| 产品描述: | 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. |
| 体外研究: |
FXR agonist 3 (compound 3a) (200 mg/kg; p.o.; daily for 4 weeks) significantly attenuates the degree of liver fibrosis in choline-deficient, l-amino acid-defined, high-fat diet (CDAHFD)-induced NASH mice model[1]. FXR agonist 3 (200 mg/kg; p.o.; daily for 4 weeks) also exerts liver-protective and anti-fibrosis activities in bile duct ligation (BDL)-induced fibrosis rat model[1]. |
| 体内研究: |
FXR agonist 3 (compound 3a) (5 μM; 24 h) shows anti-fibrogenic activity, decreases multiple fibrogenic biomarkers level in LX-2 cells in a dose-dependent manner. FXR agonist 3 shows cytotoxic concentration against LX2 cells with an CC50 value of 70.36 μM.
Metabolic stability of FXR agonist 3 in human, rat and mouse liver microsomes |
| 保存条件: |
-80°C 6个月;-20°C 1个月 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.914 ml |
9.571 ml |
19.141 ml |
| 5 mM |
0.383 ml |
1.914 ml |
3.828 ml |
| 10 mM |
0.191 ml |
0.957 ml |
1.914 ml |
| 50 mM |
0.038 ml |
0.191 ml |
0.383 ml |
|
| 注意: |
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