| Bioactivity | 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)[1]. |
| Invitro | 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: |
| 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: |
| Name | FXR agonist 4 |
| Formula | C21H28ClN3O |
| Molar Mass | 373.92 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Qin T, et al. Structural optimization and biological evaluation of 1-adamantylcarbonyl-4-phenylpiperazine derivatives as FXR agonists for NAFLD. Eur J Med Chem. 2023 Jan 5;245(Pt 1):114903. |