产品说明书
Tropifexor
 |
同义名 : | LJN452 |
| CAS号 : | 1383816-29-2 | |
| 货号 : | A708662 | |
| 分子式 : | C29H25F4N3O5S | |
| 纯度 : | 99%+ | |
| 分子量 : | 603.585 | |
| MDL号 : | MFCD31693060 | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 85 mg/mL(140.83 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
|
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Tropifexor is a novel and highly potent agonist of FXR with EC50 values of 0.2nM and 0.26nM in a HTRF assay and in a BSEP-luc assay, respectively. Tropifexor induced a robust and dose-dependent increase of FXR target genes BSEP (1nM-1μM) and SHP (10nM-1μM) on mRNA level in rat primary hepatocytes exposure to Tropifexor post 24h. Similar increased expression of this two genes could be observed in vivo in the liver of rat orally dosed of Tropifexor at 1mg/kg, as well as increased FGF15 in rat ileum. The dose-dependent decrease of CYP8B1 in rat liver could be observed in rats orally administrated of Tropifexor at doses ranging in 0.01-3mg/kg once daily for 14 days. Also, it led a dose-dependent decrease of serum triglycerides at doses ranging in 0.03-3mg/kg on day 15, at 24 h following oral administration of the compound once daily for 14 days[3]. | ||
| 作用机制 | Tropifexor can bind to FXR ligand binding domain (PDB 3DCT). | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
1.66mL 0.33mL 0.17mL |
8.28mL 1.66mL 0.83mL |
16.57mL 3.31mL 1.66mL |
| 参考文献 |
|---|