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BMS-604992 dihydrochloride

Catalog No. T38959 CAS 1469750-46-6

Synonyms: EX-1314 dihydrochloride, BMS-604992 dihydrochloride

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

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BMS-604992 dihydrochloride Chemical Structure

BMS-604992 dihydrochloride, CAS 1469750-46-6

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Description	BMS-604992 (EX-1314) dihydrochloride is a selective and orally active small-molecule agonist of the growth hormone secretagogue receptor (GHSR). It exhibits high-affinity binding (k i = 2.3 nM) and potent functional activity (EC 50 = 0.4 nM). Furthermore, BMS-604992 dihydrochloride has been shown to stimulate food intake in rodents.
Targets&IC50	GHSR:0.4 nM (EC50), GHSR:Ki: 2.3 nM
In vitro	BMS-604992 demonstrates high-affinity binding (K i =2.3 nM) and potent functional activity (EC 50 =0.4 nM) at the ghrelin receptor[1].
In vivo	BMS-604992 demonstrates diverse pharmacological activities across different dosages and administration methods in animal studies. At a dosage of 500 μg/kg administered intraperitoneally (i.p.) for 5 minutes, it significantly enhances gastric emptying in C57BL/6 mice compared to those receiving a vehicle[1]. When given orally (p.o.) at dosages ranging from 1 to 1000 mg/kg for 1 hour, BMS-604992 shows a linear relationship between dose and plasma concentration at the 1-hour mark, along with a dose-dependent increase in food consumption in C57BL/6 mice, identifying a minimum effective dose of approximately 10 mg/kg[1]. A specific 300 mg/kg oral dosage results in a notable difference in effect within just 5 minutes in SD rats[1]. Lastly, an i.p. administration of 500 μg/kg over 4 hours leads to a twofold increase in food intake in male GhrR KO and WT mice compared to vehicle-treated controls[1], highlighting its potential impact on feeding behavior and gastric processes.

Synonyms	EX-1314 dihydrochloride, BMS-604992 dihydrochloride
Molecular Weight	570.47
Formula	C24H33Cl2N7O5
CAS No.	1469750-46-6

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;329(3):1178-1186.

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Keywords

BMS-604992 dihydrochloride 1469750-46-6 EX 1314 Dihydrochloride EX 1314 BMS-604992 Dihydrochloride BMS604992 Dihydrochloride BMS604992 EX-1314 dihydrochloride BMS 604992 Dihydrochloride EX1314 Dihydrochloride EX1314 BMS 604992 dihydrochloride BMS604992 dihydrochloride EX-1314 BMS 604992 BMS-604992 EX-1314 Dihydrochloride inhibitor inhibit

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