Search Result
Results for "
major metabolite
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
49
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-136611
-
|
Drug Metabolite
|
Infection
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ω-Hydroxy-DEET is a major metabolite of insect repellent N-N-diethyl-meta-toluamide (DEET). ω-Hydroxy-DEET has anti-proliferative effects. DEET is a spatial repellent and an irritant that commonly used to prevent contact with mosquitoes .
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-
-
- HY-G0001A
-
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Drug Metabolite
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Neurological Disease
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Lurasidone Metabolite 14283 hydrochloride is a major active metabolite of Lurasidone. Lurasidone is a FDA approved agent for the treatment of schizophrenia.
|
-
-
- HY-101723
-
-
-
- HY-111741
-
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Fungal
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Infection
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M700F048 is a major plant metabolite of fungicide Fluxapyroxad .
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-
-
- HY-136347
-
-
-
- HY-116026
-
-
-
- HY-136347R
-
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HMG-CoA Reductase (HMGCR)
Drug Metabolite
|
Cardiovascular Disease
|
3α-Hydroxy pravastatin (sodium) (Standard) is the analytical standard of 3α-Hydroxy pravastatin (sodium). This product is intended for research and analytical applications. 3α-Hydroxy pravastatin sodium is the major metabolite of Pravastatin. Pravastatin is a competitive HMG-CoA reductase inhibitor .
|
-
-
- HY-116026R
-
|
Drug Metabolite
Cholinesterase (ChE)
|
Neurological Disease
|
3-Hydroxycarbofuran (Standard) is the analytical standard of 3-Hydroxycarbofuran. This product is intended for research and analytical applications. 3-Hydroxycarbofuran, a major metabolite of Carbofuran, is a reversible acetylcholinesterase (AChE) inhibitor .
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-
-
- HY-W777199
-
|
Drug Metabolite
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Others
|
Tianeptine metabolite MC5 sodium salt is a major active metabolite of tianeptine. Tianeptine and MC5 metabolite are eliminated with bile as glucuronide and glutamine conjugates .
|
-
-
- HY-W739812
-
Finasteride carboxylic acid
|
Others
|
Cancer
|
Carboxy finasteride is a metabolite of the 5α-reductase inhibitor Finasteride (HY-13635). Finasteride is biotransformed by cytochrome P450 (CYP3A4) and is successively oxidized to Hydroxy finasteride and Carboxy finasteride. Carboxy finasteride is the major metabolite in urine, while Hydroxy finasteride is the major metabolite in plasma .
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-
-
- HY-126857
-
Hydroxyomeprazole
|
Drug Metabolite
|
Others
|
5-Hydroxyomeprazole is the major metabolite of Omeprazole (HY-B0113).
|
-
-
- HY-I0177
-
|
Drug Metabolite
|
Others
|
Vilazodone carboxylic acid is a vilazodone metabolite observed in both urine (major) and plasma (minor) .
|
-
-
- HY-100050
-
-
-
- HY-43711
-
|
mAChR
|
Neurological Disease
|
Nor-benzetimide is a major metabolite of Benzetimide. Benzetimide is a mAChR antagonist with anticholinergic activity .
|
-
-
- HY-137532
-
-
-
- HY-W004464
-
-
-
- HY-W264038
-
-
-
- HY-124320
-
-
-
- HY-126995
-
|
Endogenous Metabolite
|
Metabolic Disease
|
Glycohyodeoxycholic acid is a major metabolite of Hyodeoxycholic acid in humans. Glycohyodeoxycholic acid has preventative effects on gallstone formation .
|
-
-
- HY-118093
-
|
Others
|
Others
|
N-benzoyl-L-aspartic acid, a major metabolite of benzyl glucosinolate, can be used for modification of peptides or proteins .
|
-
-
- HY-100046
-
Desmethyldoxepin hydrochloride
|
Drug Metabolite
|
Neurological Disease
|
Nordoxepin hydrochloride is the major metabolite of Doxepin. Doxepin is a tricyclic antidepressant that is widely prescribed for the research of mild depression .
|
-
-
- HY-P1488
-
-
-
- HY-N3059
-
-
-
- HY-W739861
-
1'-Hydroxytriazolam
|
Endogenous Metabolite
|
Others
|
α-Hydroxytriazolam (1'-Hydroxytriazolam) is a major metabolite of ranitidine (HY-B0693) .
|
-
-
- HY-138573
-
-
-
- HY-100662
-
Bisdesethylchloroquine
|
Drug Metabolite
|
Cardiovascular Disease
|
Didesethyl chloroquine (Bisdesethylchloroquine) is a major metabolite of the antimalarial agent Chloroquine. Didesethyl chloroquine is a potent myocardial depressant .
|
-
-
- HY-N7143
-
-
-
- HY-126708
-
|
ADC Cytotoxin
Antibiotic
|
Infection
|
Luisol A, an aromatic tetraol, is a major metabolite of an estuarine marine actinomycete of the genus Streptomyces. Luisol A, is an anthraquinone antibiotic analog .
|
-
-
- HY-P2643
-
-
-
- HY-117703
-
-
-
- HY-103005
-
-
-
- HY-129903
-
|
Others
|
Others
|
N-Desethyl vardenafil is the major metabolite of Vardenafil (HY-B0442) and can be detected in human urine .
|
-
-
- HY-148846
-
|
Drug Metabolite
|
Metabolic Disease
|
Mosapride N-Oxide is a major active metabolite of Mosapride. Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
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-
-
- HY-107850
-
NSC 1612; NSC 47462
|
Endogenous Metabolite
|
Metabolic Disease
|
Pregnanediol is the major metabolite of progesterone and can be excreted via urine. Pregnanediol offers an indirect way to measure progesterone levels in vivo .
|
-
-
- HY-125643
-
|
Drug Metabolite
|
Cardiovascular Disease
|
Pitavastatin lactone is a major metabolite of Pitavastatin in humans. Pitavastatin is a potent competitive inhibitor of HMG-CoA reductase little metabolized in hepatic microsomes .
|
-
-
- HY-117605
-
Desmethylsildenafil; UK-103,320
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
N-Desmethyl Sildenafil (Desmethylsildenafil) is a major metabolite of Sildenafil. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor .
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-
-
- HY-124265
-
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Endogenous Metabolite
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Metabolic Disease
|
4β-hydroxy Cholesterol is a major oxysterol cholesterol metabolite and a precursor in the synthesis of bile acids that is found in human circulation .
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-
-
- HY-105014
-
Norastemizole
|
Histamine Receptor
|
Inflammation/Immunology
|
Tecastemizole (Norastemizole), a major metabolite of Astemizole, is a potent and selective H1 receptor antagonist. Tecastemizole shows anti-inflammatory activities .
|
-
-
- HY-W052051
-
N-Acetylbenzylamine
|
Endogenous Metabolite
|
Others
|
N-Benzylacetamide (N-Acetylbenzylamine), as an endogenous metabolite, is the major component of the plasma metabolic profile of Benznidazole (HY-B1548) .
|
-
-
- HY-103005S
-
|
Melatonin Receptor
Drug Metabolite
|
Neurological Disease
Endocrinology
|
Ramelteon metabolite M-II-d3 is the deuterium labeled Ramelteon metabolite M-II. Ramelteon metabolite M-II is the major metabolite of Ramelteon, with IC50s of 208 pM, 1470 pM for human melatonin receptors (MT1 or MT2). Ramelteon is a selective melatonin agonist[1][2].
|
-
-
- HY-132675S
-
|
Isotope-Labeled Compounds
|
Others
|
Prochlorperazine Sulfoxide-d3 is a deuterium labeled Prochlorperazine Sulfoxide. Prochlorperazine Sulfoxide is the major metabolite of the antiemetic Prochlorperazine[1][2].
|
-
-
- HY-136327
-
|
DNA Alkylator/Crosslinker
|
Cancer
|
Phenylacetic acid mustard is the major metabolite of the cancer chemotherapeutic agent Chlorambucil (HY-13593). Chlorambucil is an alkylating agent with antitumor activity .
|
-
-
- HY-Y1771
-
Phthalaldehydic acid
|
Drug Metabolite
|
Infection
|
2-Carboxybenzaldehyde is the major metabolite found in phenanthrene metabolism. Phenanthrene can be degrade by Pseudomonas sp. Lphe-2 strain .
|
-
-
- HY-13332
-
25-hydroxy Vitamin D3-d6
|
VD/VDR
|
Metabolic Disease
|
Calcifediol-d6 is the deuterium labeled Calcifediol. Calcifediol, a major circulating metabolite of vitamin D3, is a potent VDR ligand .
|
-
-
- HY-N1902
-
-
-
- HY-19657
-
-
-
- HY-136608
-
|
nAChR
|
Neurological Disease
|
5-AAM-2-CP is a major metabolite of Acetamiprid. Acetamiprid is a neonicotinoid insecticide used worldwide and is a nAChR agonist .
|
-
-
- HY-136609
-
|
nAChR
|
Neurological Disease
|
5-AMAM-2-CP is a major metabolite of Acetamiprid. Acetamiprid is a neonicotinoid insecticide used worldwide and is a nAChR agonist .
|
-
-
- HY-136591
-
|
Drug Metabolite
|
Neurological Disease
Cancer
|
Demoxepam is a major metabolite of Chlordiazepoxide. Demoxepam exhibits cytotoxicity activity against cancer cell lines. Demoxepam has anticonvulsant and anxiolytic effects .
|
-
-
- HY-D0300
-
|
Fluorescent Dye
|
Others
|
Leucomalachite green is a triphenylmethane dye used to detect blood. Leucomalachite green, a major metabolite of malachite green, is a potential carcinogen, teratogen and mutagen .
|
-
- HY-118166
-
NSC 329491; 1,3,7-Trihydroxyxanthone
|
5-HT Receptor
|
Neurological Disease
|
Gentisein (NSC 329491), the major metabolite of Mangiferin, shows the most potent serotonin uptake inhibition with an IC50 value of 4.7 µM .
|
-
- HY-126848
-
-
- HY-N2057
-
|
Aquaporin
|
Metabolic Disease
|
Steviol is a major metabolite of the sweetening compound stevioside. Steviol slows renal cyst growth by reducing AQP2 expression and promoting AQP2 degradation .
|
-
- HY-111431
-
p-Tolyl sulfate
|
Endogenous Metabolite
|
Metabolic Disease
|
p-Cresyl Sulfate, a major uremic toxin derived from the metabolites of tyrosine and phenylalanine through liver, existed in the blood of patients with chronic kidney disease (CKD).
|
-
- HY-134200
-
|
Endogenous Metabolite
|
Others
|
1-Palmitoyl-2-oleoyl-sn-glycerol is an endogenous metabolite and is a major diacylglycerol in the hormogonium-inducing factor (HIF)-1 .
|
-
- HY-Z0548
-
Protocatechuic acid methyl ester; Methyl protocatechuate
|
Keap1-Nrf2
Apoptosis
|
Inflammation/Immunology
Cancer
|
Methyl 3,4-dihydroxybenzoate (Protocatechuic acid methyl ester; Methyl protocatechuate) is a major metabolite of antioxidant polyphenols found in green tea. Antioxidant and anti-inflammatory effect .
|
-
- HY-100635S
-
-
- HY-135811
-
|
Parasite
Toll-like Receptor (TLR)
Autophagy
|
Infection
|
Desethyl chloroquine is a major desethyl metabolite of Chloroquine. Chloroquine diphosphate is an inhibitor of autophagy and toll-like receptors (TLRs). Desethyl chloroquine possesses antiplasmodic activity .
|
-
- HY-100652A
-
|
Factor Xa
|
Cardiovascular Disease
|
O-Desmethyl apixaban sulfate sodium is a major circulating metabolite of Apixaban in humans. O-Desmethyl apixaban sulfate sodium inhibits factor X (FXa) with a Ki of 58 μM .
|
-
- HY-113344
-
-
- HY-122139
-
|
Bacterial
|
Infection
|
Desethylene Ciprofloxacin hydrochloride is a major metabolite of Ciprofloxacin (HY-B0356). Ciprofloxacin is an orally active topoisomerase IV inhibitor. Desethylene Ciprofloxacin hydrochloride has antibacterial activity .
|
-
- HY-W086896
-
-
- HY-126857A
-
|
Drug Metabolite
|
Others
|
5-Hydroxyomeprazole sodium is the major metabolite of Omeprazole (HY-B0113). Measuring 5-Hydroxyomeprazole levels in plasma can determine the extent of Omeprazole metabolism .
|
-
- HY-Z4690
-
-
- HY-135811A
-
|
Parasite
Toll-like Receptor (TLR)
Autophagy
|
Infection
|
Desethyl chloroquine diphosphate is a major desethyl metabolite of Chloroquine. Chloroquine diphosphate is an inhibitor of autophagy and toll-like receptors (TLRs). Desethyl chloroquine diphosphate possesses antiplasmodic activity .
|
-
- HY-135847
-
SSR97213
|
Parasite
Drug Metabolite
|
Infection
|
Desmethyl ferroquine (SSR97213) is the active and major metabolite of Ferroquine. Ferroquine is an antimalarial. Desmethyl ferroquine shows significant activity against Chloroquine-susceptible and resistant P. falciparum strains .
|
-
- HY-B1986
-
4,4'-DDE; p,p'-Dichlorodiphenyldichloroethylene
|
Androgen Receptor
Drug Metabolite
|
Endocrinology
|
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 .
|
-
- HY-122423
-
N-Deethylamiodarone; LB 33020
|
Apoptosis
Drug Metabolite
|
Cardiovascular Disease
Cancer
|
Desethylamiodarone (N-Deethylamiodarone) is the major metabolite of antiarrhythmic compound Amiodarone (HY-14187). Desethylamiodarone has antiarrhythmic activity. Desethylamiodaron also induces cancer cell apoptosis .
|
-
- HY-126995R
-
|
Endogenous Metabolite
|
Metabolic Disease
|
Glycohyodeoxycholic acid (Standard) is the analytical standard of Glycohyodeoxycholic acid. This product is intended for research and analytical applications. Glycohyodeoxycholic acid is a major metabolite of Hyodeoxycholic acid in humans. Glycohyodeoxycholic acid has preventative effects on gallstone formation .
|
-
- HY-125632
-
|
Parasite
|
Infection
|
Ro 19-9638 is the major metabolite of Ro 15-0216. Ro 19-9638 exhibits antiparasitic efficacy against Trypanosoma brucei rhodesiense with an IC50 of 0.0341 µg/mL .
|
-
- HY-100046R
-
|
Drug Metabolite
|
Neurological Disease
|
Nordoxepin (hydrochloride) (Standard) is the analytical standard of Nordoxepin (hydrochloride). This product is intended for research and analytical applications. Nordoxepin hydrochloride is the major metabolite of Doxepin. Doxepin is a tricyclic antidepressant that is widely prescribed for the research of mild depression .
|
-
- HY-N3059R
-
|
Drug Metabolite
|
Neurological Disease
Cancer
|
Pinostilbene (Standard) is the analytical standard of Pinostilbene. This product is intended for research and analytical applications. Pinostilbene (trans-Pinostilbene) is a major metabolite of Pterostilbene. Pinostilbene exhibits inhibitory effects on colon cancer cells .
|
-
- HY-126857R
-
|
Drug Metabolite
|
Others
|
5-Hydroxyomeprazole (Standard) is the analytical standard of 5-Hydroxyomeprazole. This product is intended for research and analytical applications. 5-Hydroxyomeprazole is the major metabolite of Omeprazole (HY-B0113).
|
-
- HY-N4067
-
isoCDCA
|
Others
|
Inflammation/Immunology
Cancer
|
Isochenodeoxycholic acid (isoCDCA) is a human fecal bile acid. Isochenodeoxycholic acid has cytoprotective against ethanol-induced cell injuries in HepG2 cells. Isochenodeoxycholic acid is a major metabolite of orally administered ursodeoxycholic acid (UDCA) .
|
-
- HY-107850S
-
NSC 1612-d5; NSC 47462-d5
|
Endogenous Metabolite
|
Metabolic 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].
|
-
- HY-137532S
-
-
- HY-100662S
-
Bisdesethylchloroquine-d4
|
Isotope-Labeled Compounds
Drug Metabolite
|
Cardiovascular Disease
|
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].
|
-
- HY-138795
-
|
Others
|
Cancer
|
Curcumin-β-D-glucuronide is a major metabolite after oral intake of Curcumin in hepatic tissue and portal blood. Curcumin-β-D-glucuronide can be used for the research of colon cancer .
|
-
- HY-137532S1
-
|
Isotope-Labeled Compounds
|
Neurological Disease
|
7-Hydroxyquetiapine-d4 (hemifumarate) is deuterium labeled 7-Hydroxyquetiapine. 7-Hydroxyquetiapine (ICI 214227) is the major active metabolite of antipsychotic medicine Quetiapine[1].
|
-
- HY-G0016
-
MADDS; Monoacetyldapsone
|
Drug Metabolite
|
Others
|
N-Acetyl dapsone (MADDS) is the major metabolite of Dapsone (HY-B0688). Dapsone is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities .
|
-
- HY-B1178R
-
|
Endogenous Metabolite
nAChR
|
Cardiovascular Disease
Inflammation/Immunology
|
Cotinine (Standard) is the analytical standard of Cotinine. This product is intended for research and analytical applications. Cotinine ((-)-Cotinine), an alkaloid in tobacco and a major metabolite of nicotine, is used as a biological indicator to measure the composition of tobacco smoke
|
-
- HY-130353
-
N-desethylamiodarone hydrochloride; LB 33020 hydrochloride
|
Potassium Channel
Autophagy
|
Cardiovascular Disease
|
Desethylamiodarone hydrochloride (N-desethylamiodarone hydrochloride) is a major active metabolite of Amiodarone. Desethylamiodarone hydrochloride is formed by CYP3A isoenzymes. Amiodarone is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM .
|
-
- HY-N7387
-
|
Endogenous Metabolite
|
Metabolic Disease
|
3-Oxocholic acid is an oxo-bile acid metabolite and also a major degradation product from cholic by C. perfringens in the intestine. 3-Oxocholic acid is steroid acid found predominantly in bile of mammals .
|
-
- HY-135895
-
-
- HY-124087
-
4-en-VPA; 2-Allylpentanoic acid
|
Drug Metabolite
|
Others
|
(±)-2-Propyl-4-pentenoic acid (4-en-VPA) is a major toxic metabolite of Valproic acid. (±)-2-Propyl-4-pentenoic acid exhibits neuroteratogenicity .
|
-
- HY-148051
-
-
- HY-135176
-
|
Endogenous Metabolite
|
Cancer
|
13-Dihydrocarminomycin (compound D788-12) is the major metabolite of the antitumor antibiotic Carminomycin (HY-B2171). 13-Dihydrocarminomycin has weak antitumor activity .
|
-
- HY-W009934
-
α-Phenyl-2-pyridineacetonitrile
|
Drug Metabolite
|
Endocrinology
|
2-Phenyl-2-(2-pyridyl)acetonitrile is the major metabolite of SC 15396 metabolized by the supernatant fraction of rat liver homogenate. SC 15396 is an antigastrin that inhibits gastric secretion .
|
-
- HY-N0929
-
|
COX
Reactive Oxygen Species
|
Cancer
|
Hexahydrocurcumin is one of the major metabolites of curcumin and a selective, orally active COX-2 inhibitor. Hexahydrocurcumin is inactive against COX-1. Hexahydrocurcumin has antioxidant, anticancer and anti-inflammatory activities .
|
-
- HY-130569
-
|
Drug Metabolite
|
Inflammation/Immunology
Cancer
|
7-Hydroxymethotrexate is a major metabolite of Methotrexate (MTX; HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis .
|
-
- HY-W040047
-
|
Endogenous Metabolite
|
Endocrinology
|
Pregnanediol 3-glucuronide is the major terminal metabolite of progesterone, playing an important role in physiological processes, such as the female menstrual cycle, pregnancy (supports gestation), embryogenesis and maternal immune response of humans and other species .
|
-
- HY-148377
-
|
Others
|
Cancer
|
Abiraterone sulfate N-oxide is a carboxylic acid. Abiraterone sulfate N-oxide also is a major metabolite of Abiraterone (HY-70013). Abiraterone sulfate N-oxide can be used for the research of prostate cancer .
|
-
- HY-N7143S
-
|
Isotope-Labeled Compounds
|
Endocrinology
|
Monobutyl phthalate-d4 is the deuterium labeled Monobutyl phthalate[1]. Monobutyl phthalate, a major metabolite of dibutyl phthalate (DBP), possesses antiandrogenic effects. Monobutyl phthalate is an embryotoxicant[2][3].
|
-
- HY-125559
-
|
Others
|
Cardiovascular Disease
|
Jesaconitine is a toxic alkaloid. Jesaconitine can be derived from Aconitum. Jesaconitine is one of the major metabolites that can be detected in the blood of the right atrium after aconitum poisoning. Various types of arrhythimia are characteristic in aconitine intoxication .
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-
- HY-N7143R
-
|
Drug Metabolite
|
Metabolic Disease
Endocrinology
|
Monobutyl phthalate (Standard) is the analytical standard of Monobutyl phthalate. This product is intended for research and analytical applications. Monobutyl phthalate, a major metabolite of dibutyl phthalate (DBP), possesses antiandrogenic effects. Monobutyl phthalate is an embryotoxicant .
|
-
- HY-118010
-
(±)-Norfenfluramine
|
Serotonin Transporter
|
Neurological Disease
|
Norfenfluramine ((±)-Norfenfluramine) is a major and brain-penetrant metabolite of Fenfluramine. Norfenfluramine can interact with 5-HT transporters to release 5-HT from neurons. Norfenfluramine displays antiepileptic effects in vivo .
|
-
- HY-142075
-
|
Bacterial
|
Infection
|
Antibacterial agent 134 (compound 1) is an diketopiperazine alkaloid with antimicrobial activity. Antibacterial agent 134 is the major metabolite in the culture of Hymeniacidon perleve associated bioactive bacterium Pseudomonas sp. NJ6-3-1 .
|
-
- HY-128038
-
|
Opioid Receptor
|
Neurological Disease
|
N-Desmethyl-loperamide is a major metabolite of loperamide, a drug that selectively activates peripheral μopioid receptors with a Ki value of 0.16 nM. N-Desmethyl-loperamide is a substrate of the ATP-dependent efflux transporter P-glycoprotein .
|
-
- HY-D0300S
-
|
Fluorescent Dye
Isotope-Labeled Compounds
|
Others
|
Leucomalachite green-d5 is the deuterium labeled Leucomalachite green. Leucomalachite green is a triphenylmethane dye used to detect blood. Leucomalachite green, a major metabolite of malachite green, is a potential carcinogen, teratogen and mutagen[1][2].
|
-
- HY-B1984
-
4,4'-DDD; p,p'-Dichlorodiphenyl dichloroethane
|
Drug Metabolite
|
Others
|
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 .
|
-
- HY-19657R
-
-
- HY-125505
-
|
Factor Xa
|
Cardiovascular Disease
|
BI-11634 is a factor Xa inhibitor. BI-11634 is metabolized by CYP3A4 to form one major metabolite and this reaction is inhibited by Quinidine (HY-B1751H) with a Ki of 7 µM .
|
-
- HY-136591R
-
|
Drug Metabolite
|
Neurological Disease
Cancer
|
Demoxepam (Standard) is the analytical standard of Demoxepam. This product is intended for research and analytical applications. Demoxepam is a major metabolite of Chlordiazepoxide. Demoxepam exhibits cytotoxicity activity against cancer cell lines. Demoxepam has anticonvulsant and anxiolytic effects .
|
-
- HY-131479A
-
|
Drug Metabolite
|
Neurological Disease
|
Threo-dihydrobupropion is a major metabolite of Bupropion, formed via oxidation and reduction exhibit pharmacological activity. Bupropion, a dual dopamine-norepinephrine uptake inhibitor and a nicotine receptor antagonist, is widely used in the management of depression and as a smoking cessation aid .
|
-
- HY-B0212
-
|
Bacterial
Antibiotic
|
Infection
Inflammation/Immunology
|
Sulfapyridine, a major metabolite of Sulfasalazine, is a sulfonamide antibiotic agent. Sulfapyridine inhibits recombinant P. carinii dihydropteroate synthetase (DHPS) with an IC50 of 0.18 μM. Sulfapyridine has antibacterial, anti-inflammatory and anti-rheumatic activities .
|
-
- HY-15895
-
ACT-132577
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of Macitentan. Aprocitentan is dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively .
|
-
- HY-W017100
-
6-Methoxysalicylic acid
|
Others
|
Neurological Disease
|
2-Hydroxy-6-methoxybenzoic acid can be used for the determination of acetylsalicylic acid and its major metabolite, salicylic acid, in animal plasma. 2-Hydroxy-6-methoxybenzoic acid exhibits significant analgesic effects .
|
-
- HY-12753S1
-
SR35021-dd6 hydrochloride
|
Isotope-Labeled Compounds
Drug Metabolite
|
Cardiovascular Disease
|
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].
|
-
- HY-12753S
-
SR35021-d7
|
Isotope-Labeled Compounds
Drug Metabolite
|
Cardiovascular Disease
|
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].
|
-
- HY-W394903
-
|
JAK
Drug Metabolite
|
Cancer
|
GS-829845 is a major, active metabolite of Filgotinib (HY-18300). GS-829845 is a JAK1 preferential inhibitor but is approximately 10-fold less potent than the parent and with a longer half-life .
|
-
- HY-17011
-
|
Others
|
Metabolic Disease
|
Croconazole is an antifungal agent containing imidazole rings. Croconazole has a unique structural feature of aryl vinyl at the imidazole ring N-1. Croconazole can be used for the identification and quantitative study of major metabolites in rat urine and bile .
|
-
- HY-N2057R
-
|
Aquaporin
|
Metabolic Disease
|
Steviol (Standard) is the analytical standard of Steviol. This product is intended for research and analytical applications. Steviol is a major metabolite of the sweetening compound stevioside. Steviol slows renal cyst growth by reducing AQP2 expression and promoting AQP2 degradation .
|
-
- HY-129903R
-
|
Others
|
Others
|
N-Desethyl vardenafil (Standard) is the analytical standard of N-Desethyl vardenafil. This product is intended for research and analytical applications. N-Desethyl vardenafil is the major metabolite of Vardenafil (HY-B0442) and can be detected in human urine .
|
-
- HY-W096561
-
|
Others
|
Cardiovascular Disease
|
Amiquinsin is a compound with hypotensive activity. Amiquinsin is metabolized in vivo, and the major metabolite is 4-amino-6,7-dimethoxy-3-quinolinol hydrochloride hydrate. The pharmacological and toxicological properties of amiquinsin have been widely discussed .
|
-
- HY-W040047S
-
-
- HY-135811S
-
-
- HY-135408
-
|
Drug Metabolite
|
Cardiovascular Disease
Inflammation/Immunology
|
Trimetazidine-N-oxide is the major active metabolite of Trimetazidine. Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM. Trimetazidine is an effective antianginal agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties.
|
-
- HY-135811S1
-
-
- HY-I1111S4
-
|
Isotope-Labeled Compounds
|
Others
|
Fmoc-L-Val-OH- 15N is a 15N-labeled Leucomalachite green. Leucomalachite green is a triphenylmethane dye used to detect blood. Leucomalachite green, a major metabolite of malachite green, is a potential carcinogen, teratogen and mutagen[1][2].
|
-
- HY-B2150
-
4-Hydroxyphenazone; NSC 174055
|
Drug Metabolite
|
Others
|
4-Hydroxyantipyrine (4-Hydroxyphenazone; NSC 174055) is the major metabolite of Antipyrine (HY-B0171), can be as a biodistribution promoter. 4-Hydroxyantipyrine can increase distribution of concentration ratio of Citicoline and Antipyrine in the brain .
|
-
- HY-W016321
-
N-Phenylbenzylamine; Benzylaniline
|
Others
|
Others
|
N-Benzylaniline (N-Phenylbenzylamine) is an N-alkylated derivative of aniline. N-benzyl aniline also is a major metabolite of the antihistamine antazoline and other N-substituted benzyl anilines. N-Benzylaniline can be used for the research of various biochemical studies .
|
-
- HY-117605R
-
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
N-Desmethyl Sildenafil (Standard) is the analytical standard of N-Desmethyl Sildenafil. This product is intended for research and analytical applications. N-Desmethyl Sildenafil (Desmethylsildenafil) is a major metabolite of Sildenafil. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor .
|
-
- HY-D0300R
-
|
Fluorescent Dye
|
Others
|
Leucomalachite green (Standard) is the analytical standard of Leucomalachite green. This product is intended for research and analytical applications. Leucomalachite green is a triphenylmethane dye used to detect blood. Leucomalachite green, a major metabolite of malachite green, is a potential carcinogen, teratogen and mutagen .
|
-
- HY-12766
-
|
Dopamine Transporter
nAChR
|
Neurological Disease
|
Bupropion morpholinol (Hydroxy Bupropion) is a major metabolite of Bupropion. Bupropion morpholinol inhibits Dopamine, Norepinephrine transporters and the α4β2 nicotinic receptor in vitro. Bupropion morpholinol contributes to antidepressant and smoking cessation activities .
|
-
- HY-117605S
-
-
- HY-N1902S
-
|
Keap1-Nrf2
Endogenous Metabolite
|
Metabolic Disease
|
4-Hydroxyphenylacetic acid-d6 is the deuterium labeled 4-Hydroxyphenylacetic acid. 4-hydroxyphenylacetic acid, a major microbiota-derived metabolite of polyphenols, is involved in the antioxidative action. 4-hydroxyphenylacetic acid induces expression of Nrf2[1].
|
-
- HY-124265S2
-
|
Endogenous Metabolite
|
Metabolic Disease
|
4β-Hydroxycholesterol-d4 is the deuterium labeled 4β-Hydroxycholesterol. 4β-hydroxy Cholesterol is a major oxysterol cholesterol metabolite and a precursor in the synthesis of bile acids that is found in human circulation[1][2].
|
-
- HY-137522A
-
3'-Azido-3'-deoxythymidine β-D-glucuronide
|
Drug Metabolite
|
Others
|
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 .
|
-
- HY-Y1771R
-
|
Drug Metabolite
|
Infection
|
2-Carboxybenzaldehyde (Standard) is the analytical standard of 2-Carboxybenzaldehyde. This product is intended for research and analytical applications. 2-Carboxybenzaldehyde is the major metabolite found in phenanthrene metabolism. Phenanthrene can be degrade by Pseudomonas sp. Lphe-2 strain .
|
-
- HY-100637
-
|
Drug Metabolite
Adrenergic Receptor
nAChR
|
Neurological Disease
|
Hydroxybupropion is the major active metabolite of Bupropion. Hydroxybupropion is metabolized by CYP2B6. Bupropion is an atypical antidepressant and smoking-cessation agent. Hydroxybupropion inhibits norepinephrine uptake with an IC50 value of 1.7 μM. Hydroxybupropion is also a nACh receptor antagonist .
|
-
- HY-B0602B
-
O-Desmethylvenlafaxine fumarate
|
5-HT Receptor
Adrenergic Receptor
Drug Metabolite
|
Neurological Disease
|
Desvenlafaxine (O-Desmethylvenlafaxine) fumarate is a selective serotonin and norepinephrine reuptake inhibitor. Desvenlafaxine (O-Desmethylvenlafaxine) fumarate is the major metabolite of the antidepressant venlafaxine. Desvenlafaxine (O-Desmethylvenlafaxine) fumarate has the potential for the research of depression and related disorders and diseases (extracted from patent WO2009049354A1) .
|
-
- HY-B0602C
-
O-Desmethylvenlafaxine hydrochloride
|
5-HT Receptor
Adrenergic Receptor
Drug Metabolite
|
Neurological Disease
|
Desvenlafaxine (O-Desmethylvenlafaxine) hydrochloride is a selective serotonin and norepinephrine reuptake inhibitor. Desvenlafaxine (O-Desmethylvenlafaxine) hydrochloride is the major metabolite of the antidepressant venlafaxine. Desvenlafaxine (O-Desmethylvenlafaxine) hydrochloride has the potential for the research of depression and related disorders and diseases (extracted from patent WO2009049354A1) .
|
-
- HY-116462
-
|
Drug Metabolite
|
Others
|
ONO-EI-601 is the major metabolite of human neutrophil elastase inhibitor ONO-5046. ONO-5046 has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19 .
|
-
- HY-P3100
-
|
Parasite
|
Infection
|
Orfamide A is a major metabolite of insecticidal biosurfactant in Pseudomonas sp. F6 and has aphidicidal activity. Orfamide A can be used for aphid control in organic agriculture. Orfamide A exhibits dose-dependent mortality against aphids with an LC50 value of 34.5 μg/mL .
|
-
- HY-122139R
-
|
Bacterial
|
Infection
|
Desethylene Ciprofloxacin (hydrochloride) (Standard) is the analytical standard of Desethylene Ciprofloxacin (hydrochloride). This product is intended for research and analytical applications. Desethylene Ciprofloxacin hydrochloride is a major metabolite of Ciprofloxacin (HY-B0356). Ciprofloxacin is an orally active topoisomerase IV inhibitor. Desethylene Ciprofloxacin hydrochloride has antibacterial activity .
|
-
- HY-135811R
-
|
Parasite
Toll-like Receptor (TLR)
Autophagy
|
Infection
|
Desethyl chloroquine (Standard) is the analytical standard of Desethyl chloroquine. This product is intended for research and analytical applications. Desethyl chloroquine is a major desethyl metabolite of Chloroquine. Chloroquine diphosphate is an inhibitor of autophagy and toll-like receptors (TLRs). Desethyl chloroquine possesses antiplasmodic activity .
|
-
- HY-109619
-
Δ4-Abiraterone; CB-7627; Abiraterone D4A metabolite
|
Androgen Receptor
Cytochrome P450
|
Cancer
|
D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor.
|
-
- HY-B2150S
-
4-Hydroxyphenazone-d3; NSC 174055-d3
|
Drug Metabolite
Isotope-Labeled Compounds
|
Others
|
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].
|
-
- HY-W016388
-
9-Hydroxyfluorene
|
Dopamine Receptor
Drug Metabolite
|
Neurological Disease
|
9-Fluorenol (9-Hydroxyfluorene; compound 3) is a dopamine (DAT) inhibitor with IC50 value of 9 μM. 9-Fluorenol is a major metabolite of compound developed as a wake promoting agent. 9-Fluorenol shows wake promotion activity in vivo .
|
-
- HY-19657S
-
-
- HY-130353S
-
|
Isotope-Labeled Compounds
Potassium Channel
Autophagy
|
Cardiovascular Disease
|
Desethyl Amiodarone-d4 (hydrochloride) is the deuterium labeled Desethylamiodarone hydrochloride. Desethylamiodarone hydrochloride (N-desethylamiodarone hydrochloride) is a major active metabolite of Amiodarone. Desethylamiodarone hydrochloride is formed by CYP3A isoenzymes. Amiodarone is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM[1][2][3].
|
-
- HY-124265S1
-
-
- HY-15895S
-
-
- HY-122009
-
Indoxyl-β-D-glucoside
|
Fluorescent Dye
OAT
|
Others
|
Indican (Indoxyl-β-D-glucoside), a glycoside of indoxyl, is a precursor of the dyesindigo and indirubin. Indican has a major metabolite, indoxyl sulfate (IS). IS, an uremic toxin, is a substrate/inhibitor of organic anion transporter (OAT) 1, OAT 3 and multidrug resistance-associated protein (MRP) 4 .
|
-
- HY-N1902S1
-
|
Keap1-Nrf2
Endogenous Metabolite
|
Metabolic Disease
|
4-Hydroxyphenylacetic acid-d4 is the deuterium labeled 4-Hydroxyphenylacetic acid[1]. 4-hydroxyphenylacetic acid, a major microbiota-derived metabolite of polyphenols, is involved in the antioxidative action. 4-hydroxyphenylacetic acid induces expression of Nrf2[2].
|
-
- HY-129431
-
|
Others
|
Others
|
U-89843A is a precursor of U-97924 and forms U-97924 as the major metabolite. Although U-97924 showed mutagenic potential in rat hepatocytes in a serum-free in vitro assay, no genotoxicity of U-97924 was observed in rats at high oral doses. Rat serum also inhibited the in vitro metabolism of U-89843 and the formation of the corresponding hydroxylated metabolite, U-97924 .
|
-
- HY-136578
-
-
- HY-N8796
-
|
Others
|
Cancer
|
2',4'-Dihydroxy-4,6'-diMethoxydihydrochalcone is a dihydrochalcone compound isolated from Iryanthera juruensis Warb. 2',4'-Dihydroxy-4,6'-diMethoxydihydrochalcone is a major cytotoxic metabolite when tested against a panel of cancer cell lines .
|
-
- HY-130353R
-
N-desethylamiodarone (hydrochloride)(Standard); LB 33020 hydrochloride (Standard)
|
Potassium Channel
Autophagy
|
Cardiovascular Disease
|
Desethylamiodarone (hydrochloride) (Standard) is the analytical standard of Desethylamiodarone (hydrochloride). This product is intended for research and analytical applications. Desethylamiodarone hydrochloride (N-desethylamiodarone hydrochloride) is a major active metabolite of Amiodarone. Desethylamiodarone hydrochloride is formed by CYP3A isoenzymes. Amiodarone is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM .
|
-
- HY-W086896R
-
|
Drug Metabolite
|
Inflammation/Immunology
|
α-Demethylnaproxen (Standard) is the analytical standard of α-Demethylnaproxen. This product is intended for research and analytical applications. α-Demethylnaproxen is the major metabolite of Nabumetone (HY-B0559), Nabumetone is an orally active COX-2 inhibitor with anti-inflammatory activity .
|
-
- HY-W018392
-
MEHP; Phthalic acid mono-2-ethylhexyl ester
|
Endogenous Metabolite
|
Metabolic Disease
|
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) .
|
-
- HY-18646
-
24-Oxo-23,25-dihydroxyvitamin D3
|
Endogenous Metabolite
|
Metabolic Disease
|
23,25-Dihydroxy-24-oxovitamin D3 is a major metabolite of 24(R),25-Dihydroxyvitamin D3. 23,25-Dihydroxy-24-oxovitamin D3 can be used for the research of metabolic diseases .
|
-
- HY-B1986S
-
4,4'-DDE-d8; p,p'-Dichlorodiphenyldichloroethylene-d8
|
Androgen Receptor
Drug Metabolite
|
Endocrinology
|
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].
|
-
- HY-N0929R
-
|
COX
Reactive Oxygen Species
|
Cancer
|
Hexahydrocurcumin (Standard) is the analytical standard of Hexahydrocurcumin. This product is intended for research and analytical applications. Hexahydrocurcumin is one of the major metabolites of curcumin and a selective, orally active COX-2 inhibitor. Hexahydrocurcumin is inactive against COX-1. Hexahydrocurcumin has antioxidant, anticancer and anti-inflammatory activities .
|
-
- HY-B1986R
-
|
Androgen Receptor
Drug Metabolite
|
Endocrinology
|
p,p'-DDE (Standard) is the analytical standard of p,p'-DDE. This product is intended for research and analytical applications. 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 .
|
-
- HY-137263
-
|
Others
|
Infection
|
Propionylmaridomycin is a macrolide antibiotic with antibacterial activity. Propionylmaridomycin is rapidly absorbed from the gastrointestinal tract and rapidly distributed to tissues. Propionylmaridomycin radioactivity levels in the liver, kidneys, and lungs were significantly higher than in plasma, while distribution to the brain was less. Propionylmaridomycin is excreted primarily through the feces, and the high fecal recovery rate is due to unabsorbed compounds and biliary excretion of compounds and their metabolites. Propionylmaridomycin exhibits the highest antibacterial activity in the lungs. Propionylmaridomycin is completely converted to several metabolites in rats, of which 4''-depropionyl-9-propionylmaridomycin was identified as the major metabolite .
|
-
- HY-148642
-
12-hydroxy-NVP; 12-OH-NVP
|
Drug Metabolite
|
Infection
|
12-Hydroxynevirapine (12-hydroxy-NVP; 12-OH-NVP) is a major oxidative metabolite of Nevirapine (HY-10570). Nevirapine is a non-nucleoside reverse transcriptase inhibitor indicated for the HIV-1 infections. Nevirapine causes idiosyncratic hepatotoxicity and mild-to-severe skin rashes. 12-Hydroxynevirapine, a non-reactive metabolite, can be bioactivated by sulphotransferases (SULTs) in the liver and skin, yielding the reactive species 12-Sulphoxy-nevirapine .
|
-
- HY-B0539S
-
-
- HY-B0539S1
-
-
- HY-107096
-
TP3076
|
Topoisomerase
|
Cancer
|
CH-0793076 (TP3076), a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein) .
|
-
- HY-Z0548S1
-
|
Isotope-Labeled Compounds
Keap1-Nrf2
Apoptosis
|
Inflammation/Immunology
Cancer
|
Methyl 3,4-dihydroxybenzoate-d3-1 is the deuterium labeled Methyl 3,4-dihydroxybenzoate. Methyl 3,4-dihydroxybenzoate (Protocatechuic acid methyl ester; Methyl protocatechuate) is a major metabolite of antioxidant polyphenols found in green tea. Antioxidant and anti-inflammatory effect[1].
|
-
- HY-B0539S3
-
-
- HY-118010A
-
|
5-HT Receptor
|
Cardiovascular Disease
|
(+)-Norfenfluramine hydrochloride, a major hepatic metabolite of (+)-fenfluramine, is a selective 5-HT2B receptor agonist (Ki: 11.2 nM). (+)-Norfenfluramine hydrochloride potently stimulates the hydrolysis of inositol phosphates and increases intracellular Ca 2+. (+)-Norfenfluramine hydrochloride can be used for the research of primary pulmonary hypertension and valvular heart disease .
|
-
- HY-W131725
-
|
5-HT Receptor
|
Cardiovascular Disease
|
(+)-Norfenfluramine a major hepatic metabolite of (+)-fenfluramine, is a selective 5-HT2B receptor agonist (Ki: 11.2 nM). (+)-Norfenfluramine potently stimulates the hydrolysis of inositol phosphates and increases intracellular Ca 2+. (+)-Norfenfluramine can be used for the research of primary pulmonary hypertension and valvular heart disease .
|
-
- HY-130569S
-
|
Isotope-Labeled Compounds
Drug Metabolite
|
Inflammation/Immunology
Cancer
|
7-Hydroxymethotrexate-d3 (sodium) is deuterium labeled 7-Hydroxymethotrexate. 7-Hydroxymethotrexate is a major metabolite of Methotrexate (MTX; HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis[1][2].
|
-
- HY-130569S1
-
|
Drug Metabolite
|
Metabolic Disease
|
7-Hydroxymethotrexate-d3 is the deuterium labeled 7-Hydroxymethotrexate. 7-Hydroxymethotrexate is a major metabolite of Methotrexate (MTX; HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis[1][2].
|
-
- HY-125296
-
|
GABA Receptor
|
Neurological Disease
|
Fipronil sulfone is the major metabolite of Fipronil.Fipronil sulfone selectively inhibits GABA receptor with IC50 of 175 nM (assayed by displacement of 4′-ethynyl-4-n-[2,3-3H2]- propylbicycloorthobenzoate ([3H]EBOB) from the noncompetitive blocker site).
|
-
- HY-128554S
-
|
Isotope-Labeled Compounds
Parasite
|
Infection
|
N-Desethyl amodiaquine-d5 is the deuterium labeled N-Desethyl amodiaquine. N-Desethyl amodiaquine is the major biologically active metabolite of Amodiaquine. N-Desethyl amodiaquine is an antiparasitic agent. IC50 values for strains V1/S and 3D7 are 97 nM and 25 nM, respectively[1].
|
-
- HY-128554S1
-
|
Isotope-Labeled Compounds
Parasite
|
Infection
|
N-Desethyl amodiaquine-d5 (dihydrochloride) is the deuterium labeled N-Desethyl amodiaquine dihydrochloride. N-Desethyl amodiaquine dihydrochloride is the major biologically active metabolite of Amodiaquine. N-Desethyl amodiaquine dihydrochloride is an antiparasitic agent. IC50 values for strains V1/S and 3D7 are 97 nM and 25 nM, respectively[1].
|
-
- HY-129099
-
|
PKC
Estrogen Receptor/ERR
Drug Metabolite
Endogenous Metabolite
|
Cancer
|
N-Desmethyltamoxifen is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation .
|
-
- HY-129099A
-
|
PKC
Estrogen Receptor/ERR
Drug Metabolite
Endogenous Metabolite
|
Cancer
|
N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation .
|
-
- HY-107096B
-
TP3076 TFA
|
Topoisomerase
|
Cancer
|
CH-0793076 (TP3076) TFA, a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 TFA inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 TFA is efficacious against cells expressing BCRP (breast cancer resistance protein) .
|
-
- HY-124953
-
|
MAP3K
Apoptosis
|
Cancer
|
7,3',4'-Trihydroxyisoflavone, a major metabolite of Daidzein, is an ATP-competitive inhibitor of Cot (Tpl2/MAP3K8) and MKK4. 7,3',4'-Trihydroxyisoflavone has anticancer, anti-angiogenic, chemoprotective, and free radical scavenging activities .
|
-
- HY-130569S2
-
|
Drug Metabolite
|
Metabolic Disease
|
7-Hydroxymethotrexate-d3 (ammonium) is the deuterium labeled 7-Hydroxymethotrexate ammonium. 7-Hydroxymethotrexate is a major metabolite of Methotrexate (MTX; HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis[1][2].
|
-
- HY-B0539R
-
-
- HY-B0212R
-
|
Bacterial
Antibiotic
|
Infection
Inflammation/Immunology
|
Sulfapyridine (Standard) is the analytical standard of Sulfapyridine. This product is intended for research and analytical applications. Sulfapyridine, a major metabolite of Sulfasalazine, is a sulfonamide antibiotic agent. Sulfapyridine inhibits recombinant P. carinii dihydropteroate synthetase (DHPS) with an IC50 of 0.18 μM. Sulfapyridine has antibacterial, anti-inflammatory and anti-rheumatic activities .
|
-
- HY-15895R
-
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
Aprocitentan (Standard) is the analytical standard of Aprocitentan. This product is intended for research and analytical applications. Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of Macitentan. Aprocitentan is dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively .
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-
- HY-124542
-
|
Drug Metabolite
Apoptosis
|
Cancer
|
5-Hydroxydiclofenac is a major metabolite of Diclofenac (HY-15036). 5-Hydroxydiclofenac is formed by the cytochrome P450 (CYP) isoforms CYP3A4, CYP2C189, CYP2C19, and CYP2C8. 5-Hydroxydiclofenac shows apoptotic effects in hepatocytes .
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-
- HY-120045A
-
|
Others
|
Neurological Disease
|
DuP 747 hydrochloride is an analgesic with selective kappa-opioid receptor agonist activity. DuP 747 showed less spiradoline-appropriate selection when administered SC, but showed a partial generalized response to spiradoline when administered IP or PO. The 5-hydroxy-desmethoxy metabolite of DuP 747 induced selection of the saline-appropriate lever only. The effects of DuP 747 suggest that its metabolites may play a major role in the similar responses to spiradoline after IP and PO administration .
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-
- HY-N1967
-
|
Fatty Acid Synthase (FASN)
|
Metabolic Disease
|
Dihydrocurcumin, a major metabolites of curcumin, reduces lipid accumulation and oxidative stress. Dihydrocurcumin regulates mRNA and protein expression levels of SREBP-1C, PNPLA3 and PPARα, increases protein expression levels of pAKT and PI3K, and reduced the levels of cellular NO and ROS via Nrf2 signaling pathways .
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-
- HY-N0179
-
α-Ecdysone
|
Endogenous Metabolite
Apoptosis
|
Metabolic Disease
|
Ecdysone (α-Ecdysone), a major steroid hormone in insects and herbs, triggers mineralocorticoid receptor (MR) activation and induces cellular apoptosis. Ecdysone plays essential roles in coordinating developmental transitions and homeostatic sleep regulation through its active metabolite 20-hydroxyecdysone (Crustecdysone; 20E; HY-N6979) .
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-
- HY-P1141
-
|
GCGR
|
Metabolic Disease
|
GLP-1(9-36)amide is a major metabolite of glucagon-like peptide-1-(7-36) amide formed by the enzyme dipeptidyl peptidase-4 (DPP-4). GLP-1(9-36)amide acts as an antagonist to the human pancreatic GLP-1 receptor .
|
-
- HY-B1984S
-
4,4'-DDD-d8; p,p'-Dichlorodiphenyl dichloroethane-d8
|
Drug Metabolite
|
Others
|
p,p'-DDD-d8 is the deuterium labeled p,p'-DDD[1]. 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[2][3].
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-
- HY-161125
-
|
Others
|
Others
|
(+)-JQ1-OH is the major metabolite of (+)-JQ1(HY-13030). (+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy .
|
-
- HY-B0539S4
-
-
- HY-B1984R
-
|
Drug Metabolite
|
Others
|
p,p'-DDD (Standard) is the analytical standard of p,p'-DDD. This product is intended for research and analytical applications. 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 .
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-
- HY-A0019
-
9-Hydroxyrisperidone
|
Drug Metabolite
Dopamine Receptor
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia .
|
-
- HY-B0539S2
-
-
- HY-135810
-
Desethylhydroxychloroquine
|
Influenza Virus
Parasite
|
Infection
Inflammation/Immunology
|
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 .
|
-
- HY-P1141A
-
|
GCGR
|
Metabolic Disease
|
GLP-1(9-36)amide TFA is a major metabolite of glucagon-like peptide-1-(7-36) amide formed by the enzyme dipeptidyl peptidase-4 (DPP-4). GLP-1(9-36)amide TFA acts as an antagonist to the human pancreatic GLP-1 receptor .
|
-
- HY-Y0469
-
|
Drug Metabolite
|
Others
|
1-Aminohydantoin hydrochloride is a major metabolite of nitrofurantoin in animal tissues and can be used as a standard for the determination of residues of veterinary agents in meat, milk et.al. 1-Aminohydantoin hydrochloride covalently binds to tissue proteins and is released from the tissues under slightly acidic conditions and derivatized with 2-nitrobenzaldehyde to form nitrophenyl derivatives of AHD before detection .
|
-
- HY-B2150R
-
4-Hydroxyphenazone (Standard); NSC 174055 (Standard)
|
Drug Metabolite
|
Others
|
4-Hydroxyantipyrine (Standard) is the analytical standard of 4-Hydroxyantipyrine. This product is intended for research and analytical applications. 4-Hydroxyantipyrine (4-Hydroxyphenazone; NSC 174055) is the major metabolite of Antipyrine (HY-B0171), can be as a biodistribution promoter. 4-Hydroxyantipyrine can increase distribution of concentration ratio of Citicoline and Antipyrine in the brain .
|
-
- HY-76569
-
PNU-200577; 5-Hydroxymethyl Tolterodine
|
mAChR
|
Neurological Disease
|
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) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
|
-
- HY-G0021
-
Norclozapine; Desmethylclozapine; Normethylclozapine
|
mAChR
Opioid Receptor
Drug Metabolite
Virus Protease
|
Infection
|
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 .
|
-
- HY-135334
-
|
Drug Metabolite
Btk
Cytochrome P450
|
Cancer
|
ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC50 of 5.0 nM for Bruton tyrosine kinase (BTK). ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM .
|
-
- HY-108263B
-
(R)-CGP52421
|
FLT3
Drug Metabolite
|
Cancer
|
(R)-3-Hydroxy Midostaurin ((R)-CGP52421) is a potent kinases inhibitor. (R)-3-Hydroxy Midostaurin is a major metabolite of midostaurin (PKC412; HY-10230) undergoing by the hepatic CYP3A4 enzyme. (R)-3-Hydroxy Midostaurin has the potential for acute myeloid leukemia (AML) .
|
-
- HY-139427
-
β-Methylglutaconic acid
|
GABA Receptor
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
|
3-Methylglutaconic acid is the major metabolites accumulating in 3-Methylglutaconic aciduria (MGTA). 3-Methylglutaconic acid can induce lipid oxidative damage and protein oxidative. 3-Methylglutaconic acid decreases the non-enzymatic antioxidant defenses in cerebral cortex supernatants to elicit oxidative stress in the cerebral cortex. 3-Methylglutaconic acid can be used for brain damage disease research .
|
-
- HY-B0602
-
O-Desmethylvenlafaxine
|
Serotonin Transporter
|
Neurological Disease
|
Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter .
|
-
- HY-D0004
-
Azure B chloride
|
Monoamine Oxidase
|
Neurological Disease
|
Azure B is a cationic dye and the major metabolite of Methylene blue. Azure B is used in making Azure eosin stains for blood smear staining. Azure B is a high-potency, selective and reversible inhibitor of monoamine oxidases (MAO)-A, with IC50s of 11 and 968 nM for recombinant human MAO-A and MAO-B, respectively. Azure B possesses significant antidepressant-like effects .
|
-
- HY-N7307
-
|
Bacterial
|
Infection
|
Pachybasin is a major metabolite from culture broth of endophytic coelomyceteous AFKR-18 fungus. Pachybasin showes antimicrobial activities against E. coli, B. subtilis, M. luteus, S. cerevisiae, C. albicans, A. niger, and A. flavus, with MIC values of 64.0 μg/mL, and against S. aureus and F. oxysporum with MIC values of 32.0 and 16.0 μg/mL respectively .
|
-
- HY-W016388R
-
|
Dopamine Receptor
Drug Metabolite
|
Neurological Disease
|
9-Fluorenol (Standard) is the analytical standard of 9-Fluorenol. This product is intended for research and analytical applications. 9-Fluorenol (9-Hydroxyfluorene; compound 3) is a dopamine (DAT) inhibitor with IC50 value of 9 μM. 9-Fluorenol is a major metabolite of compound developed as a wake promoting agent. 9-Fluorenol shows wake promotion activity in vivo .
|
-
- HY-16170
-
O-Desmethylvenlafaxine succinate; Wy-45233 succinate
|
Serotonin Transporter
|
Neurological Disease
Metabolic Disease
|
Desvenlafaxine succinate, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine succinate (DVS) shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter .
|
-
- HY-B0602A
-
O-Desmethylvenlafaxine succinate hydrate; Desvenlafaxine succinate monohydrate
|
Serotonin Transporter
|
Neurological Disease
|
Desvenlafaxine succinate hydrate, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine succinate hydrate shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter .
|
-
- HY-135774
-
|
Drug Metabolite
Phosphatase
|
Cardiovascular Disease
|
6-Hydroxybenzbromarone is the major metabolite of Benzbromarone with a longer half-life and greater pharmacological potency than the parent compound. 6-Hydroxybenzbromarone is a protein Eyes Absent 3 (EYA3) inhibitor with an IC50 value of 21.5 μM. 6-Hydroxybenzbromarone is an anti-angiogenic agent, has strong inhibitory effects on cell migration, tubulogenesis, and angiogenic sprouting .
|
-
- HY-135810A
-
Desethylhydroxychloroquine oxalate
|
Influenza Virus
Parasite
|
Infection
Inflammation/Immunology
|
Cletoquine oxalate (Desethylhydroxychloroquine oxalate) is a major active metabolite of Hydroxychloroquine. Cletoquine oxalate is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine oxalate is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine oxalate has antimalarial effects and has the potential for autoimmune diseases treatment .
|
-
- HY-123349
-
|
Drug Metabolite
|
Cardiovascular Disease
|
5α-Hydroxy-6-keto cholesterol is major metabolite of β-epoxide (5α,6β-epoxycholesterol) during direct exposure of intact cultured human bronchial epithelial cells (16-HBE) to ozone. 5α-Hydroxy-6-keto cholesterol inhibits cholesterol synthesis with an IC50 of 350 nM .
|
-
- HY-125296R
-
|
GABA Receptor
|
Neurological Disease
|
Fipronil sulfone (Standard) is the analytical standard of Fipronil sulfone. This product is intended for research and analytical applications. Fipronil sulfone is the major metabolite of Fipronil.Fipronil sulfone selectively inhibits GABA receptor with IC50 of 175 nM (assayed by displacement of 4′-ethynyl-4-n-[2,3-3H2]- propylbicycloorthobenzoate ([3H]EBOB) from the noncompetitive blocker site).
|
-
- HY-A0019S
-
|
Dopamine Receptor
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
Paliperidone-d4 is the deuterium labeled Paliperidone. Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia[1].
|
-
- HY-N6720
-
|
Endogenous Metabolite
|
Metabolic Disease
|
T-2 Triol is a trichothecene mycotoxin derived by the metabolism of T-2 toxin. It is less toxic than T-2 toxin . T-2 Triol major metabolites are evaluated in broiler chickens with Half-lives (t1/2λz), Peak plasma concentrations (Cmax) and Tmax values of 9.6 mins, 563 ng/ml , 2.5 mins, respectively .
|
-
- HY-135810S
-
Desethylhydroxychloroquine-d4
|
Isotope-Labeled Compounds
Influenza Virus
Parasite
|
Infection
Inflammation/Immunology
|
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].
|
-
- HY-A0252A
-
|
Others
|
Cancer
|
Bupranolol hydrochloride is a non-selective β-adrenergic blocker with potent membrane stabilizing activity. Bupranolol hydrochloride is able to significantly modulate the contractile activity of the non-pregnant human uterus. Bupranolol hydrochloride showed significant effects on spontaneous uterine contractions in an in vitro study in patients with ovarian cancer. Bupranolol hydrochloride is similar in potency to propranolol, another β-adrenergic blocker. Bupranolol hydrochloride is rapidly and completely absorbed in vivo, and its major metabolite is carboxybupranolol .
|
-
- HY-A0019R
-
|
Drug Metabolite
Dopamine Receptor
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
Paliperidone (Standard) is the analytical standard of Paliperidone. This product is intended for research and analytical applications. Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia .
|
-
- HY-N0407
-
6'-Cinnamoylcatalpol
|
STAT
|
Inflammation/Immunology
|
Picroside I is the major ingredient of Picrorhiza scrophulariiflora. Picrorhiza scrophulariiflora is a high value medicinal herb due to rich source of hepatoprotective metabolites, Picroside-I and Picroside-II . Picroside I is a promising agent for the management of asthma. Picroside I reduces the inflammation significantly at its higher dose. Picroside I also downregulates pSTAT6 and GATA3 expressions. Picroside I dose-dependently increases the serum levels of IFN-γ .
|
-
- HY-135810S1
-
Desethylhydroxychloroquine-d4-1
|
Isotope-Labeled Compounds
Influenza Virus
Parasite
|
Infection
Inflammation/Immunology
|
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].
|
-
- HY-17366
-
|
mAChR
Dopamine Receptor
Drug Metabolite
|
Neurological Disease
|
Clozapine N-oxide is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide can cross the blood-brain barrier . Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist .
|
-
- HY-17366A
-
|
mAChR
Dopamine Receptor
Drug Metabolite
|
Neurological Disease
|
Clozapine N-oxide dihydrochloride is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide dihydrochloride activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide dihydrochloride can cross the blood-brain barrier . Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist .
|
-
- HY-B0602S2
-
|
Isotope-Labeled Compounds
Serotonin Transporter
|
Neurological Disease
|
Desvenlafaxine-d6 is deuterium labeled Desvenlafaxine. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter[1][2].
|
-
- HY-B0602S3
-
|
Isotope-Labeled Compounds
Serotonin Transporter
|
Neurological Disease
|
Desvenlafaxine-d10 is deuterium labeled Desvenlafaxine. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter[1][2].
|
-
- HY-76569R
-
|
mAChR
|
Neurological Disease
|
Desfesoterodine (Standard) is the analytical standard of Desfesoterodine. This product is intended for research and analytical applications. 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) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
|
-
- HY-32343
-
(24R)-24,25-Dihydroxyvitamin D3
|
Endogenous Metabolite
VD/VDR
|
Metabolic Disease
Inflammation/Immunology
|
Secalciferol ((24R)-24,25-Dihydroxyvitamin D3) is the major active metabolite of Vitamin D. Secalciferol activates vitamin D receptor (VDR) with an EC50 value of 150 nM. Secalciferol is involved in a wide range of biological functions such as calcium homeostasis, cellular differentiation and proliferation processes, as well as other functions related to the immune system, which is promising for research of rickets, osteomalacia, hypercalcemia and autoimmune disorders .
|
-
- HY-G0021S
-
Norclozapine-d8; Desmethylclozapine-d8; Normethylclozapine-d8
|
mAChR
Opioid Receptor
Drug Metabolite
Virus Protease
|
Infection
|
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].
|
-
- HY-G0021S1
-
Norclozapine-d8 hydrochloride; Desmethylclozapine-d8 hydrochloride; Normethylclozapine-d8 hydrochloride
|
mAChR
Opioid Receptor
Drug Metabolite
Virus Protease
|
Infection
|
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].
|
-
- HY-W018392S
-
MEHP-d4; Phthalic acid mono-2-ethylhexyl ester-d4
|
Isotope-Labeled Compounds
|
Metabolic Disease
|
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) .
|
-
- HY-76569S1
-
PNU-200577-d14; 5-Hydroxymethyl Tolterodine-d14
|
mAChR
Isotope-Labeled Compounds
|
Neurological Disease
|
(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) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
|
-
- HY-W018392R
-
|
Endogenous Metabolite
|
Metabolic Disease
|
Mono-(2-ethylhexyl) phthalate (Standard) is the analytical standard of Mono-(2-ethylhexyl) phthalate. This product is intended for research and analytical applications. 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) .
|
-
- HY-Y0469R
-
|
Drug Metabolite
|
Others
|
1-Aminohydantoin (hydrochloride) (Standard) is the analytical standard of 1-Aminohydantoin (hydrochloride). This product is intended for research and analytical applications. 1-Aminohydantoin hydrochloride is a major metabolite of nitrofurantoin in animal tissues and can be used as a standard for the determination of residues of veterinary agents in meat, milk et.al. 1-Aminohydantoin hydrochloride covalently binds to tissue proteins and is released from the tissues under slightly acidic conditions and derivatized with 2-nitrobenzaldehyde to form nitrophenyl derivatives of AHD before detection .
|
-
- HY-N6660
-
Tricaprin; Glyceryl tridecanoate
|
Endogenous Metabolite
Androgen Receptor
|
Cardiovascular Disease
Metabolic Disease
|
Trisdecanoin (Tricaprin; Glyceryl tridecanoate) is an orally available precursor of decanoic acid (DA precursor) that can be hydrolyzed to decanoic acid. Trisdecanoin and its metabolite capric acid not only provide the body with a quick source of energy, but can also affect lipid metabolism. Trisdecanoin is a major component of medium chain triglycerides (MCT), which has preventive or inhibitory properties for abdominal aortic aneurysms (AAA), inhibition of cardiovascular disease, and anti-androgen (NSAA) and anti-hyperglycemic properties. Trisdecanoin can be used as an additive in food, medicine and cosmetics .
|
-
- HY-135334S
-
|
Isotope-Labeled Compounds
Drug Metabolite
Btk
Cytochrome P450
|
Cancer
|
ACP-5862-d4 is deuterium labeled ACP-5862. ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC50 of 5.0 nM for Bruton tyrosine kinase (BTK). ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM[1][2].
|
-
- HY-D0004R
-
|
Monoamine Oxidase
|
Neurological Disease
|
Azure B (Standard) is the analytical standard of Azure B. This product is intended for research and analytical applications. Azure B is a cationic dye and the major metabolite of Methylene blue. Azure B is used in making Azure eosin stains for blood smear staining. Azure B is a high-potency, selective and reversible inhibitor of monoamine oxidases (MAO)-A, with IC50s of 11 and 968 nM for recombinant human MAO-A and MAO-B, respectively. Azure B possesses significant antidepressant-like effects .
|
-
- HY-16940
-
24S-OHC; 24S-HC; Cerebrosterol
|
LXR
iGluR
Endogenous Metabolite
|
Metabolic Disease
|
24(S)-Hydroxycholesterol (24S-OHC), the major brain cholesterol metabolite, plays an important role to maintain homeostasis of cholesterol in the brain. 24(S)-Hydroxycholesterol (24S-OHC) is one of the most efficient endogenous LXR agonist known and is present in the brain and in the circulation at relatively high levels. 24(S)-Hydroxycholesterol (24S-OHC) is a very potent, direct, and selective positive allosteric modulator of NMDARs with a mechanism that does not overlapthat of other allosteric modulators .
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-
- HY-137522S
-
3'-Azido-3'-deoxythymidine β-D-glucuronide-d3 sodium
|
Isotope-Labeled Compounds
|
Others
|
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 .
|
-
- HY-N0407R
-
|
STAT
|
Inflammation/Immunology
|
Picroside I (Standard) is the analytical standard of Picroside I. This product is intended for research and analytical applications. Picroside I is the major ingredient of Picrorhiza scrophulariiflora. Picrorhiza scrophulariiflora is a high value medicinal herb due to rich source of hepatoprotective metabolites, Picroside-I and Picroside-II . Picroside I is a promising agent for the management of asthma. Picroside I reduces the inflammation significantly at its higher dose. Picroside I also downregulates pSTAT6 and GATA3 expressions. Picroside I dose-dependently increases the serum levels of IFN-γ .
|
-
- HY-137522
-
3'-Azido-3'-deoxythymidine β-D-glucuronide sodium
|
Drug Metabolite
|
Others
|
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 . Zidovudine O-β-D-glucuronide (sodium) is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
- HY-N6660R
-
|
Endogenous Metabolite
Androgen Receptor
|
Metabolic Disease
|
Trisdecanoin (Standard) is the analytical standard of Trisdecanoin. This product is intended for research and analytical applications. Trisdecanoin (Tricaprin; Glyceryl tridecanoate) is an orally available precursor of decanoic acid (DA precursor) that can be hydrolyzed to decanoic acid. Trisdecanoin and its metabolite capric acid not only provide the body with a quick source of energy, but can also affect lipid metabolism. Trisdecanoin is a major component of medium chain triglycerides (MCT), which has preventive or inhibitory properties for abdominal aortic aneurysms (AAA), inhibition of cardiovascular disease, and anti-androgen (NSAA) and anti-hyperglycemic properties. Trisdecanoin can be used as an additive in food, medicine and cosmetics .
|
-
- HY-135541
-
YM150 maleate
|
Others
|
Cardiovascular Disease
|
Darexaban maleate (YM150 maleate) is a direct factor Xa inhibitor with activity in preventing venous thromboembolism. The major metabolite of Darexaban maleate in humans is Darexaban glucitol, which acts pharmacologically. The glucitolation reaction of Darexaban maleate is mainly catalyzed by UGT1A9 and UGT1A10 in the human liver and intestine. The K(m) value of Darexaban maleate glucitolation in the liver is greater than 250 μM, while in the intestine it exhibits substrate inhibition kinetics with a K(m) value of 27.3 μM. The unbound K(m) value of Darexaban maleate is significantly reduced by the influence of fatty acid-free bovine serum albumin in both HLM and UGT1A9 .
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-
- HY-148682
-
Glycyrrhetic acid 3-O-hydrogen sulfate
|
OAT
11β-HSD
Drug Metabolite
|
Metabolic Disease
Inflammation/Immunology
|
18β-Glycyrrhetyl-3-O-sulfate (Glycyrrhetic acid 3-O-(hydrogen sulfate)) is a potent type 2 11β-hydroxysteroid dehydrogenase (11β-HSD2) inhibitor with an IC50 of 0.10 µM using rat kidney microsome. 18β-Glycyrrhetyl-3-O-sulfate is the major metabolite of Glycyrrhetinic acid (GA). 18β-Glycyrrhetyl-3-O-sulfate is the substrate of organic anion transporter (OAT) 1 and OAT3. 18β-Glycyrrhetyl-3-O-sulfate has anti-inflammatory effects and has the potential for pseudohyperaldosteronism research .
|
-
- HY-N1902R
-
|
Keap1-Nrf2
Endogenous Metabolite
|
Metabolic Disease
|
4-Hydroxyphenylacetic acid (Standard) is the analytical standard of 4-Hydroxyphenylacetic acid. This product is intended for research and analytical applications. 4-hydroxyphenylacetic acid, a major microbiota-derived metabolite of polyphenols, is involved in the antioxidative action. 4-hydroxyphenylacetic acid induces expression of Nrf2 .
IC50 & Target:Nrf2
In Vivo: 4-Hydroxyphenylacetic acid (6, 12, or 25 mg/kg) increases Nrf2 translocation to the nucleus and enhances the activity of phase II and antioxidant enzymes. The protein levels of nuclear Nrf2 are increased by 170% and 230% in pre-treated 12 and 25 mg/kg 4-Hydroxyphenylacetic acid groups, respectively, compared with the control group.The 4-Hydroxyphenylacetic acid pretreatment at a final dose of 25 mg/kg markedly and selectively up-regulated the target genes of phase II enzymes and resulted in higher up-regulation than that of the control group by 270%, 400%, and 500% or UGT1A1, UGT1A9, and SULT2A1, respectively. 4-Hydroxyphenylacetic acid also suppresses the expression of CYP2E1 .
|
-
Cat. No. |
Product Name |
Type |
-
- HY-D0300
-
|
Dyes
|
Leucomalachite green is a triphenylmethane dye used to detect blood. Leucomalachite green, a major metabolite of malachite green, is a potential carcinogen, teratogen and mutagen .
|
-
- HY-D0004
-
Azure B chloride
|
Dyes
|
Azure B is a cationic dye and the major metabolite of Methylene blue. Azure B is used in making Azure eosin stains for blood smear staining. Azure B is a high-potency, selective and reversible inhibitor of monoamine oxidases (MAO)-A, with IC50s of 11 and 968 nM for recombinant human MAO-A and MAO-B, respectively. Azure B possesses significant antidepressant-like effects .
|
-
- HY-D0300R
-
|
Dyes
|
Leucomalachite green (Standard) is the analytical standard of Leucomalachite green. This product is intended for research and analytical applications. Leucomalachite green is a triphenylmethane dye used to detect blood. Leucomalachite green, a major metabolite of malachite green, is a potential carcinogen, teratogen and mutagen .
|
-
- HY-D0004R
-
|
Dyes
|
Azure B (Standard) is the analytical standard of Azure B. This product is intended for research and analytical applications. Azure B is a cationic dye and the major metabolite of Methylene blue. Azure B is used in making Azure eosin stains for blood smear staining. Azure B is a high-potency, selective and reversible inhibitor of monoamine oxidases (MAO)-A, with IC50s of 11 and 968 nM for recombinant human MAO-A and MAO-B, respectively. Azure B possesses significant antidepressant-like effects .
|
Cat. No. |
Product Name |
Type |
-
- HY-W264038
-
p-Fluorohippuric acid; YM-385461
|
Biochemical Assay Reagents
|
4-Fluorohippuric acid is a major metabolite of flupirtine with research potential against pain and epilepsy .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1488
-
-
- HY-P1141
-
|
GCGR
|
Metabolic Disease
|
GLP-1(9-36)amide is a major metabolite of glucagon-like peptide-1-(7-36) amide formed by the enzyme dipeptidyl peptidase-4 (DPP-4). GLP-1(9-36)amide acts as an antagonist to the human pancreatic GLP-1 receptor .
|
-
- HY-P1141A
-
|
GCGR
|
Metabolic Disease
|
GLP-1(9-36)amide TFA is a major metabolite of glucagon-like peptide-1-(7-36) amide formed by the enzyme dipeptidyl peptidase-4 (DPP-4). GLP-1(9-36)amide TFA acts as an antagonist to the human pancreatic GLP-1 receptor .
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-
- HY-P2643
-
-
- HY-P3100
-
|
Parasite
|
Infection
|
Orfamide A is a major metabolite of insecticidal biosurfactant in Pseudomonas sp. F6 and has aphidicidal activity. Orfamide A can be used for aphid control in organic agriculture. Orfamide A exhibits dose-dependent mortality against aphids with an LC50 value of 34.5 μg/mL .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99469
-
PB 2452; MEDI 2452
|
Inhibitory Antibodies
|
Metabolic Disease
|
Bentracimab (PB 2452) is a neutralizing monoclonal antibody that binds Ticagrelor (HY-1006) and its major active circulating metabolite with high affinity. Bentracimab can rapidly reverse the antiplatelet effect of Ticagrelor .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
- HY-16940
-
-
- HY-N0407R
-
|
Structural Classification
Iridoids
Terpenoids
Source classification
Scrophulariaceae
Plants
Picrorhiza scrophulariiflora Pennell
|
STAT
|
Picroside I (Standard) is the analytical standard of Picroside I. This product is intended for research and analytical applications. Picroside I is the major ingredient of Picrorhiza scrophulariiflora. Picrorhiza scrophulariiflora is a high value medicinal herb due to rich source of hepatoprotective metabolites, Picroside-I and Picroside-II . Picroside I is a promising agent for the management of asthma. Picroside I reduces the inflammation significantly at its higher dose. Picroside I also downregulates pSTAT6 and GATA3 expressions. Picroside I dose-dependently increases the serum levels of IFN-γ .
|
-
- HY-N6660R
-
|
Ketones, Aldehydes, Acids
Source classification
umbellularia californica
Plants
Lauraceae
|
Endogenous Metabolite
Androgen Receptor
|
Trisdecanoin (Standard) is the analytical standard of Trisdecanoin. This product is intended for research and analytical applications. Trisdecanoin (Tricaprin; Glyceryl tridecanoate) is an orally available precursor of decanoic acid (DA precursor) that can be hydrolyzed to decanoic acid. Trisdecanoin and its metabolite capric acid not only provide the body with a quick source of energy, but can also affect lipid metabolism. Trisdecanoin is a major component of medium chain triglycerides (MCT), which has preventive or inhibitory properties for abdominal aortic aneurysms (AAA), inhibition of cardiovascular disease, and anti-androgen (NSAA) and anti-hyperglycemic properties. Trisdecanoin can be used as an additive in food, medicine and cosmetics .
|
-
- HY-N1902R
-
|
Structural Classification
Human Gut Microbiota Metabolites
Monophenols
Source classification
Phenols
Plants
Compositae
Endogenous metabolite
Erythrina latissima E. Mey.
|
Keap1-Nrf2
Endogenous Metabolite
|
4-Hydroxyphenylacetic acid (Standard) is the analytical standard of 4-Hydroxyphenylacetic acid. This product is intended for research and analytical applications. 4-hydroxyphenylacetic acid, a major microbiota-derived metabolite of polyphenols, is involved in the antioxidative action. 4-hydroxyphenylacetic acid induces expression of Nrf2 .
IC50 & Target:Nrf2
In Vivo: 4-Hydroxyphenylacetic acid (6, 12, or 25 mg/kg) increases Nrf2 translocation to the nucleus and enhances the activity of phase II and antioxidant enzymes. The protein levels of nuclear Nrf2 are increased by 170% and 230% in pre-treated 12 and 25 mg/kg 4-Hydroxyphenylacetic acid groups, respectively, compared with the control group.The 4-Hydroxyphenylacetic acid pretreatment at a final dose of 25 mg/kg markedly and selectively up-regulated the target genes of phase II enzymes and resulted in higher up-regulation than that of the control group by 270%, 400%, and 500% or UGT1A1, UGT1A9, and SULT2A1, respectively. 4-Hydroxyphenylacetic acid also suppresses the expression of CYP2E1 .
|
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-103005S
-
|
Ramelteon metabolite M-II-d3 is the deuterium labeled Ramelteon metabolite M-II. Ramelteon metabolite M-II is the major metabolite of Ramelteon, with IC50s of 208 pM, 1470 pM for human melatonin receptors (MT1 or MT2). Ramelteon is a selective melatonin agonist[1][2].
|
-
-
- HY-132675S
-
|
Prochlorperazine Sulfoxide-d3 is a deuterium labeled Prochlorperazine Sulfoxide. Prochlorperazine Sulfoxide is the major metabolite of the antiemetic Prochlorperazine[1][2].
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-
-
- HY-13332
-
|
Calcifediol-d6 is the deuterium labeled Calcifediol. Calcifediol, a major circulating metabolite of vitamin D3, is a potent VDR ligand .
|
-
-
- HY-N7143S
-
|
Monobutyl phthalate-d4 is the deuterium labeled Monobutyl phthalate[1]. Monobutyl phthalate, a major metabolite of dibutyl phthalate (DBP), possesses antiandrogenic effects. Monobutyl phthalate is an embryotoxicant[2][3].
|
-
-
- HY-100635S
-
|
Diacetolol-d7 is a deuterium labeled Diacetolol. Diacetolol is the major metabolite of Acebutolol. Diacetolol is a β-adrenoceptor blocking and anti-arrhythmic agent[1].
|
-
-
- HY-107850S
-
|
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].
|
-
-
- HY-137532S
-
|
7-Hydroxy Quetiapine-d8 is the deuterium labeled 7-Hydroxyquetiapine. 7-Hydroxyquetiapine (ICI 214227) is the major active metabolite of antipsychotic medicine Quetiapine[1].
|
-
-
- HY-100662S
-
|
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].
|
-
-
- HY-137532S1
-
|
7-Hydroxyquetiapine-d4 (hemifumarate) is deuterium labeled 7-Hydroxyquetiapine. 7-Hydroxyquetiapine (ICI 214227) is the major active metabolite of antipsychotic medicine Quetiapine[1].
|
-
-
- HY-D0300S
-
|
Leucomalachite green-d5 is the deuterium labeled Leucomalachite green. Leucomalachite green is a triphenylmethane dye used to detect blood. Leucomalachite green, a major metabolite of malachite green, is a potential carcinogen, teratogen and mutagen[1][2].
|
-
-
- HY-12753S1
-
|
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].
|
-
-
- HY-12753S
-
|
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].
|
-
-
- HY-W040047S
-
|
Pregnanediol 3-glucuronide- 13C5 is 13C-labeled Pregnanediol (HY-107850) Pregnanediol is the major metabolite of progesterone and can be excreted via urine. Pregnanediol offers an indirect way to measure progesterone levels in vivo.
|
-
-
- HY-135811S
-
|
Desethyl chloroquine-d4 is the deuterium labeled Desethyl chloroquine. Desethyl chloroquine is a major desethyl metabolite of Chloroquine. Chloroquine diphosphate is an inhibitor of autophagy and toll-like receptors (TLRs). Desethyl chloroquine possesses antiplasmodic activity[1][2].
|
-
-
- HY-135811S1
-
|
Desethyl chloroquine-d5 is deuterium labeled Desethyl chloroquine. Desethyl chloroquine is a major desethyl metabolite of Chloroquine. Chloroquine diphosphate is an inhibitor of autophagy and toll-like receptors (TLRs). Desethyl chloroquine possesses antiplasmodic activity[1][2].
|
-
-
- HY-I1111S4
-
|
Fmoc-L-Val-OH- 15N is a 15N-labeled Leucomalachite green. Leucomalachite green is a triphenylmethane dye used to detect blood. Leucomalachite green, a major metabolite of malachite green, is a potential carcinogen, teratogen and mutagen[1][2].
|
-
-
- HY-117605S
-
|
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].
|
-
-
- HY-N1902S
-
|
4-Hydroxyphenylacetic acid-d6 is the deuterium labeled 4-Hydroxyphenylacetic acid. 4-hydroxyphenylacetic acid, a major microbiota-derived metabolite of polyphenols, is involved in the antioxidative action. 4-hydroxyphenylacetic acid induces expression of Nrf2[1].
|
-
-
- HY-124265S2
-
|
4β-Hydroxycholesterol-d4 is the deuterium labeled 4β-Hydroxycholesterol. 4β-hydroxy Cholesterol is a major oxysterol cholesterol metabolite and a precursor in the synthesis of bile acids that is found in human circulation[1][2].
|
-
-
- HY-B2150S
-
|
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].
|
-
-
- HY-19657S
-
|
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 .
|
-
-
- HY-130353S
-
|
Desethyl Amiodarone-d4 (hydrochloride) is the deuterium labeled Desethylamiodarone hydrochloride. Desethylamiodarone hydrochloride (N-desethylamiodarone hydrochloride) is a major active metabolite of Amiodarone. Desethylamiodarone hydrochloride is formed by CYP3A isoenzymes. Amiodarone is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM[1][2][3].
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-
-
- HY-124265S1
-
|
4β-Hydroxycholesterol-d5 is the deuterium labeled 4β-Hydroxycholesterol (HY-124265). 4β-hydroxy Cholesterol is a major oxysterol cholesterol metabolite and a precursor in the synthesis of bile acids that is found in human circulation[1][2].
|
-
-
- HY-15895S
-
|
Aprocitentan-d4 is a deuterium labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively[1].
|
-
-
- HY-N1902S1
-
|
4-Hydroxyphenylacetic acid-d4 is the deuterium labeled 4-Hydroxyphenylacetic acid[1]. 4-hydroxyphenylacetic acid, a major microbiota-derived metabolite of polyphenols, is involved in the antioxidative action. 4-hydroxyphenylacetic acid induces expression of Nrf2[2].
|
-
-
- HY-B1986S
-
|
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].
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-
-
- HY-B0539S
-
|
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].
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-
-
- HY-B0539S1
-
|
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].
|
-
-
- HY-Z0548S1
-
|
Methyl 3,4-dihydroxybenzoate-d3-1 is the deuterium labeled Methyl 3,4-dihydroxybenzoate. Methyl 3,4-dihydroxybenzoate (Protocatechuic acid methyl ester; Methyl protocatechuate) is a major metabolite of antioxidant polyphenols found in green tea. Antioxidant and anti-inflammatory effect[1].
|
-
-
- HY-B0539S3
-
|
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].
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-
-
- HY-130569S
-
|
7-Hydroxymethotrexate-d3 (sodium) is deuterium labeled 7-Hydroxymethotrexate. 7-Hydroxymethotrexate is a major metabolite of Methotrexate (MTX; HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis[1][2].
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-
-
- HY-130569S1
-
|
7-Hydroxymethotrexate-d3 is the deuterium labeled 7-Hydroxymethotrexate. 7-Hydroxymethotrexate is a major metabolite of Methotrexate (MTX; HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis[1][2].
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-
-
- HY-128554S
-
|
N-Desethyl amodiaquine-d5 is the deuterium labeled N-Desethyl amodiaquine. N-Desethyl amodiaquine is the major biologically active metabolite of Amodiaquine. N-Desethyl amodiaquine is an antiparasitic agent. IC50 values for strains V1/S and 3D7 are 97 nM and 25 nM, respectively[1].
|
-
-
- HY-128554S1
-
|
N-Desethyl amodiaquine-d5 (dihydrochloride) is the deuterium labeled N-Desethyl amodiaquine dihydrochloride. N-Desethyl amodiaquine dihydrochloride is the major biologically active metabolite of Amodiaquine. N-Desethyl amodiaquine dihydrochloride is an antiparasitic agent. IC50 values for strains V1/S and 3D7 are 97 nM and 25 nM, respectively[1].
|
-
-
- HY-130569S2
-
|
7-Hydroxymethotrexate-d3 (ammonium) is the deuterium labeled 7-Hydroxymethotrexate ammonium. 7-Hydroxymethotrexate is a major metabolite of Methotrexate (MTX; HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis[1][2].
|
-
-
- HY-B1984S
-
|
p,p'-DDD-d8 is the deuterium labeled p,p'-DDD[1]. 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[2][3].
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-
-
- HY-B0539S4
-
|
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 .
|
-
-
- HY-B0539S2
-
|
Desloratadine-3,3,5,5-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].
|
-
-
- HY-A0019S
-
|
Paliperidone-d4 is the deuterium labeled Paliperidone. Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia[1].
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-
-
- HY-135810S
-
|
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].
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-
-
- HY-135810S1
-
|
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].
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-
-
- HY-B0602S2
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Desvenlafaxine-d6 is deuterium labeled Desvenlafaxine. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter[1][2].
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- HY-B0602S3
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Desvenlafaxine-d10 is deuterium labeled Desvenlafaxine. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter[1][2].
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- HY-G0021S
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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].
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- HY-G0021S1
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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].
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- HY-W018392S
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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) .
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- HY-76569S1
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(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) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
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- HY-135334S
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ACP-5862-d4 is deuterium labeled ACP-5862. ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC50 of 5.0 nM for Bruton tyrosine kinase (BTK). ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM[1][2].
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- HY-137522S
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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 .
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- HY-137522
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3'-Azido-3'-deoxythymidine β-D-glucuronide sodium
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Azide
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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 . Zidovudine O-β-D-glucuronide (sodium) is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-17639
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RX-10045
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Alkynes
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Navamepent is an analog of naturally occurring resolvin E1 (a major dietary omega-3 polyunsaturated fatty-acid metabolite) with potent anti-inflammatory and cell survival benefits. Navamepent is highly effective against dry eye and goblet cell loss thereby accelerating tear production. Also, Navamepent can reduce corneal inflammation, epithelial damage, and accelerate corneal tissue repair. In addition, Navamepent can inhibit the release of several key proinflammatory mediators from corneal epithelial cells. Navamepent is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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