BMS-604992 free base  (Synonyms: EX-1314 free base)

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 (k_i=2.3 nM) and potent functional activity (EC₅₀=0.4 nM). BMS-604992 free base can stimulate food intake in rodents^[1].

EC50: 0.4 nM (GHSR), Ki: 2.3 nM (GHSR)^[1]

BMS-604992 exhibits high-affinity binding (K_i=2.3 nM) and potent functional activity (EC₅₀=0.4 nM) for ghrelin receptor^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

497.55

C₂₄H₃₁N₇O₅

760944-56-7

O=C(OCC1=CC=CC2=NN=C([C@H](NC(C(C)(N)C)=O)COCC3=CC=CC=C3)N12)N(CC(N)=O)C

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Charoenthongtrakul S, et, al. Enhanced gastrointestinal motility with orally active ghrelin receptor agonists. J Pharmacol Exp Ther. 2009 Jun;329(3):1178-86.  [Content Brief]