产品
编 号:F422778
分子式:C24H32ClN7O5
分子量:534.01
产品类型
结构图
CAS No: 674343-47-6
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产品详情
生物活性:
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.
体内研究:
BMS-604992 (500 μg/kg; i.p.; 5 minutes) results in a significant increase in gastric emptying compared with vehicle-treated mice.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.BMS-604992 (300 mg/kg; p.o.; 5~20 minutes) produces a significant difference at the 5 minutes time point..BMS-604992 (500 μg/kg; i.p.; 4 hours) increases food intake approximately 2-fold compared with vehicle-treated controls.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.
体外研究:
BMS-604992 exhibits high-affinity binding (Ki=2.3 nM) and potent functional activity (EC50=0.4 nM) for ghrelin receptor.