FXR agonist 3 是一种抗 NASH 试剂，通过激活 FXR 起作用。FXR agonist 3 抑制
COL1A1、
TGF-β1、
α-SMA和
TIMP1的表达，具有抗纤维化活性。FXR agonist 3 显著减轻肝脏脂肪变性和炎症，改善肝纤维化水平。
| 生物活性 |
FXR agonist3 is an anti-NASH agent, acting by activatingFXR.FXR agonist3 inhibitsCOL1A1,TGF-β1,α-SMAandTIMP1expression with anti-fibrogenic activity.FXR agonist3 significantly reduces liver steatosis and inflammation, improves liver fibrosis level[1].
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体外研究
(In Vitro) |
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 |
T1/2(h) |
CLInt (mic)(μg/min/mg) |
CLInt (liver)(μg/min/mg) |
Remaining Ratio (%) (T=60 min) |
| Human |
53.3 |
26.0 |
23.4 |
44.1 |
| Rat |
7.4 |
187.8 |
338.0 |
0.4 |
| Mouse |
7.4 |
187.9 |
744.1 |
39.0 |
Western Blot Analysis[1]
| Cell Line: |
LX-2 cells |
| Concentration: |
0, 2.5, 5, 7.5, and 10 μM |
| Incubation Time: |
24 hours; with or without 2 ng/mL TGF-β1 for another 24 hr |
| Result: |
Decreased COL1A1, TGF-β1, α-SMA, and TIMP1 protein expressions in a dose-dependent manner. |
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体内研究
(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: |
C57BL/6 N mice fed CDAHFD diet for 16 weeks[1] |
| Dosage: |
200 mg/kg |
| Administration: |
Oral gavage; daily for 4 weeks after CDAHFD-induced |
| Result: |
Decreased expression of IL-1β and IL-6 in livers, indicating the liver-protective effect of 3a in CDAHFD mice may partially through inhibiting inflammasome activation.
Lowered the serum levels of biochemical markers of ALT, AST, ALP, LDH, LDL and TBiL significantly, while raised HDL and GLU levels. |
| Animal Model: |
C57BL/6 N mice inuced with BDL[1] |
| Dosage: |
200 mg/kg |
| Administration: |
Oral gavage; daily for 4 weeks after induced |
| Result: |
Protected liver from accumulated bile acid-induced injury.
Increased the expression of FXR and decreased the expression of NTCP in BDL rats. |
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| 分子量 |
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| Formula |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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