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编 号：F762958
分子式：C21H28ClN3O
分子量：373.92
分子式：C21H28ClN3O
分子量：373.92
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CAS No: 3025841-47-5
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生物活性：
FXR agonist 4 (compound 10a) is an agonist of farnesoid X receptor (FXR) with an EC50 value of 1.05 μM. FXR agonist 4 effectively improves hyperlipidemia, hepatic steatosis, insulin resistance and hepatic inflammation in DIO mice. FXR agonist 4 can be used for the research of non-alcoholic fatty liver disease (NAFLD).
体内研究：
FXR agonist 4 (100 mg/kg；口服给药，一次) 改善 DIO 小鼠的高脂血症，肝脏脂肪变性，胰岛素抵抗和肝脏炎症。Animal Model:High fat diet (HFD)-induced C57BL/6J obese (DIO) mice
Dosage:100 mg/kg
Administration:Oral administration; 100 mg/kg once
Result:Decreased blood triglyceride, total cholesterol and low-density lipoprotein cholesterol levels of DIO mice after treatment for 3 week. Significantly decreased the serum alanine aminotransferase (ALT) level and promoted cholesterol excretion after treatment for 45 days. Increased the expression of Srebp1c, stearoyl-CoA desaturase 1 (Scd1), fatty acid synthetase (Fasn), Diac ylgycerol Acyltransferase 2 (Dgat2), 3 Hydroxy-3-methylglutaryl Coenzyme A Reductase (Hmgcr) and sterol regulatory element binding protein 2 (Srebp2). Improved insulin sensitivity of DIO mice. Reduced mRNA levels of interleukin 1 beta (Il-1β), Il5, Il6, cluster of differentiation 36 (Cd36), inducible nitric oxide synthase (iNOS) and mouse EGF-like module-containing mucin-like hormone receptor-like 1 (F4/80).
体外研究：
FXR agonist 4 (10 nM-10 μM) 对 FXR 具有激动活性，在 HEK293T 细胞中的 EC50 值为 1.05 μM。FXR agonist 4 (1 nM-10 μM) 剂量依赖性地增加类固醇受体辅激活物 SRC-2 募集，EC50 值为 1.04 μM。FXR agonist 4 (0.1 nM-10 μM) 可激活脂肪堆积的细胞中的 FXR。FXR agonist 4 (10-50 μM; 48 h) 对 HepG2 细胞无毒性。
FXR agonist 4 (compound 10a) is an agonist of farnesoid X receptor (FXR) with an EC50 value of 1.05 μM. FXR agonist 4 effectively improves hyperlipidemia, hepatic steatosis, insulin resistance and hepatic inflammation in DIO mice. FXR agonist 4 can be used for the research of non-alcoholic fatty liver disease (NAFLD).
体内研究：
FXR agonist 4 (100 mg/kg；口服给药，一次) 改善 DIO 小鼠的高脂血症，肝脏脂肪变性，胰岛素抵抗和肝脏炎症。Animal Model:High fat diet (HFD)-induced C57BL/6J obese (DIO) mice
Dosage:100 mg/kg
Administration:Oral administration; 100 mg/kg once
Result:Decreased blood triglyceride, total cholesterol and low-density lipoprotein cholesterol levels of DIO mice after treatment for 3 week. Significantly decreased the serum alanine aminotransferase (ALT) level and promoted cholesterol excretion after treatment for 45 days. Increased the expression of Srebp1c, stearoyl-CoA desaturase 1 (Scd1), fatty acid synthetase (Fasn), Diac ylgycerol Acyltransferase 2 (Dgat2), 3 Hydroxy-3-methylglutaryl Coenzyme A Reductase (Hmgcr) and sterol regulatory element binding protein 2 (Srebp2). Improved insulin sensitivity of DIO mice. Reduced mRNA levels of interleukin 1 beta (Il-1β), Il5, Il6, cluster of differentiation 36 (Cd36), inducible nitric oxide synthase (iNOS) and mouse EGF-like module-containing mucin-like hormone receptor-like 1 (F4/80).
体外研究：
FXR agonist 4 (10 nM-10 μM) 对 FXR 具有激动活性，在 HEK293T 细胞中的 EC50 值为 1.05 μM。FXR agonist 4 (1 nM-10 μM) 剂量依赖性地增加类固醇受体辅激活物 SRC-2 募集，EC50 值为 1.04 μM。FXR agonist 4 (0.1 nM-10 μM) 可激活脂肪堆积的细胞中的 FXR。FXR agonist 4 (10-50 μM; 48 h) 对 HepG2 细胞无毒性。
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