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Catalog No.
Product Name
Application
Product Information
Product Citation
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Histamine Receptor antagonist
Bepotastine Beslilate (Bepreve) is a histamine H1 receptor anatagonist.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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mGluR5 antagonists
Dipraglurant (ADX 48621) is a mGluR5 antagonists with IC50 of 0.021 μM. -
glucagon receptor antagonist
Glucagon receptor antagonists-1 is a highly potent glucagon receptor antagonist. -
Glucagon receptor antagonist
Glucagon receptor antagonists-2 is a highly potent glucagon receptor antagonist. -
Glucagon receptor antagonist
Glucagon receptor antagonists-3 is a highly potent glucagon receptor antagonist. -
A2A antagonist
Istradefylline (KW-6002) is a selective antagonist at the A2A receptor. It has been found to be useful in the treatment of Parkinson's disease.- PU Hamor, .et al. , Prog Neuropsychopharmacol Biol Psychiatry, 2020, Dec 20;103:109979 PMID: 32470496
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KOR antagonist
JDTic (dihydrochloride) is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception. -
mGluR-2 antagonist
LY 341495 has been shown to be a highly potent and selective group II metabotropic glutamate receptor (mGluR-2) antagonist with Ki / IC50 values are 2.3, 1.3, 173, 990, 6800, 8200 and 22000 nM for human mGluR-2, mGluR-3, mGluR-8 , mGluR-7a, mGluR-1a, mGluR-5a and mGluR-4a. -
CysLT1 receptor antagonist
Montelukast (sodium) (MK0476) is a potent, selective CysLT1 receptor antagonist. -
Endothelin receptor antagonist
Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH). -
EP4 antagonist
MK-2894 sodium salt is a highly potent and selective second generation EP4 antagonist. -
CaSR antagonist
NPS-2143 hydrochloride (SB-262470A hydrochloride), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. -
EP4 antagonist
ONO-AE3-208 is an EP4 antagonist, and suppresses cell invasion, migration, and metastasis of prostate cancer. -
CXCR1/CXCR2 antagonist
SCH527123 is a potent and selective antagonist of the human CXCR1 and CXCR2 receptors with IC50 of 42 nM and 3 nM, respectively.- Ruijie Zhang, .et al. , Int J Oncol, 2022, May;60(5):50 PMID: 35315502
- Fu S, .et al. , Int J Oncol, 2018, Jul;53(1):349-357 PMID: 29749433
- Fu S, .et al. , Anticancer Res, 2018, Nov;38(11):6271-6279 PMID: 30396947
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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. -
ETA receptor antagonist
Sitaxentan sodium (TBC-11251) is a selective endothelin receptor-A antagonist with IC50 and Ki of 1.4 nM and 0.43 nM, respectively. -
ETA receptor antagonist
Sitaxsentan (IPI 1040; TBC-11251) is a selective endothelin A (ETA) receptor antagonist. Antihypertensive. Sitaxsentan is used in treatment of chronic heart failure. -
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 -
histamine receptor antagonist
Cyproheptadine hydrochloride is a histamine receptor antagonist for 5-HT2 receptor with IC50 of 0.6 nM. -
NMDA receptor antagonist
Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker. -
H2 receptor antagonist
Lafutidine is a second generation H2 receptor antagonist having multimodal mechanism of action. -
5-HT antagonist
Tegaserod functions as a motility stimulant, achieving its desired therapeutic effects through activation of the 5-HT4 receptors of the enteric nervous system in the gastrointestinal tract. It also stimulates gastrointestinal motility and the peristaltic reflex, and allegedly reduces abdominal pain. Additionally, tegaserod is a 5-HT2B receptor antagonist. -
neurokinin-1 receptor antagonist
Fosaprepitant (MK-0517, L-758,298) is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist. -
Prostaglandin D2 receptor CRTH2 antagonist
CAY10471 Racemate (TM30089 Racemate) is a potent and highly selective prostaglandin D2 receptor CRTH2 antagonist. -
CCK-A receptor antagonist
Loxiglumide (CR1505) is a cholecystokinin antagonist -
D2/5-HT2 receptor antagonist
Blonanserin is a D2/5-HT2 receptor antagonist; atypical antipsychotic. -
Leukotriene receptor antagonist
Pranlukast is a selective cysteinyl leukotriene receptor antagonist. -
CB1 antagonist
CP 945598 is a potent and highly selective CB1 antagonist. -
CXCR4 antagonist
AMD 3465 is a potent, selective CXCR4 antagonist.- Kentaro Suzuki, .et al. , Sci Rep, 2019, 9: 15284
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AR antagonist
Diprophylline is a xanthine derivative with bronchodilator and vasodilator effects. -
PAR4 antagonist
BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 (PAR4) antagonist, with IC50s of 9.5 nM and 2.1 nM in human and monkey blood, respectively. -
PAF antagonist
Aglafoline is an effective PAF antagonist not only in vitro, but also in vivo. -
5-HT4 receptor antagonist
5-HT4 antagonist 1 is a 5-HT4 receptor antagonist with a pKi of 9.6. -
5-HT2A receptor antagonist
Lumateperone Tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a SERT blocker (Ki = 61 nM). -
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.
