CAS:1032229-33-6A939572

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Synonyms: Stearoyl-CoA Desaturase Inhibitor;SCD Inhibitor

A939572 is an inhibitor of SCD1 with IC50 values of 4 nM and 37 nM for mSCD1 and hSCD1.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

技术信息

CAS号

1032229-33-6

储存条件

分子式

C20H22ClN3O3

运输

蓝冰

分子量

387.86

别名

Stearoyl-CoA Desaturase Inhibitor;SCD Inhibitor

溶解度

DMSO	95.0 mg/mL (244.9 mM) warming

动物实验配方

生物活性

描述SCD1 (stearoyl-CoA desaturase1) plays an important role in lipid metabolism and body weight control. Higher SCD1 activity in humans has been correlated with elevated plasma triglyceride levels. A939572 is an orally bioavailable and potent SCD1 inhibitor with IC₅₀ values of <4 nM and 37 nM for mSCD1 and hSCD1, respectively . A939572 demonstrated a significant dose-dependent decrease in proliferation in Caki1, A498, Caki2, and ACHN at day 5 (IC₅₀s of 65 nM, 50 nM, 65 nM, and 6 nM respectively). Moreover, A939572 induced apoptosis in all four cell lines . A939572 has modest volume of distribution and high oral bioavailability in mice (CL_p= 0.4 L/h/kg; V_ss= 0.4 L/kg; F= 92%). In ob/ob mice, A939572 (10 mpk bid) consistently reduced desaturation indices of all these lipid categories (cholesterol ester, diacylglycerol, free fatty acid, free cholesterol, total phospholipids, and triacylglycerol) to lean level, or even lower. A dose dependent triglyceride desaturation index reduction by A939572 was also observed in ob/ob mice .