BMS-604992

BMS-604992 (EX-1314) is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 demonstrates high-affinity binding (K_i=2.3 nM) and potent functional activity (EC₅₀=0.4 nM). BMS-604992 can stimulate food intake in rodents^[1]. IC50 & Target: EC50: 0.4 nM (GHSR), Ki: 2.3 nM (GHSR)^[1] In Vitro: BMS-604992 exhibits high-affinity binding (K_i=2.3 nM) and potent functional activity (EC₅₀=0.4 nM) for ghrelin receptor^[1]. In Vivo: BMS-604992 (500 μg/kg; i.p.; 5 minutes) results in a significant increase in gastric emptying compared with vehicle-treated mice^[1].
BMS-604992 (1~1000 mg/kg; p.o.; 1 hour) Shows a dose-linear increase in plasma concentrations at the 1 hour time point and elicits a dose-responsive increase in food intake relative to vehicle-treated controls, with a minimum effective dose of approximately 10 mg/kg^[1].
BMS-604992 (300 mg/kg; p.o.; 5~20 minutes) produces a significant difference at the 5 minutes time point.^[1].
BMS-604992 (500 μg/kg; i.p.; 4 hours) increases food intake approximately 2-fold compared with vehicle-treated controls^[1].