Elafibranor
产品说明书
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同义名 : | - |
| CAS号 : | 923978-27-2 | |
| 货号 : | A118286 | |
| 分子式 : | C22H24O4S | |
| 纯度 : | 95% | |
| 分子量 : | 384.489 | |
| MDL号 : | MFCD27987940 | |
| 存储条件： |
Pure form Sealed in dry,2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 35 mg/mL(91.03 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 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Elafibranor, also known as GFT505, is a dual agonist of peroxisome proliferator-activated receptor-α/δ (PPAR-α/δ) with EC50 values of 45 and 175nM, respectively[3]. Treatment of hApoE2 KI mice with Elafibranor (30 mg/kg/day) for 6 weeks significantly decreased the plasma concentrations of total cholesterol, triglycerides, and free fatty acids, and greatly increased the level of high-density lipoprotein cholesterol compared to vehicle-treated group. In both hApoE2 KI and hApoE2 KI/PPAR‐α KO mice, Elafibranor treatment significantly reduced hepatic expressions of interleukin‐1β, tumor necrosis factor‐α, transforming growth factor‐β, and tissue inhibitor of metalloproteinase-2. Methionine- and choline-deficient diet induced steatohepatitis in db/db mice, whereas supplementation with Elafibranor (1, 3, or 10 mg/kg/day) for 7 weeks reduced intrahepatic cholesterol and triglyceride content in a dose‐dependent manner. In SD rats concomitantly injected with CCl4 and treated with Elafibranor (30 mg/kg/day) for 7 weeks, the fibrotic surface and hepatic collagen content were significantly decreased, and the number of macrophages and activated hepatic stellate cells were significantly reduced as compared to CCl4 control group[4]. | ||
| 作用机制 | Elafibranor is a PPAR-α/δ agonist that exhibits liver-protective effects in non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, and liver fibrosis. It has also been shown to reduce fasting glucose and improve insulin sensitivity similar to PPAR-γ agonist rosiglitazone. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.60mL 0.52mL 0.26mL |
13.00mL 2.60mL 1.30mL |
26.01mL 5.20mL 2.60mL |
| 参考文献 |
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