BMS-604992 free base_product_DataBase

Bioactivity	BMS-604992 (EX-1314) free base is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 free base demonstrates high-affinity binding (ki=2.3 nM) and potent functional activity (EC50=0.4 nM). BMS-604992 free base can stimulate food intake in rodents[1].
Target	EC50: 0.4 nM (GHSR), Ki: 2.3 nM (GHSR)
Invitro	BMS-604992 exhibits high-affinity binding (Ki=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]. Animal Model:
Name	BMS-604992 free base
CAS	760944-56-7
Formula	C24H31N7O5
Molar Mass	497.55
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Charoenthongtrakul S, et, al. Enhanced gastrointestinal motility with orally active ghrelin receptor agonists. J Pharmacol Exp Ther. 2009 Jun;329(3):1178-86.

PeptideDB

BMS-604992 free base

CAS: 760944-56-7 F: C24H31N7O5 W: 497.55