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BMS-604992 dihydrochloride

BMS-604992 dihydrochloride

产品编号 T38959   CAS 1469750-46-6
别名: EX-1314 dihydrochloride, BMS-604992 dihydrochloride

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.

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BMS-604992 dihydrochloride Chemical Structure
BMS-604992 dihydrochloride, CAS 1469750-46-6
规格 价格/CNY 货期 数量
25 mg ¥ 10,600 6-8周
其他形式的 BMS-604992 dihydrochloride:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: BMS-604992 dihydrochloride (T38959)
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参考文献
产品描述 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.
靶点活性 GHSR:0.4 nM (EC50), GHSR:Ki: 2.3 nM
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.
别名 EX-1314 dihydrochloride, BMS-604992 dihydrochloride
分子量 570.47
分子式 C24H33Cl2N7O5
CAS No. 1469750-46-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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TargetMol Library Books参考文献

1. Charoenthongtrakul S, et al. Enhanced gastrointestinal motility with orally active ghrelin receptor agonists. J Pharmacol Exp Ther. 2009;329(3):1178-1186.

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Keywords

BMS-604992 dihydrochloride 1469750-46-6 EX 1314 Dihydrochloride EX 1314 BMS-604992 Dihydrochloride BMS604992 Dihydrochloride BMS604992 EX-1314 dihydrochloride BMS 604992 Dihydrochloride EX1314 Dihydrochloride EX1314 BMS 604992 dihydrochloride BMS604992 dihydrochloride EX-1314 BMS 604992 BMS-604992 EX-1314 Dihydrochloride Inhibitor inhibitor inhibit

 

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