mchr1

AZD1979 is a highly potent MCHR1 (Melanin-concentrating hormone receptor 1) antagonist with an IC50 of 12 nM, exhibiting improved central nervous system (CNS) exposure and enhanced insulin sensitivity in steady-state model assessments, making it suitable for the treatment of obesity.

MCHR1 antagonist 2 is an inhibitor of melanin-concentrating hormone receptor 1 (MCH1-R, IC50 = 65 nM) and also inhibits hERG.

MCHR1 antagonist 1 is a selective antagonist of the melanin-concentrating hormone-1 (MCH1) receptor with a Kb of 1 nM and a Ki of 4 nM at the human MCH1 receptor.

MCHR1 antagonist 3, a potent antagonist of the melanin-concentrating hormone receptor-1 (MCHR1), is employed for the regulation of energy metabolism.

MCHR1antagonist 4 (Compound 2m) is an MCHR1 antagonist capable of penetrating the blood-brain barrier, with Ki values of 0.74 nM and 0.76 nM for hMCHR1 and rMCHR1, respectively. Additionally, it serves as an effective anti-obesity agent.

GW-803430 (GW-3430) is an orally active and selective melanin-concentrating hormone receptor 1 (MCH R1) antagonist used in the study of obesity.

SNAP 94847 hydrochloride is a melanin-concentrating hormonereceptor1 (MCHR1) antagonist(Ki= 2.2 nM)

BMS-819881, a melanin-concentrating hormone receptor 1 (MCHR1) antagonist, binds rat MCHR1 with a Ki of 7 nM, and is selective and potent for CYP3A4 activity with an EC50 of 13 μM.

NGD-4715 is a selective, orally active antagonist of melanin-concentrating hormone receptor 1 (MCHR1).

ATC 0175 hydrochloride is an orally active melanocyte concentrating hormone 1 receptor antagonist that is potent and selective. ATC 0175 hydrochloride has affinity for MCH1R, MCH2R, MCH1, 5-HT2B receptors and 5-HT1A receptors with IC50s of 13.5 nM, >10,000 nM, 13 nM, 9.66 nM and 16.9 nM, respectively. ATC 0175 hydrochloride exhibits antidepressant and anxiolytic effects in animal models. aTC 0175 can be used to study depression and/or anxiety disorders.

BMS-814580 is a potent and selective functional antagonist (Kb = 117 nM) of human MCHR1. BMS-814580 exhibits potent binding affinity (Ki = 17 nM) for human MCHR1. BMS-814580 also exhibits potent binding affinities for cynomolgus monkey and rat MCHR1 (Ki o

T-226296 is a antagonist of melanin concentrating hormone receptor 1 (MCHR1).

SNAP 94847 (SNAP-94847) is a selective and competitive MCH1 receptor (MCH1-R) antagonist (Ki: 2.2 nM). It has anxiolytic and antidepressant activity and reduces food intake in mice.

AMG-076 free base is a potent and selective MCHR1 antagonist.

ATC0065 dihydrochloride is a novel nonpeptidic and potent melanin-concentrating hormone receptor 1 (MCHR1) selective antagonist.

[Ala17]-MCH TFA, a selective ligand for MCHR 1 (K i =0.16 nM) over MCHR 2 (K i =34 nM), is an analogue of MCH. When labeled with a [Eu 3+ chelate], [Ala17]-MCH exhibits high affinity for MCHR 1 (K d =0.37 nM) and negligible binding affinity for MCHR 2.

MCH(human, mouse, rat) is a potent endogenous agonist at melanin-concentration hormone (MCH) receptors (IC50 values are 0.3 and 1.5 nM and EC50 values are 3.9 and 0.1 nM at MCH1 and MCH2 receptors respectively). Increases food intake in vivo.

[Ala17]-MCH acetate is a selective ligand for MCHR1 with a Ki of 0.16 nM and Kd of 0.37 nM(Eu3+ chelate-labeled). [Ala17]-MCH acetate shows selectivity over MCHR2 with Ki of 34 nM.