Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
产品类别：
抑制剂
货号：
T38959
Product Introduction
Bioactivity
名称
BMS-604992 dihydrochloride
描述
BMS-604992 (EX-1314) dihydrochloride is a selective and orally active small-molecule agonist of the growth hormone secretagogue receptor (GHSR). It exhibits high-affinity binding (k i = 2.3 nM) and potent functional activity (EC 50 = 0.4 nM). Furthermore, BMS-604992 dihydrochloride has been shown to stimulate food intake in rodents.
体外活性
BMS-604992 exhibits high-affinity binding (K i =2.3 nM) and potent functional activity (EC 50 =0.4 nM) for ghrelin receptor[1].
体内活性
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.
存储条件
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
