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BMS-604992
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BMS-604992图片
CAS NO:674343-47-6
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
EX-1314
产品介绍
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

534.01

Formula

C24H32ClN7O5

CAS 号

674343-47-6

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.