-15-keto Prostaglandin F2α (HY-113208). 13,14-Dihydro-15-keto Prostaglandin F2α-d4 is an endogenous metabolite present in Blood that can be used for the research of Pregnancy .
Cyclic GMP- 13C, 15N2 is 13C and 15N labeled Cyclic GMP. Cyclic GMP (cGAMP) is an endogenous second messenger that triggers interferon production in response to cytoplasmic DNA. Cyclic GMP activates the stimulator of interferon genes (STING), activating a signaling cascade that leads to the production of type I interferons and other immune mediators [3].
L-Phenylalanine- 13C9, 15N is the 13C- and 15N-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
8-Hydroxy-2'-deoxyguanosine- 13C, 15N2 is 13C and 15N labeled 8-Hydroxy-2'-deoxyguanosine. 8-Hydroxy-2'-deoxyguanosine is a critical biomarker of oxidative stress and carcinogenesis .
Ile-(Leu-13C6,15N)-OH (TFA) is 13C- and 15N-labeled L-Isoleucyl-L-leucine (HY-W269700). L-Isoleucyl-L-leucine has a role as a metabolite and can be used to inhibit movement-induced muscle damage and muscle defective condition.
(Leu-13C6,15N)-Ile-OH (L-Leucyl-13C6,15N-L-isoleucine) TFA is the deuterium labeled Leu-Ile-OH. Leu-Ile-OH protects against neuronal death by inducing brain-derived neurotrophic factor (BDNF) and glial cell line-derived neurotrophic factor (GDNF) synthesis .
Eicosapentaenoic acid 1,2,3,4,5- 13C5 (EPA 1,2,3,4,5- 13C, FA 20:5- 13C5) is 13C labeled Eicosapentaenoic Acid. Eicosapentaenoic Acid (EPA) is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid can promote relaxation of vascular smooth muscle cells and vasodilation [3] .
Citrinin- 13C13 (NSC 186- 13C13) is the 13C labeled Citrinin (HY-N6746). Citrinin (NSC 186) is a mycotoxin that causes food contamination and has different toxic effects. Citrinin is an effective oral anticancer agent. Citrinin has various regulatory effects on mouse immune system, including regulating the number of immune cells, inducing apoptosis and autophagy of immune cells, altering toll-like receptor expression and cytokine production. Citrinin can induce oxidative stress and lead to early apoptosis of oocytes. Low doses of Citrinin have neuroprotective effects against glutamate-induced excitotoxicity in rat cortical neurons. In addition, Citrinin also has antibacterial activity [3] .
N-Acetyl-D-glucosamine- 13C8, 15N is 13C and 15N labeled N-Acetyl-D-glucosamine (HY-A0132). N-Acetyl-D-glucosamine is a monosaccharide derivative of glucose.
N-Acetyl-D-glucosamine- 13C2, 15N is the 13C and 15N labeled N-Acetyl-D-glucosamine. N-Acetyl-D-Glucosamine (N-Acetyl-2-amino-2-deoxy-D-glucose) is a monosaccharide derivative of gluc[1][2].
Tenuazonic acid-(acetyl- 13C2) (mixture of diastereomers) in methanol (3-(Acetyl- 13C2)-5-((S)-sec-butyl)-4-hydroxy-1,5-dihydro-2H-pyrrol-2-one) is 13C labeled Tenuazonic acid-(acetyl) (mixture of diastereomers) in methanol .
(1S,3aR,6aS)-(2S)-2-Cyclohexyl-N-(2-pyrazinylcarbonyl)glycyl-3-methyl-L-valyl-N-[(1R)-1-[2-(cyclopropylamino)-2-oxoacetyl]butyl]octahydrocyclopenta[c]pyrrole-1-carboxamide-d4 is deuterated labeled (1S,3aR,6aS)-(2S)-2-Cyclohexyl-N-(2-pyrazinylcarbonyl)glycyl-3-methyl-L-valyl-N-[(1R)-1-[2-(cyclopropylamino)-2-oxoacetyl]butyl]octahydrocyclopenta[c]pyrrole-1-carboxamide.
ABCB5 P-gp; ATP binding cassette sub family B (MDR/TAP) member 5; P glycoprotein ABCB5
WB, ICC/IF
Human
ABCB5 Antibody (YA836) is a non-conjugated and Mouse origined monoclonal antibody about 139 kDa, targeting to ABCB5 (8D2). It can be used for WB,ICC/IF assays with tag free, in the background of Human.
p-pg; PGP; ABCB1; MDR1; PGY1; Multidrug resistance protein 1; ATP-binding cassette sub-family B member 1; P-glycoprotein 1; CD antigen CD243
WB
Human
P Glycoprotein Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 141 kDa, targeting to P Glycoprotein. It can be used for WB assays with tag free, in the background of Human.
ABC30 antibody;
abcC2 antibody;
ATP binding cassette sub family C (CFTR/MRP) member 2 antibody;
ATP binding cassette subfamily C member 2 antibody;
ATP-binding cassette sub-family C member 2 antibody;
Canalicular multidrug resistance protein antibody;
Canalicular multispecific organic anion transporter 1 antibody;
CMOAT antibody;
CMOAT1 antibody;
cMRP antibody;
DJS antibody;
KIAA1010 antibody;
MRP 2 antibody;
MRP2_HUMAN antibody;
Multidrug resistance associated protein 2 antibody;
Multidrug resistance-associated protein 2 antibody;
WB, ICC/IF, FC
Human
MRP2/ABCC2 Antibody is an unconjugated, approximately 174 kDa, rabbit-derived, anti-MRP2/ABCC2 monoclonal antibody. MRP2/ABCC2 Antibody can be used for: WB, ICC/IF, FC expriments in human background without labeling.
Rasagiline- 13C3 (mesylate racemic) is a 13C-labeled Rasagiline mesylate racemic. Rasagiline mesylate racemic is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor[1]. Rasagiline-13C3 (mesylate racemic) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Erlotinib-d6 (hydrochloride) a deuterium labeled Erlotinib Hydrochloride. Erlotinib Hydrochloride inhibits purified EGFR kinase with an IC50 of 2 nM[1]. Erlotinib-d6 (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Ethynyl Estradiol-d4 is the deuterium labeled Ethynyl Estradiol. Ethynyl Estradiol (17α-Ethynylestradiol;Ethynylestradiol) is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills. Ethynyl Estradiol-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Norgestimate metabolite norelgestromin-d6 is the deuterium labeled Norgestimate metabolite norelgestromin. Norelgestromin is a metabolite of Norgestimate, which is a progestin or synthetic progestogen. Norgestimate metabolite norelgestromin-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Zidovudine-d3 is the deuterium labeled Zidovudine. Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection.
Zidovudine- 13C,d3 is the 13C- and deuterium labeled Zidovudine. Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI), widely used to treat HIV infection.
Erlotinib-d6 (CP-358774 D6) is a deuterium labeled Erlotinib (CP-358774). Erlotinib is a directly acting inhibitor EGFR tyrosine kinase inhibitor with an IC50 of 2 nM for human EGFR[1]. Erlotinib-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Gestodene-d6is the deuterium labeled Gestodene. Gestodene(SHB 331) is a progestogen hormonal contraceptive[1][2]. Gestodene-d6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Erlotinib- 13C6 (hydrochloride) is the 13C labeled Erlotinib Hydrochloride[1]. Erlotinib Hydrochloride (CP-358774 Hydrochloride) inhibits purified EGFR kinase with an IC50 of 2 nM[2]. Erlotinib-13C6 (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Levonorgestrel-d8 is the deuterium labeled Levonorgestrel. Levonorgestrel is a synthetic progestogen used as an active ingredient in some hormonal contraceptives[1][2]. Levonorgestrel-d8 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Ethynyl Estradiol- 13C2 is the 13C-labeled Ethynyl Estradiol. Ethynyl Estradiol-13C2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
N-Desmethyl Selegiline-dd5 hydrochloride is the deuterium labeled N-Desmethyl Selegiline hydrochloride[1]. N-Desmethyl Selegiline-d5 hydrochloride is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Norethindrone acetate-d8 is the deuterium labeled Norethindrone acetate. Norethindrone acetate is a female hormone used for the research of endometriosis[1]. Norethindrone acetate-d8 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
MK-6186 is a novel non-nucleoside reverse transcriptase inhibitor with sub-nanomolar activity against wild-type viruses and the two most common NNRTI-resistant RT mutants (K103N and Y181C). MK-6186 exhibits excellent antiviral activity against K103N and Y181C mutant viruses. When MK-6186 targets 12 common NNRTI-associated mutant viruses, only two relatively rare mutants (Y188L and V106I/Y188L) show high resistance, with FC values exceeding 100, while the FC values of the remaining viruses are all below 10. In addition, when MK-6186 faces 96 clinical virus isolates carrying NNRTI-resistant mutations, most (70%) viruses show more than 10-fold resistance to efavirenz (EFV), while only 29% of mutant viruses show more than 10-fold resistance to MK-6186 .
SUB1 Human Pre-designed siRNA Set A contains three designed siRNAs for SUB1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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