FXR agonist 4 (compound 10a) 是法尼酯 X 受体 (FXR) 激动剂，EC50值为 1.05 μM。FXR agonist 4 有效改善 DIO 小鼠高脂血症、肝脏脂肪变性、胰岛素抵抗和肝脏炎症。FXR agonist 4 可用于非酒精性脂肪性肝病 (NAFLD) 的研究。
| 生物活性 | FXR agonist4 (compound 10a) is an agonist of farnesoid X receptor (FXR) with anEC50value of 1.05 μM.FXR agonist4 effectively improves hyperlipidemia, hepatic steatosis,insulinresistance and hepatic inflammation in DIO mice.FXR agonist4 can be used for the research of non-alcoholic fatty liver disease (NAFLD)[1]. |
体外研究
(In Vitro) | 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[1]。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[1]。FXR agonist 4 (0.1 nM-10 μM) 可激活脂肪堆积的细胞中的 FXR[1]。FXR agonist 4 (10-50 μM; 48 h) 对 HepG2 细胞无毒性[1]。
Cell Cytotoxicity Assay[1] | Cell Line: | HepG2 cell line | | Concentration: | 10, 30 and 50 μM | | Incubation Time: | 48 hours | | Result: | Showed no toxic effects to HepG2 cells at the testing dose up to 50 μM. |
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体内研究
(In Vivo) | 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[1]。
| Animal Model: | High fat diet (HFD)-induced C57BL/6J obese (DIO) mice[1] | | 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). |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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