GW 4064 is a potentFXRagonist with anEC₅₀of 65 nM.

EC50: 65 nM (FXR)^[1]

Treatment with different concentrations of GW4064 (1, 2.5, 5, 10 μM) reduces the lipid accumulation in the cells. Concordantly, GW4064 treatment significantly represses oleic acid-induced CD36 protein levels in a dose-dependent manner. Taken together, these data indicate that prevention of hepatic lipid accumulation is likely due to an inhibition ofCd36expression by long-term GW4064 treatment^[2].

GW4064 suppresses weight gain in C57BL/6 mice fed with either a high-fat diet (HFD) or high-fat, high-cholesterol diet. GW4064 treatment of mice on HFD significantly represses diet-induced hepatic steatosis as evidenced by lower triglyceride and free fatty acid level in the liver. GW4064 markedly reduces lipid transporter CD36 expression without affecting expression of genes that are directly involved in lipogenesis. GW4064 treatment attenuates hepatic inflammation while having no effect on white adipose tissue^[2]. GW4064 (30 mg/kg) treatment results in substantial, statistically significant reductions in serum activities of ALT, AST, LDH, and ALP in the ANIT-treated rats. Serum bile acid levels are also significantly reduced by GW4064 treatment. Bilirubin levels are decreased in the GW4064-treated rats, but statistical significance is not achieved. Notably, GW4064 is much more effective in decreasing these markers of liver damage than TUDCA, which reduces only LDH levels^[3].

542.84

Solid

C₂₈H₂₂Cl₃NO₄

278779-30-9

Room temperature in continental US; may vary elsewhere.

DMSO : 100 mg/mL(184.22 mM;Need ultrasonic)

DMF : 100 mg/mL(184.22 mM;Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMF    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 2.5 mg/mL (4.61 mM); Clear solution
• 2.

  请依序添加每种溶剂： 10% DMF    90%corn oil

  Solubility: ≥ 2.5 mg/mL (4.61 mM); Clear solution
• 3.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 2.5 mg/mL (4.61 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (4.61 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 4.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.08 mg/mL (3.83 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (3.83 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。