BMS-604992 (EX-1314) free base 是一种选择性的口服活性小分子growth hormone secretagogue receptor (GHSR)激动剂。BMS-604992 free base 具有高亲和力 (ki=2.3 nM) 和强大的功能活性 (EC50=0.4 nM)。BMS-604992 free base 能刺激啮齿动物进食。
| 生物活性 | BMS-604992 (EX-1314) free base is a selective, orally active small-moleculegrowth hormone secretagogue receptor (GHSR)agonist. BMS-604992 free base demonstrates high-affinity binding (ki=2.3 nM) and potent functional activity (EC50=0.4 nM). BMS-604992 free base 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].
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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. |
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| 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. |
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