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Catalog No.
Product Name
Application
Product Information
Product Citation
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Opioid Receptor Agonist
Cebranopadol is a potent nociceptin/orphanin FQ peptide (NOP) and opioid receptor agonist -
A2A Receptor Antagonist
SCH 442416 is a selective adenosine A2A receptor antagonist; binds to human and rat A2A receptors with high affinity (Ki values are 0.048 and 0.5 nM respectively). Displays > 23000-fold selectivity for hA2A over hA1 in vitro with minimal affinity for hA2B and hA3 receptors (IC50 > 10 μM). -
PAR-1 Antagonist
Vorapaxar (SCH 530348) is a potent and orally active thrombin receptor (PAR-1) antagonist with Ki of 8.1 nM.- Arundhasa Chandrabalan, .et al. , Sci Rep, 2023, Jan 20;13(1):1124 PMID: 36670151
- Cansu Tekin, .et al. , Cell Oncol (Dordr), 2020, Aug 18 PMID: 32809114
- Cansu Tekin, .et al. , Oncotarget, 2018, Aug 10; 9(62): 32010-32023 PMID: 30174793
- Claushuis TA, .et al. , J Thromb Haemost, 2017, Apr;15(4):744-757 PMID: 28092405
- Maaike Waasdorp, .et al. , Biochem Biophys Rep, 2017, Jul; 10: 152-156 PMID: 29114573
- Joseph C. Mudd, .et al. , J Infect Dis, 2016, Dec 15; 214(12): 1808-1816 PMID: 27703039
- Corey E. Tabit, .et al. , Circulation, 2016, Jul 12; 134(2): 141-152 PMID: 27354285
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5-HT2A and 5-HT2C receptors antagonist
Deramciclane has a high affinity for 5-HT2A and 5-HT2C receptors; it acts as an antagonist at both receptor subtypes and has inverse agonist properties at the 5-HT2C receptors without direct stimulatory agonist. -
D1/D5 receptor antagonist
SCH 23390 hydrochloride is a potent dopamine receptor antagonist (Ki values are 0.2 nM and 0.3 nM at D1 and D5 receptor sub-types, respectively). -
5-HT1B receptor agonist
Eletriptan is a selective 5-hydroxytryptamine 1B/1D (5-HT1B) receptor agonist -
CGRP receptor antagonist
BMS-927711 is a potent, selective, competitive human calcitonin gene-related peptide (CGRP) receptor antagonist that has shown in vivo efficacy without vasoconstrictor effect. -
angiotensin AT2 receptor antagonist
PD 123319 ditrifluoroacetate is a potent, selective, non-peptide angiotensin AT2 receptor antagonist. IC50 values are 34 and 210 nM in rat adrenal tissue and brain respectively.- Dao-Lai Zhang, .et al. , eLife, 2018, 7: e33432 PMID: 29393851
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guanylate cyclase activator
(4-Acetamidocyclohexyl) nitrate (BM121307) is a guanylate cyclase activator that was in phase I development for the treatment of ischaemic heart disorders. The research has been discontinued. -
Adrenoceptors antagonist
SR 59230A hydrochloride is a β3-adrenoceptor antagonist. -
Adrenergic Receptor agonist
Xylazine hydrochloride is an activator of α2A-AR, α2B-AR and α2C-AR. -
Histamine H4 receptor antagonist
A 943931 2HCl is a potent and selective histamine H4 receptor antagonist (pKi values are 7.15 and 8.12 at human and rat receptors respectively). -
serotonin uptake inhibitor
Norfluoxetine is an active metabolite of the antidepressant fluoxetine that inhibits serotonin uptake with a pKi value of 7.35.1 The S-enantiomer of norfluoxetine has 20-times higher serotonin reuptake blocking potency than the R-enantiomer (pKis = 7.86 versus 6.51, respectively). -
GPR40/FFA1 agonist
AMG-837 calcium hydrate is a potent, orally bioavailable GPR40 agonist. -
prostaglandin F2α analog
Cloprostenol is a synthetic analog of prostaglandin F2α (PGF2α). It is 200 times and 100 times more potent than PGF2α in terminating pregnancy in hamsters and rats, respectively, without the side effects associated with PGF2α. -
5-HT2C agonist
S 32212 hydrochloride is an inverse agonist of 5-HT2C receptors (pKi = 8.18 at human 5-HT2C INI receptors). -
EDG-1 (S1P1) agonist
CYM 5442 HCl is a potent and selective EDG-1 (S1P1) agonist in vitro (EC50 = 1.35 nM). -
histamine H3 receptor agonist
Immethridine hydrobromide is a strong and highly selective histamine H3 receptor agonist (pEC50 = 9.74) that displays 300-fold selectivity over the H4 receptor (pKi values are 9.07 and 6.61 respectively). -
human 5'-methylthioadenosine phosphorylase inhibitor
MT-DADMe-ImmA is an inhibitor of human 5'-methylthioadenosine phosphorylase (MTAP) with a Ki of 90 pM. -
β3 adrenergic agonist
CL 316243 disodium salt, a beta-3 adrenergic agonist, was developed as an anti-obesity and diabetes drug, and causes rapid decreases in blood glucose levels in mice. -
β3-adrenergic receptors agonist
BRL-37344 is a b3-AR (b 3-adrenoceptor) selective agonist with lipolytic activity. -
somatostatin receptor 2 antagonist
CYN-154806 is a potent selective somatostatin receptor 2 (sst2) antagonist. -
ETA antagonist
Atrasentan is an experimental drug that is being studied for the treatment of various types of cancer, including non-small cell lung cancer. It is an endothelin receptor antagonist selective for subtype A (ETA). -
H1-receptor antagonist
Astemizole is a potent antihistamine (H1-receptor antagonist, IC50 = 4 nM) that displays selectivity over dopamine, 5-HT, and muscarinic acetylcholine receptors. This compound has shown potent hERG K+ channel blocking activity (IC50 = 0.9 nM), antimalarial activity in multidrug resistant strains in vitro (IC50 = 227 - 734 nM), and has been used as a chaperone to correct folding defects and restore protein function for some mutated forms of hERG channels.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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LPA1 receptor antagonist
AM966 is a high affinity, selective, oral antagonist of LPA1 receptor (lysophosphatidic acid receptor) with an IC50 value of 17 nM.- Maria F Fernandes, .et al. , Int J Mol Sci, 2022, Apr 9;23(8):4163 PMID: 35456981
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NMDA& mGlu receptor agonist
Ibotenic acid is a neuroexcitatory amino acid originally isolated from Amanita species that functions as a NMDA and metabotropic glutamate receptor agonist. -
5-HT6 serotonin receptor antagonist
SB 258585 hydrochloride has been found to be a selective and potent SR-6 antagonist. This compound displays more than a 160-fold selectivity over other serotonin receptor subtypes. -
GLP-1 receptor agonist
ixisenatide inhibit glucagon release, markedly reduce postprandial glucago. have a promoting effct in diabetes mellitus (T2DM). - Bifeprunox Mesylate is an antipsychotic compound through activation of the serotonin 5-hydroxytryptamine (5-HT)1A receptor.
