rat mchr1

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

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

MCH(human, mouse, rat) 是MCH-R 肽激动剂，对 CHO 细胞系中 MCH-2R 高度敏感，激活 MCH-1R 和 MCH-2R 的IC50 值分别为 0.3 和 1.5 nM，EC50值对分别为 3.9 和 0.1 nM。