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.