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A939572
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。
A939572图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
50mg电议
500mg电议
1g电议

产品介绍
A939572 是一种有效的口服生物可利用的硬脂酰辅酶 A 去饱和酶 1 (SCD1) 抑制剂,对 mSCD1 和 hSCD1 的 IC50 值分别为<4 nM 和 37 nM。

Animal models

ob/ob mice

Dosage form

10 mg/kg; b.i.d.

Applications

In ob/ob mice, A939572 lowered the desaturation index (18:0/18:1n9). Moreover, A939572 reduced triglyceride desaturation index in a dose-dependent manner.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

产品描述

A939572 is a potent and orally bioavailable inhibitor of stearoyl-CoA desaturase1 (SCD1) with IC50 value of 37nM [1].

SCD is a microsomal enzyme that catalyzes the biosynthesis of monounsaturated fatty acids. One member of SCD family, SCD1, is regulated by dietary and hormonal factors and is proved to play an important role in lipid metabolism and body weight control. Thus, SCD1 is a target for the treatment of obesity and diabetes. A939572 is a synthetic inhibitor of SCD1 with improved inhibitory activity and lipophilicity than its parent compound. It shows inhibition of mouse SCD1 and human SCD1 with IC50 values of<4nM and 37nM, respectively. In addition, A939572 has no inhibitory activity to the co-enzymes of SCD1, cytochrome b5 and cytochrome b5 reductase. It suggests that A939572 interacts with SCD1 directly and specifically. Furthermore, A939572 shows high oral bioavailability in mice [1].

References:
[1] Xin Z, Zhao H, Serby M D, et al. Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors. Bioorganic & medicinal chemistry letters, 2008, 18(15): 4298-4302.