| Identification | Back Directory | [Name]
BMS 604992 | [CAS]
674343-47-6 | [Synonyms]
EX 1314
BMS 604992
EX-1314 HCl
EX-1314 hydrochloride
DFDPBEQMMOYQHK-GMUIIQOCSA-N
EX-1314 hydrochloride, BMS-604992 | [Molecular Formula]
C24H32ClN7O5 | [MOL File]
674343-47-6.mol | [Molecular Weight]
534.008 |
| Hazard Information | Back Directory | [Uses]
BMS-604992 (EX-1314) is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 demonstrates high-affinity binding (Ki=2.3 nM) and potent functional activity (EC50=0.4 nM). BMS-604992 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.
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| 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.
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| 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.
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| 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.
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| [References]
[1] Charoenthongtrakul S, et, al. Enhanced gastrointestinal motility with orally active ghrelin receptor agonists. J Pharmacol Exp Ther. 2009 Jun;329(3):1178-86. DOI:10.1124/jpet.108.150193 |
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