BMS-604992 (EX-1314) 是一种选择性的口服活性小分子growth hormone secretagogue receptor (GHSR)激动剂。BMS-604992 具有高亲和力 (ki=2.3 nM) 和强大的功能活性 (EC50=0.4 nM)。BMS-604992 能刺激啮齿动物进食。
生物活性 | BMS-604992 (EX-1314) is a selective, orally active small-moleculegrowth 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]. |
IC50& Target | EC50: 0.4 nM (GHSR), Ki: 2.3 nM (GHSR)[1] |
体外研究 (In Vitro) | BMS-604992 exhibits high-affinity binding (Ki=2.3 nM) and potent functional activity (EC50=0.4 nM) for ghrelin receptor[1].
|
体内研究 (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. |
|
分子量 | |
Formula | |
CAS 号 | |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |