ChemicalBook CAS DataBase List 1469750-46-6

1469750-46-6

Name	Carbamic acid, N-(2-amino-2-oxoethyl)-N-methyl-, [3-[(1S)-1-[(2-amino-2-methyl-1-oxopropyl)amino]-2-(phenylmethoxy)ethyl]-1,2,4-triazolo[4,3-a]pyridin-5-yl]methyl ester, dihydrochloride (1:2)
CAS	1469750-46-6
Molecular Formula	C24H32ClN7O5
Molecular Weight	534.01
MOL File	1469750-46-6.mol

Hazard Information

Uses

BMS-604992 (EX-1314) dihydrochloride is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 dihydrochloride demonstrates high-affinity binding (ki=2.3 nM) and potent functional activity (EC50=0.4 nM). BMS-604992 dihydrochloride can stimulate food intake in rodents[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.

References

[1] Charoenthongtrakul S, et al. Enhanced gastrointestinal motility with orally active ghrelin receptor agonists. J Pharmacol Exp Ther. 2009;329(3):1178-1186. DOI:10.1124/jpet.108.150193

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