GW-803430

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

GW-803430 (GW-3430) is a potent and selective melanin-concentrating hormone receptor 1 (MCH R1) antagonist with a pIC50 of 9.3. GW-803430 is orally active in an animal model of obesity.

GW-803430 demonstrates a potent antagonist activity towards MCH induced MCHR1 receptor with an IC50 value of ~13?nM.

GW-803430 (0.3, 3, and 15 mg/kg; oral administration; once daily) causes a sustained dose-dependent weight loss relative to vehicle controls.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.Animal Model:High fat diet-induced obese AKR/J mice 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.

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GPCR/G Protein

MCHR

Melanin-concentrating Hormone Receptor (MCHR)

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515141-51-2

481.99

C25H24ClN3O3S

>98% (HPLC)

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O=C1C=2SC(=CC2N=CN1C3=CC=C(OCCN4CCCC4)C(OC)=C3)C=5C=CC(Cl)=CC5

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(-20℃)

With Ice Pack

≥ 2 years