| Bioactivity | FXR agonist 3 is an anti-NASH agent, acting by activating FXR. FXR agonist 3 inhibits COL1A1, TGF-β1, α-SMA and TIMP1 expression with anti-fibrogenic activity. FXR agonist 3 significantly reduces liver steatosis and inflammation, improves liver fibrosis level[1]. |
| Invitro | FXR agonist 3 (化合物3a) (5 μM; 24 h) 显示抗纤维化活性，以剂量依赖的方式降低 LX-2细胞中的多种纤维化生物标志物水平[1]。FXR agonist 3 对 LX2 细胞的细胞毒浓度 (CC50) 为 70.36 μM[1]。FXR agonist 3 在人、大鼠和小鼠肝微粒体中的代谢稳定性[1]Species |
| In Vivo | FXR agonist 3 (化合物3a) (200 mg/kg; 口服; 每日给药, 共 4 周) 可显著减轻胆碱缺乏、l-氨基酸的、高脂饮食 (CDAHFD) 诱导的 NASH 小鼠模型的肝纤维化程度[1]。FXR agonist 3 (200 mg/kg; 口服; 每日给药, 共 4 周) 诱导的纤维化大鼠模型也有保护肝和抗纤维化作用[1]。 Animal Model: |
| Name | FXR agonist 3 |
| Formula | C28H28BrNO4 |
| Molar Mass | 522.43 |
| 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]. Zhang N, et al. Discovery and development of palmatine analogues as anti-NASH agents by activating farnesoid X receptor (FXR). Eur J Med Chem. 2023 Jan 5;245(Pt 1):114886. |