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- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥3965.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥1300.0 |
| 规格： | 5 mg | 产品价格： | ￥3450.0 |
| 规格： | 10 mg | 产品价格： | ￥5520.0 |
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FXR agonist 3
MCE 国际站：FXR agonist 3
产品活性：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。
研究领域：Metabolic Enzyme/Protease
作用靶点：FXR
In Vitro: 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
| 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 |
In Vivo: 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.
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.
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三句话读懂一篇 CNS：颜宁团队 2023 首个研究成果发表；长期单身，患老年痴呆风险更高
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