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GPCR

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Cat. No. Product Name Field of Application Chemical Structure
DC7192 LY-404039 Featured LY404039 is an inhibitor for mGluR1(Ki=149 nM) and mGluR2(Ki= 92 nM), which can also inhibit dopamine receptor.
DC1012 Macitentan (Actelion-1,ACT-064992) Featured macitentan (Actelion-1, ACT-064992) is an orally active, non-peptide dual endothelin (ET)A/B receptor antagonist with IC50 of 0.5 nM/391 nM.
DC9519 Maropitant Maropitant is a neurokinin (NK1) receptor antagonist.
DC7681 Mavoglurant (AFQ 056) Featured Mavoglurant (AFQ056) is an experimental drug candidate for the treatment of fragile X syndrome.It exerts its effect as an antagonist of the metabotropic glutamate receptor 5 (mGLU5).
DC9297 MDK-5220(Orexin-2 receptor agonist) Featured MDK-5220(Orexin-2 receptor agonist) is the first selective nonpeptidic orexin 2 receptor (OX2R) agonist (OX2R EC50 = 0.023 μM, Emax = 98%; OX1R EC50 = 1.616 μM, Emax = 100%)
DC7757 (R)-Meclizine Meclizine is a histamine H1 receptor antagonist used to treat nausea and motion sickness.
DCAPI1580 Medetomidine Medetomidine hydrochloride is a potent and highly selective α2-AR adrenoceptor agonist (Ki values are 1.08 and 1750 nM for α2- and α1-adrenoceptors respectively). Shows greater selectivity over α1-adrenoceptors than clonidine and UK 14,304 (1620-, 220- an
DC11083 Dersimelagon Featured Dersimelagon, also known as MT-7117 and WHO 10832, is a novel, orally-administered, small molecule, selective melanocortin-1 receptor (MC1R) agonist that increases skin melanin without sun exposure and is being developed to increase light tolerance in EPP/XLP patients. Dersimelagon significantly boosted sunlight tolerance in patients with erythropoietic protoporphyria in a multicenter, phase 2, randomized trial.
DC9526 Meptazinol (hydrochloride) Featured Meptazinol Hcl(WY-22811 Hcl) is a unique centrally active opioid analgesic.
DC10407 Mequitazine Mequitazine is a potent, nonsedative and long-acting histamine H1 antagonist.
DC9527 Methylnaltrexone (Bromide) Featured Methylnaltrexone Bromide is a pheriphally-acting μ-opioid antagonist that acts on the gastrointestinal tract to decrease opioid-induced constipation.
DC9191 Metoprolol tartrate Metoprolol is a cardioselective β1-adrenergic blocking agent.
DC8249 MF498 MF498 is a novel and selective E prostanoid receptor 4 (EP4) inhibitor, relieves joint inflammation and pain in rodent models of rheumatoid and osteoarthritis.
DC11902 Minesapride Minesapride (DSP-6952) is a novel potent, selective, orally active 5-HT4 receptor partial agonist with Ki of 50-100 nM for human 5-HT4a/4b/4c.
DC3172 Mirabegron Featured Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.
DC9468 Mizolastine Mizolastine is a histamine H1-receptor antagonist with IC50 of 47 nM used in the treatment of hay fever (seasonal allergic rhinitis), hives and other allergic reactions.
DC1009 Laropiprant Featured MK 0524 is a potent, selective DP1 receptor antagonist with Ki values of 0.57 nM and 0.75 µM for the DP1 and DP2 receptors, respectively.
DC9456 MK-0354 MK-0354 is a partial agonist of GPR109a receptor, for hGPR109a/ mGPR109a with EC50 of 1.65/1.08 μM, showed no activation of GPR109b.
DC10045 MK-0557 Featured MK-0557 is a highly selective, orally administered neuropeptide NPY5R antagonist, could limit weight regain after very-low-calorie diet (VLCD)-induced weight loss.
DC3167 MK0812 MK-0812 is chemokine receptor CCR-2 antagonist
DC9398 MK-0974 MK-0974(Telcagepant) is a highly potent, selective, and orally bioavailable CGRP receptor antagonist with Ki values of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors respectively; displays >1500-fold lower affinity for the canine and rat receptors
DC9966 MK-1064 Featured MK-1064 is a selective orexin 2 receptor antagonist (2-SORA) for the research of insomnia.
DC9607 MK-2894 MK-2894 is a highly potent and selective second generation EP4 antagonist.
DC9397 MK-3207 (Hydrochloride) MK-3207 is a potent and orally bioavailable CGRP receptor antagonist (IC50= 0.12 nM; Ki value= 0.024 nM); highly selective versus human AM1, AM2, CTR, and AMY3.
DC7646 MK3697 MK-3697 is a third insomnia drug, currently being developed by Merck. MK-3697 is a potent and selective Orexin receptor antagonist with Ki = 0.95 nM.
DC9279 MK-571 Featured MK-571 is a selective, orally active CysLT1 receptor antagonist.
DC9455 MK-6892 MK-6892 is a highly potential GPR109A agonist with Ki value of 4.0 nM.
DC10785 MK-7246 Featured MK-7246 is a potent and selective CRTH2 antagonist with a Ki of 2.5±0.5 nM.
DC11142 MK-8318 MK-8318 (MK8318) is a potent, selective, orally available CRTh2 receptor antagonist with Ki of 5 nM, shows nM potency in functional assay (cAMP IC50=8 nM, β-Arrestin IC50=3.5 nM.
DC12333 ML-109 Featured ML-109 is a potent and full thyroid stimulating hormone receptor (TSHR) agonist, with an EC50 of 40 nM.

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