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产地 | 中国 |
品牌 | 爱必信(absin) |
货号 | abs812162 |
用途 | 见爱必信官网 |
英文名称 | 见爱必信官网 |
包装规格 | 5mg,5mg,5mg,10mg,10mg,10mg,50mg,50mg,50mg |
纯度 | >98%% |
CAS编号 | 278779-30-9 |
别名 | GW-4064; GW 4064 |
是否进口 | 否 |
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抑制剂描述: 产品名称:GW4064 产品别名:见爱必信官网 英文别名:GW4064 靶点:FXR CAS:278779-30-9 纯度:>98% 外观:见爱必信官网 保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. 描述: GW4064是一种farnesoid X receptor (FXR)激动剂,CV1细胞系中EC50为65 nM。 溶解性:DMSO : 54.3 mg/mL (100 mM) 体外研究:
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. 体内研究: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.
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