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BMS-604992 free base

Catalog No. T40876 CAS 760944-56-7

Synonyms: BMS-604992 free base, EX-1314 free base

BMS-604992 (EX-1314) free base is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. It exhibits high-affinity binding (k i = 2.3 nM) and potent functional activity (EC 50 = 0.4 nM). Moreover, BMS-604992 free base has the ability to stimulate food intake in rodents.

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BMS-604992 free base, CAS 760944-56-7

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Biological Description

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Description	BMS-604992 (EX-1314) free base is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. It exhibits high-affinity binding (k i = 2.3 nM) and potent functional activity (EC 50 = 0.4 nM). Moreover, BMS-604992 free base has the ability to stimulate food intake in rodents.
Targets&IC50	GHSR:0.4 nM (EC50), GHSR:Ki: 2.3 nM
In vitro	BMS-604992 exhibits high-affinity binding (K i =2.3 nM) and potent functional activity (EC 50 =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: C57BL/6 mice Dosage: 500 μg/kg Administration: I.p.; 5 minutes Result: Resulted in a significant increase in gastric emptying compared with vehicle-treated mice. Animal Model: C57BL/6 mice Dosage: 1~1000 mg/kg Administration: P.o.; 1 hour Result: Showed a dose-linear increase in plasma concentrations at the 1 hour time point and elicited a dose-responsive increase in food intake relative to vehicle-treated controls, with a minimum effective dose of approximately 10 mg/kg. Animal Model: SD rat Dosage: 300 mg/kg Administration: P.o.; 5~20 minutes Result: Observed a significant difference at the 5 minutes time point. Animal Model: Male GhrR KO and WT mice Dosage: 500 μg/kg Administration: I.p.; 4 hours Result: Increased food intake approximately 2-fold compared with vehicle-treated controls.

Synonyms	BMS-604992 free base, EX-1314 free base
Molecular Weight	497.556
Formula	C24H31N7O5
CAS No.	760944-56-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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

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Keywords

BMS-604992 free base 760944-56-7 EX-1314 BMS 604992 free base BMS604992 free base BMS 604992 BMS-604992 EX-1314 free base BMS604992 EX1314 EX 1314 inhibitor inhibit

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