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GW-4064

CAS No. 278779-30-9

GW-4064 ( GW 4064 | GW4064 )

产品货号. M13852 CAS No. 278779-30-9

一种有效的选择性 FXR 激动剂,在无细胞测定中 EC50 为 15 nM。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
5MG ¥373 有现货
10MG ¥616 有现货
25MG ¥1150 有现货
50MG ¥2001 有现货
100MG ¥3621 有现货
200MG ¥5451 有现货
500MG ¥8586 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    GW-4064
  • 注意事项
    本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
  • 产品简述
    一种有效的选择性 FXR 激动剂,在无细胞测定中 EC50 为 15 nM。
  • 产品描述
    A potent and selective FXR agonist with EC50 of 15 nM in cell-free assay, >200-fold more potent than CDCA; has an EC50 of 80 and 90 nM, respectively, in CV-1 cells transfected with mouse and human FXR expression vectors; significantly reducess serum alanine aminotransferase, aspartate aminotransferase, and lactate dehydrogenase, as well as other markers of liver damage in rat models of cholestasis.(In Vitro):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 of Cd36 expression by long-term GW4064 treatment. (In Vivo):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. 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.
  • 体外实验
    ——
  • 体内实验
    ——
  • 同义词
    GW 4064 | GW4064
  • 通路
    Metabolic Enzyme/Protease
  • 靶点
    FXR
  • 受体
    FXR
  • 研究领域
    Metabolic Disease
  • 适应症
    ——

化学信息

  • CAS Number
    278779-30-9
  • 分子量
    542.8376
  • 分子式
    C28H22Cl3NO4
  • 纯度
    >98% (HPLC)
  • 溶解度
    10 mM in DMSO
  • SMILES
    O=C(O)C1=CC=CC(/C=C/C2=CC=C(OCC3=C(C(C)C)ON=C3C4=C(Cl)C=CC=C4Cl)C=C2Cl)=C1
  • 化学全称
    Benzoic acid, 3-[2-[2-chloro-4-[[3-(2,6-dichlorophenyl)-5-(1-methylethyl)-4-isoxazolyl]methoxy]phenyl]ethenyl]-

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

参考文献

1. Maloney PR, et al. J Med Chem. 2000 Aug 10;43(16):2971-4. 2. Liu Y, et al. J Clin Invest. 2003 Dec;112(11):1678-87. 3. Kast HR, et al. J Biol Chem. 2002 Jan 25;277(4):2908-15.
产品手册
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