产品说明书

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 : 542.838
MDL号 : MFCD09971006
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(193.43 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

DMF: 100 mg/mL(184.22 mM)，配合低频超声助溶
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].
作用机制 FXR has a structural conserved ligand-binding pocket with conformational flexibility to allow the binding of specific ligands. GW4064, as an FXR agonist, enters the FXR pocket and occupies a binding site to mediate the function of FXR.
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 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.