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Catalog No.
Product Name
Application
Product Information
Product Citation
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CGRP Receptor antagonist
MK 3207 hydrochloride is a potent CGRP receptor antagonist with IC50 of 0.12 nM.- Marlene Dallmayer, .et al. , bioRxiv, 2018, 2018
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Angiotensin II receptor antagonist
Tasosartan is an angiotensin II receptor antagonist. -
H3-receptor antagonist
Ciproxifan maleate is a potent, selective H3 histamine receptor antagonist. -
CGRP receptor antagonist
MK-0974 (Telcagepant) is a potent and selective antagonist of the human and rhesus CGRP receptors. -
Opioid antagonist
Alvimopan behaves as a peripherally acting μ-opioid antagonist. Alvimopan competitively binds to mu-opioid receptor in the gastrointestinal tract. -
D2 receptor antagonist
Adoprazine is part of the Antidepressant Agent group -
CXCR4 antagonist
AMD 070 is a CXCR4 chemokine receptor antagonist.- Uchida D, .et al. , Oncol Rep, 2018, Jul;40(1):303-308 PMID: 29749473
- Mamoru Morimoto, .et al. , BMC Cancer, 2016, 16: 305 PMID: 27175473
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mGluR5 antagonists
Dipraglurant (ADX 48621) is a mGluR5 antagonists with IC50 of 0.021 μM. -
KOR antagonist
JDTic (dihydrochloride) is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception. -
EP4 antagonist
MK-2894 sodium salt is a highly potent and selective second generation EP4 antagonist. -
EP4 antagonist
ONO-AE3-208 is an EP4 antagonist, and suppresses cell invasion, migration, and metastasis of prostate cancer. -
A2a receptor antagonist
SYN115 is an orally administered, potent and selective inhibitor of the adenosine 2a (A2a) receptor that is being developed initially for the treatment of Parkinson?€?s disease, but may also have utility in other CNS disorders. -
5-HT6 receptor antagonist
SB271046 Hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9. -
LTD4 receptor antagonist
Verlukast (MK-0679) is a potent leukotriene D4 antagonist -
CB1 antagonist
CP 945598 is a potent and highly selective CB1 antagonist. -
AR antagonist
Diprophylline is a xanthine derivative with bronchodilator and vasodilator effects. -
MCH-1 antagonist
MCH-1 antagonist 1 is a potent melanin concentrating hormone (MCH-1) antagonist with a Ki of 2.6 nM. MCH-1 antagonist 1 also inhibits CYP3A4 with an IC50 of 10 μM. -
Dopamine receptor antagonist
cis-(Z)-Flupentixol dihydrochloride is a dopamine receptor antagonist, antipsychotic, neuroleptic agent. -
OX Antagonist
Almorexant(ACT078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively. -
D2 receptor antagonist
Pipamperone (Floropipamide; McN-JR 3345; R 3345) is a high-affinity antagonist of 5-HT2A receptor (pKi=8.2) and D4 receptor (pKi=8.0) and a low-affinity antagonist of D2 receptor (pKi=6.7). -
CXCR2 antagonists
CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonists with a pIC50 of 9.3. -
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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Adrenoceptors antagonist
SR 59230A hydrochloride is a β3-adrenoceptor antagonist. -
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). -
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).
