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GW 4064 {[allProObj[0].p_purity_real_show]}

货号:A170958

GW 4064 是一种 FXR 激动剂,IC50 值为 190 nM。GW 4064 具有调节胆固醇和脂质代谢的作用,主要用于研究代谢性疾病和肝脏疾病。

GW 4064 化学结构 CAS号:278779-30-9
GW 4064 化学结构
CAS号:278779-30-9
GW 4064 3D分子结构
CAS号:278779-30-9
GW 4064 化学结构 CAS号:278779-30-9
GW 4064 3D分子结构 CAS号:278779-30-9
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GW 4064 纯度/质量文件 产品仅供科研

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ULK2, IC50: 711 nM

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PFK-015 ++

PFKFB3, IC50: 207 nM

99%+
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ULK2, IC50: 1.1 nM

ULK1, IC50: 2.9 nM

99%+
ROC-325 99%+
Autophinib +++

Autophagy, IC50: 40 nM

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Lys05 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

GW 4064 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].
体内研究

GW4064 effectively suppresses weight gain in C57BL/6 mice on high-fat diets, including those with added cholesterol. It significantly mitigates diet-induced hepatic steatosis, as evidenced by reduced triglyceride and free fatty acid levels in the liver, and notably decreases CD36 expression without altering lipogenesis-related gene expressions. Additionally, GW4064 alleviates hepatic inflammation without impacting white adipose tissue[2].

In ANIT-treated rats, GW4064 administration (30 mg/kg) leads to substantial reductions in serum levels of ALT, AST, LDH, and ALP, and significantly lowers serum bile acid levels. Although bilirubin levels decrease, they do not reach statistical significance. Notably, GW4064 proves more effective in reducing these liver damage markers than TUDCA, which only reduces LDH levels[3].

体外研究

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.

GW 4064 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
human Caco-2 cells 1 μM Function assay 6 days Activation of IBABP gene expression in human Caco-2 cells at 1 uM after 6 days by RT-PCR 17963371

GW 4064 动物研究

Dose Mice: 20 mg/kg[3] (i.p.), 50 mg/kg[4] (i.p.); 2.5 mg/kg[5] (i.v.); 150 mg/kg[6] (p.o.)
Administration i.p., i.v., p.o.

GW 4064 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.

GW 4064 实验方案

计算器
存储液制备 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

GW 4064 技术信息

CAS号278779-30-9
分子式C28H22Cl3NO4
分子量 542.838
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

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

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