GW 4064

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Chemical Structure| 278779-30-9 同义名 : -
CAS号 : 278779-30-9
货号 : A170958
分子式 : C28H22Cl3NO4
纯度 : 99%+
分子量 : 542.84
MDL号 : MFCD09971006
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：

IP 2% DMSO+2% Tween80+40% PEG300+water 5 mg/mL clear

PO 0.5% CMC-Na 38 mg/mL suspension

生物活性
描述 Treatment with varying concentrations of GW4064 (1, 2.5, 5, 10 μM) decreases lipid accumulation in cells. Specifically, GW4064 treatment notably reduces oleic acid-induced CD36 protein levels in a dose-dependent manner, indicating that the inhibition of CD36 expression is a key mechanism in preventing hepatic lipid accumulation[2].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
HEK293 cells Function assay Agonist activity at human FXR expressed in HEK293 cells by luciferase reporter gene assay, EC50=0.026 μM 25305688
HEK293 cells Function assay Agonistic activity at FXR in HEK293 cells by GAL4 transactivation activity, EC50=0.07 μM 17292610
HeLa cells Function assay 24 h Agonist activity at human full length FXR expressed in HeLa cells cotransfected with pSG5-human RXR after 24 hrs by Dual-Glo luciferase reporter gene assay, EC50=0.51 μM 25934227
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.84mL

0.37mL

0.18mL

9.21mL

1.84mL

0.92mL

18.42mL

3.68mL

1.84mL
参考文献

[1]Ma Y, et al. Synthetic FXR agonist GW4064 prevents diet-induced hepatic steatosis and resistance. Pharm Res. 2013 May;30(5):1447-57.

[2]Liu Y, et al. Hepatoprotection by the farnesoid X receptor agonist GW4064 in rat models of intra- and extrahepatic cholestasis. J Clin Invest. 2003 Dec;112(11):1678-87.