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GW-803430
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。
GW-803430图片
CAS NO:515141-51-2
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品名称
GW-3430
产品介绍
GW-803430 (GW-3430) 是一种有效的选择性黑色素浓缩激素受体 1 (MCH R1) 拮抗剂,pIC50为 9.3。GW-803430 在肥胖动物模型中具有口服活性。
生物活性

GW-803430 (GW-3430) is a potent and selective melanin-concentrating hormone receptor 1 (MCH R1) antagonist with apIC50of 9.3. GW-803430 is orally active in an animal model of obesity[1].

IC50& Target

pIC50: 9.3 (MCH R1)[1]

体外研究
(In Vitro)

GW-803430 demonstrates a potent antagonist activity towards MCH induced MCHR1 receptor with an IC50value of ~13 nM[2].

体内研究
(In Vivo)

GW-803430 (0.3, 3, and 15 mg/kg; oral administration; once daily) causes a sustained dose-dependent weight loss relative to vehicle controls[1].
GW-803430 is a suitable compound for its good pharmacokinetic properties (bioavailability=31%, t1/2=11 h) and brain penetration (6:1 brain:plasma concentration) in mice[1].

Animal Model:High fat diet-induced obese AKR/J mice[1]
Dosage:0.3, 3, and 15 mg/kg
Administration:Orally, qd,12 days
Result:Caused a sustained dose-dependent weight loss of -6.2%, -12.1%, and -13.1%, respectively, relative to vehicle controls.
分子量

481.99

性状

Solid

Formula

C25H24ClN3O3S

CAS 号

515141-51-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
In solvent-80°C6 months
-20°C1 month