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39

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7

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2

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B1017
    Molindone hydrochloride

    EN-1733A

    		 Dopamine Receptor Neurological Disease
    Molindone hydrochloride (EN-1733A) is a therapeutic antipsychotic, used in the treatment of schizophrenia, works by blocking the effects of dopamine in the brain, leading to diminished psychoses.
    Molindone hydrochloride
  • HY-B0530
    Azacyclonol
    1 Publications Verification

    γ-pipradol

    		 Histamine Receptor Neurological Disease
    Azacyclonol (γ-pipradol), a metabolite of Terfenadine, is a central depressant agent. Azacyclonol is a ganglion-blocking agent. Azacyclonol can be used to diminish psychoses-induced hallucinations .
    Azacyclonol
  • HY-19988
    THZ1-R
    3 Publications Verification

    		 CDK Cancer
    THZ1-R is a non-cysteine reactive analog of THZ1 which displays diminished activity for CDK7 inhibition. THZ1-R binds to CDK7 with a Kd of 142 nM.
    THZ1-R
  • HY-107434S
    Molindone-d8

    (±)-Molindone-d8; SPN-810M-d8

    		 Isotope-Labeled Compounds Dopamine Receptor Neurological Disease
    Molindone-d8 is the deuterium labeled Molindone. Molindone hydrochloride (EN-1733A) is a therapeutic antipsychotic, used in the treatment of schizophrenia, works by blocking the effects of dopamine in the brain, leading to diminished psychoses[1][2].
    Molindone-d8
  • HY-14886
    Fasitibant chloride

    MEN16132 free base

    		 Bradykinin Receptor Cardiovascular Disease Neurological Disease
    Fasitibant chloride (MEN16132 free base) is a potent and selective nonpeptide bradykinin B2 receptor (B2R) antagonist. Fasitibant chloride reduces joint pain and diminishes joint oedema in Carrageenan-induced arthritis rat model .
    Fasitibant chloride
  • HY-P5265
    Tetrapeptide

    		DNA/RNA Synthesis Metabolic Disease
    Tetrapeptide, an analogue of α-MSH, induces melanin synthesis. Tetrapeptide diminishes DNA damage by reducing the production of reactive oxidative species and enhancing repair of DNA photoproducts .
    Tetrapeptide
  • HY-120865
    1,3-PBIT dihydrobromide

    		NO Synthase Inflammation/Immunology
    1,3-PBIT is a potent inhibitor of iNOS with a Ki of 47 nM compared to Ki values for eNOS and nNOS are 9 and 0.25 μM, respectively, for the purified human enzymes. Its inhibition in whole cells is greatly diminished, presumably to poor membrane permeability.
    1,3-PBIT dihydrobromide
  • HY-116408
    Propiverine

    		mAChR Neurological Disease
    Propiverine is a potent antimuscarinic agent. Propiverine inhibits cellular calcium influx, thereby diminishing muscle spasm. Propiverine has neurotropic and musculotropic effects on the urinary bladder smooth muscle. Propiverine can used for overactive bladder (OAB) research .
    Propiverine
  • HY-B0530R
    Azacyclonol (Standard)

    		Histamine Receptor Neurological Disease
    Azacyclonol (Standard) is the analytical standard of Azacyclonol. This product is intended for research and analytical applications. Azacyclonol (γ-pipradol), a metabolite of Terfenadine, is a central depressant agent. Azacyclonol is a ganglion-blocking agent. Azacyclonol can be used to diminish psychoses-induced hallucinations .
    Azacyclonol (Standard)
  • HY-144285
    CXCR4 antagonist 4

    		CXCR HIV Inflammation/Immunology
    CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC50=7 nM) .
    CXCR4 antagonist 4
  • HY-50683S
    JNJ-38877605-d1

    		c-Met/HGFR Cancer
    JNJ-38877605-d1 (compound DO-2) is a highly selective MNNG HOS transforming (MET) inhibitor. JNJ-38877605-d1 is thought to diminish the formation of the Aldehyde Oxidase 1 inactive metabolite M3 .
    JNJ-38877605-d1
  • HY-108022
    Azemiglitazone

    MSDC-0602

    		 Mitochondrial Metabolism PPAR Neurological Disease Metabolic Disease Inflammation/Immunology
    Azemiglitazone (MSDC-0602) is an orally active thiazolidinedione (TZD) -like molecule, which binds to PPARγ with low binding and activating affinity. Azemiglitazone inhibits mitochondrial pyruvate carrier (MPC), which inhibits Alzheimer’s disease and diminishes nonalcoholic steatohepatitis (NASH) caused liver injury .
    Azemiglitazone
  • HY-12532
    Astemizole
    5 Publications Verification

    R 43512

    		 Histamine Receptor Potassium Channel Inflammation/Immunology Endocrinology
    Astemizole (R 43512), a second-generation antihistamine agent to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC50 of 4 nM. Astemizole also shows potent hERG K + channel blocking activity with an IC50 of 0.9 nM. Astemizole has antipruritic effects .
    Astemizole
  • HY-18638
    TCID
    2 Publications Verification

    4,5,6,7-Tetrachloroindan-1,3-dione

    		 Deubiquitinase Neurological Disease
    TCID (4,5,6,7-Tetrachloroindan-1,3-dione) is a potent and selective neuronal ubiquitin C-terminal hydrolase (UCH-L3) inhibitor with an IC50 of 0.6 μM . TCID diminishes glycine transporter GlyT2 ubiquitination in brainstem and spinal cord primary neurons .
    TCID
  • HY-157416
    COP1-ATGL modulator 1

    		Others Metabolic Disease
    COP1-ATGL modulator 1 (86) is an orally active modulator for COP1-ATGL axis. COP1-ATGL modulator 1 (86) could increase ATGL protein expression, reduce ATGL ubiquitination and COP1 autoubiquitination, and diminish lipid accumulation in hepatocytes in the nanomolar range .
    COP1-ATGL modulator 1
  • HY-162946
    Alkyne-P60

    		Ligands for Target Protein for PROTAC Cancer
    Alkyne-P60 is a potent 15-mer peptide inhibitor of Foxp3. Alkyne-P60 can bind with Foxp3, hinder its nuclear translocation, and diminish Foxp3-mediated inhibition of NFKB and NFAT functions. Alkyne-P60 is a ligand for target protein for PROTAC (HY-162943).
    Alkyne-P60
  • HY-126020
    Bractoppin
    2 Publications Verification

    		 DNA/RNA Synthesis RAD51 Cancer
    Bractoppin is a potent and selective agent-like inhibitor of phosphopeptide recognition by the human BRCA1 tandem(t) BRCT domain (binding IC50: 74 nM). Bractoppin diminishes BRCA1 recruitment to DNA breaks, in turn suppressing damage-induced G2 arrest and assembly of the recombinase, RAD51. Bractoppin preferentially inhibits BRCA1 tBRCT-dependent steps in the DNA damage response .
    Bractoppin
  • HY-107426
    Verrucarin A

    Muconomycin A

    		 Apoptosis Reactive Oxygen Species Cancer
    Verrucarin A (Muconomycin A), a Type D macrocyclic mycotoxin derived from the pathogen fungus Myrothecium verrucaria, is an inhibitor of protein synthesis. Verrucarin A inhibits growth of leukemia cell lines and activates caspases and apoptosis and inflammatory signaling in macrophages. Verrucarin A effectively increased the phosphorylation of p38 MAPK and diminished the phosphorylation of ERK/Akt. Verrucarin A caused cell cycle deregulation through the induction of p21 and p53 .
    Verrucarin A
  • HY-12532R
    Astemizole (Standard)

    		Histamine Receptor Potassium Channel Inflammation/Immunology Endocrinology
    Astemizole (Standard) is the analytical standard of Astemizole. This product is intended for research and analytical applications. Astemizole (R 43512), a second-generation antihistamine agent to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC50 of 4 nM. Astemizole also shows potent hERG K + channel blocking activity with an IC50 of 0.9 nM. Astemizole has antipruritic effects .
    Astemizole (Standard)
  • HY-124704
    Chst15-IN-1

    		Others Neurological Disease
    Chst15-IN-1 is a potent reversible covalent Chst15 inhibitor. Chst15-IN-1 effectively inhibits chondroitin sulfate-E (CS-E) sulfation levels and other closely related glycosaminoglycans (GAG) sulfotransferases. Chst15-IN-1, as a selective sulfotransferase inhibitor, can diminish the inhibitory effects of chondroitin sulfate proteoglycans (CSPGs), and can be used for the stimulation of neuronal repair .
    Chst15-IN-1
  • HY-146097
    RMS5

    		P-glycoprotein Apoptosis Cancer
    RMS5, a tetrandrine analogue, is a potent P-glycoprotein (P-gp) inhibitor. RMS5 has markedly antiproliferative and cytotoxic effects on cancer cells. RMS5 slightly diminishes the expression of the anti-apoptotic Bcl-2 family proteins Bcl-XL and Mcl-1. RMS3 causes PARP cleavage, a marker for cells undergoing apoptosis. RMS5 has strong anticancer property .
    RMS5
  • HY-110143
    CLP257

    		Potassium Channel Neurological Disease
    CLP257 is a selective K +-Cl ? cotransporter KCC2 activator with an EC50 of 616 nM. CLP257 is inactive against NKCC1, GABAA receptors, KCC1, KCC3 or KCC4. CLP257 restores impaired Cl ? transport in neurons with diminished KCC2 activity. CLP257 alleviates hypersensitivity in rats with neuropathic pain. CLP257 modulates plasmalemmal KCC2 protein turnover post-translationally .
    CLP257
  • HY-144075
    JAK-IN-19

    		JAK Inflammation/Immunology
    JAK-IN-19 is a potent JAK inhibitor (PBMC IFNγ pIC50=7.2 and HLF Eotaxin pIC50=7.7). JAK-IN-19 has good retentive properties in the lung via mitigating being metabolized by Aldehyde Oxidase (AO), with diminished VEGFR2 selectivity (VEGFR2 pIC50=7.0, Aurora B pIC50=5.8) .
    JAK-IN-19
  • HY-110246
    Quin C1

    		Others Inflammation/Immunology
    Quin C1 is a highly specific and potent agonist for formyl peptide receptor 2 (FPR2/ALX). Quin-C1 significantly reduces the neutrophil and lymphocyte counts in BALF, diminishes expression of TNF-α, IL-1β, KC, and TGF-β1, and decreases collagen deposition in lung tissue. Quin C1 has the potential for the research of lung injury .
    Quin C1
  • HY-120349
    LL-Z1640-4

    		p38 MAPK JNK Apoptosis Reactive Oxygen Species Cancer
    LL-Z1640-4 is a potent p38/JNK signaling inhibitor. LL-Z1640-4 significantly diminishes p38 and JNK activation in HCC cells transfected with MLK4 siRNA. LL-Z1640-4 markedly attenuates ROS production induced by MLK4 knockdown. LL-Z1640-4 significantly reduces the apoptotic cells in HCC cells transfected with siMLK4 .
    LL-Z1640-4
  • HY-133121
    WDR5-IN-1

    		Histone Methyltransferase Apoptosis Cancer
    WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines .
    WDR5-IN-1
  • HY-131445A
    SS-RJW100

    		Others Metabolic Disease Inflammation/Immunology
    SS-RJW100 is a enantiomer of RJW100, which is a racemic agonist of nuclear receptor liver receptor homolog 1 (LRH-1) and steroidogenic factor 1 (SF-1). SS-RJW100 promotes recruitment of coregulator protein fragments in vitro, recruits the transcriptional intermediary factor 2 (Tif2) coactivator to LRH-1. SS-RJW100 diminishes LRH-1 allosteric activation networks, shows poor thermal stability .
    SS-RJW100
  • HY-13588A
    Cefsulodin

    SCE-129

    		 Others Others
    Cefsulodin (SCE-129) showed potent activity against Pseudomonas aeruginosa and strains susceptible to penicillin and gentamicin, with effectiveness comparable to that of gentamicin and debendazole. However, its effectiveness was diminished against penicillin-resistant strains of P. aeruginosa, particularly strains that were also resistant to gentamicin. For P. aeruginosa maltofila, SCE-129 showed similar minimum inhibitory concentrations to penicillin, gentamicin, and debendazole. Pseudomonas cepacia strains generally showed moderate resistance to SCE-129 and penicillin, and high resistance to gentamicin and debendazole .
    Cefsulodin
  • HY-123461
    Sul-121 hydrochloride

    		Others Inflammation/Immunology
    Sul-121 hydrochloride is a novel compound with anti-oxidative capacity that effectively inhibits airway inflammation and hyperresponsiveness (AHR) in experimental models of chronic obstructive pulmonary disease (COPD). Sul-121 hydrochloride prevents lipopolysaccharide-induced airway neutrophilia and AHR in a dose-dependent manner. Sul-121 hydrochloride also demonstrates the ability to reduce oxidative stress markers in human airway smooth muscle cells. Sul-121 hydrochloride inhibits nuclear translocation of the NF-κB subunit, p65, thereby diminishing pro-inflammatory cytokine release.
    Sul-121 hydrochloride
  • HY-162606
    MAO-A/B-IN-3

    		Monoamine Oxidase Cholinesterase (ChE) Neurological Disease
    MAO-A/B-IN-3 (Compound 12) stands out as a key dual MAO-AChE inhibitor, displaying excellent multi-target efficacy against MAO-A, MAO-B, and AChE with IC50 values of 67 nM, 29 nM, and 1370 nM respectively. MAO-A/B-IN-3 is adept at altering the A site (hydrophobic ring) and C site (semicarbazone chain) within ketone amine-based MTDLs to bolster the inhibitory potential against MAO-A/B while notably diminishing activity against AChE. MAO-A/B-IN-3 is poised for research applications in the field of neurodegenerative diseases .
    MAO-A/B-IN-3
  • HY-146307
    TrxR-IN-3

    		TrxR Cancer
    TrxR-IN-3 (Compound 2c) is a potent inhibitor of TrxR. TrxR-IN-3 exhibits potent antiproliferative activities against five human cancer cell lines, especially against breast tumor cells. TrxR-IN-3 increases ROS levels and resulted in marked apoptosis by regulating apoptosis-related proteins expressed in the breast cancer cells. TrxR-IN-3 also triggers the formation of autophagosomes and autolysosomes by promoting the expression of LC3-II and Beclin-1 and diminishing the expression of LC3-I and p62 proteins .
    TrxR-IN-3
  • HY-165061
    5(Z),11(Z),14(Z)-Eicosatrienoic acid

    Sciadonic acid

    		 Others Inflammation/Immunology
    5(Z),11(Z),14(Z)-Eicosatrienoic acid (Sciadonic acid), a polyunsaturated fatty acid sourced from maritime pine seed oil, gymnospermae leaves and seeds, and freshwater gastropods, has been shown to reduce high-density lipoprotein and ApoA1 levels in transgenic mice expressing human ApoA1 when included in their diet. In vitro studies indicate that it diminishes cholesterol efflux, and when applied topically in its methyl ester form, it alleviates inflammatory processes, likely by displacing arachidonic acid from phospholipid pools and lowering concentrations of downstream inflammatory mediators such as prostaglandin E2 and leukotrienes.
    5(Z),11(Z),14(Z)-Eicosatrienoic acid
  • HY-15048
    GPI 15427

    		PARP Inflammation/Immunology
    GPI 15427 is a potent inhibitor of the enzyme poly (ADP-ribose) polymerase-1 (PARP-1), which plays a harmful role during inflammation. In a rat model of gut injury and inflammation, including splanchnic artery occlusion (SAO) shock and dinitrobenzene sulfonic acid (DNBS)-induced colitis, GPI 15427 demonstrated strong anti-inflammatory effects. It reduced inflammatory cell infiltration, histological injury, and delayed clinical signs of inflammation. GPI 15427 also diminished the accumulation of poly (ADP-ribose) in the ileum and colon of treated rats. These results suggest GPI 15427 could be useful for treating intestinal ischemia and inflammation .
    GPI 15427
  • HY-16094
    Bethanidine sulfate

    BW 467C60

    		 Adrenergic Receptor Neurological Disease
    Bethanidine sulfate and its ortho-chloro derivative (BW 392C60) are potent adrenergic neurone blockers with sympathomimetic effects similar to bretylium and guanethidine in various animal models, particularly in cats. They inhibit the release of noradrenaline during nerve stimulation and enhance smooth muscle responses to adrenaline and noradrenaline. Bethanidine sulfate increases pressor responses to tyramine, though this effect diminishes with higher doses. Unlike guanethidine, Bethanidine sulfate does not deplete pressor amine content in the iris of cats post-administration. It also briefly inhibits autonomic cholinergic mechanisms and causes temporary neuromuscular paralysis in large doses, contrasting with its prolonged adrenergic neurone blocking effects .
    Bethanidine sulfate
  • HY-121183
    Aprikalim

    RP 52891

    		 Potassium Channel Cardiovascular Disease
    Aprikalim (RP 52891), a potassium channel opener (KCO), activates ATP-sensitive K+ (KATP) channels in guinea pig ventricular myocytes. Using patch-clamp techniques, it was found that aprikalim enhances KATP channel activity more effectively in Mg-NDP solution compared to standard solutions. In Mg-NDP solution, aprikalim reduced the sensitivity of KATP channels to ATP, increasing the concentration of ATP required to inhibit channel activity by half (K1) from 56 μM to 180 μM. However, this effect diminished over time. Aprikalim's ability to activate KATP channels in Mg-NDP solution suggests potential therapeutic implications in modulating cardiac excitability and may relate to changes in channel protein enzymatic activity under experimental conditions .
    Aprikalim
  • HY-12031B
    (2Z,3Z)-U0126

    		Others Inflammation/Immunology
    (2Z,3Z)-U0126 is a selective inhibitor of MEK1 and MEK2, demonstrating potent antiinflammatory effects by noncompetitively inhibiting AP-1 transcriptional activity with IC50 values of 72 nM for MEK1 and 58 nM for MEK2. (2Z,3Z)-U0126 also inhibits anchorage-independent growth of Ki-ras-transformed rat fibroblasts by blocking both the extracellular signal-regulated kinase and mammalian target of rapamycin pathways. Additionally, (2Z,3Z)-U0126 can undergo isomerization and cyclization, resulting in various products that show reduced affinity for MEK and diminished AP-1 inhibition compared to the parent compound.
    (2Z,3Z)-U0126
  • HY-155297
    Nebidrazine

    FLA-136

    		 Histamine Receptor Cardiovascular Disease
    Nebidrazine is a centrally-acting hypotensive agent compared to clonidine, demonstrating weaker cardiovascular effects in rats. It induces dose-dependent hypotension and bradycardia when administered intracerebroventricularly (i.c.v.), with significantly lower sedative potential than clonidine in conscious rats. Yohimbine attenuates the cardiovascular effects of both Nebidrazine and clonidine, suggesting involvement of central alpha-autoreceptors sensitive to yohimbine. Unlike clonidine, Nebidrazine does not affect peripheral alpha-adrenoceptors in pithed rats, indicating a selective central mechanism. Chemical sympathectomy reduces Nebidrazine's cardiovascular effects more than clonidine's, and metiamide diminishes responses to both drugs, implicating central histamine receptors. These findings highlight Nebidrazine's distinct pharmacological profile and potential therapeutic application in managing hypertension through central alpha-autoreceptor stimulation .
    Nebidrazine
  • HY-139121
    15(R)-17-Phenyl trinor Prostaglandin F2α

    15-epi Bimatoprost free acid; 15(R)-Bimatoprost free acid; 15(R)-17-phenyl trinor PGF2α

    		 Prostaglandin Receptor Endocrinology
    17-phenyl trinor Prostaglandin F2α (17-phenyl trinor PGF2α) N-ethyl amide is an F-series prostaglandin analog which has been approved for use as an ocular hypotensive agent. Investigations in our lab have shown that 17-phenyl trinor PGF2α ethyl amide is converted by an amidase enzymatic activity in the human cornea to yield the corresponding free acid, with a conversion rate of about 25 μg/cornea/24 hr. The free acid, 17-phenyl trinor PGF2α, is a potent FP receptor agonist. 15(R)-17-phenyl trinor PGF2α is the 15-epi, or “unnatural” isomer of this active free acid metabolite. It has much diminished FP receptor-mediated activity, which is generally 1.5 to 2 logs less than the 15(S)-isomer. In human and animal models of glaucoma, FP receptor agonist activity corresponds very closely with intraocular hypotensive activity.
    15(R)-17-Phenyl trinor Prostaglandin F2α
  • HY-N0086R
    N6-Methyladenosine (Standard)

    		Influenza Virus Endogenous Metabolite Infection
    N6-Methyladenosine (Standard) is the analytical standard of N6-Methyladenosine. This product is intended for research and analytical applications. N6-Methyladenosine is the most prevalent internal (non-cap) modification present in the messenger RNA (mRNA) of all higher eukaryotes. N6-Methyladenosine can modifies viral RNAs and has antiviral activities. In Vitro: N6-methyladenosine (m6A) is selectively recognized by the human YTH domain family 2 (YTHDF2) protein to regulate mRNA degradation. N6-methyladenosine (m6A), a prevalent internal modification in the messenger RNA of all eukaryotes, is post-transcriptionally installed by m6A methyltransferase (e.g., MT-A70) within the consensus sequence of G(m6A)C (70%) or A(m6A)C (30%). N6-methyladenosine (m6A)-containing RNAs are greatly enriched in the YTHDF-bound portion and diminished in the flow-through portion . N6-methyladenosine (m6A), the most abundant internal RNA modification, functions in diverse biological processes, including regulation of embryonic stem cell self-renewal and differentiation. N6-methyladenosine (m6A) is a large protein complex, consisting in part of methyltransferase-like 3 (METTL3) and methyltransferase-like 14 (METTL14) catalytic subunits .
    N6-Methyladenosine (Standard)

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