| Description | FXR agonist 3 is an anti-NASH compound with antifibrotic and anti-fibrotic activity, inhibiting the expression of COL1A1, TGF-β1, α-SMA, and TIMP1, with an IC50 value of 8.19 μmol/L for COL1A1. FXR agonist 3 ameliorates CDAHFD and BDL-induced liver injury in vivo by activating FXR. |
| In vitro | 在 LX-2 细胞中，FXR agonist 3（0、2.5、5、7.5和 10 μM；24 小时；有或无 2 ng/mL TGF-β1 再持续 24 小时）能够以剂量依赖性方式降低 COL1A1、TGF-β1、α-SMA 和 TIMP1 蛋白的表达[1]。 |
| In vivo | 在喂食 CDAHFD 饮食 16 周的 C57BL/6 N小鼠中，FXR agonist 3（200 mg/kg；口服灌胃；在 CDAHFD 诱导后每日一次，持续 4 周）能够降低肝脏中 IL-1β 和 IL-6 的表达[1]。 |
| molecular weight | 521.12 |
| Molecular formula | C28H28BrNO4 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 200 mg/mL (382.83 mM), Sonication is recommended. |
| References | 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. |