| 产品描述： | Elafibranor (GFT505) 是PPAR-alpha和PPAR-δ的激动剂，改善胰岛素敏感度、有益于葡萄糖稳态、脂质代谢并减少炎症 |
| 靶点： |
PPARα; PPARδ ;PPAR |
| 体外研究： |
GFT505 is a novel PPAR modulator that shows a preferential activity on PPAR-α and concomitant activity on PPAR-δ |
| 体内研究： |
Elafibranor (GFT505) is a dual PPARα/δ agonist that has demonstrated efficacy in disease models of nonalcoholic fatty liver disease (NAFLD)/NASH and liver fibrosis. In the rat, GFT505 concentrated in the liver with limited extrahepatic exposure and underwent extensive enterohepatic cycling. Elafibranor confers liver protection by acting on several pathways involved in NASH pathogenesis, reducing steatosis, inflammation, and fibrosis. GFT505 improved liver dysfunction markers, decreased hepatic lipid accumulation, and inhibited proinflammatory (interleukin-1 beta, tumor necrosis factor alpha, and F4/80) and profibrotic (transforming growth factor beta, tissue inhibitor of metalloproteinase 2, collagen type I, alpha 1, and collagen type I, alpha 2) gene expression |
| 细胞实验： |
Cell lines: hSKP-HPCs Concentrations: 30 µM Incubation Time: 24 h Method: Cells were treated with indicated concentration of drug for 24 h. |
| 动物实验： |
Animal Models: hApoE2 KI and hApoE2 KI/PPAR-α KO mice Dosages: 30 mg/kg Administration: oral gavage |
| 参考文献： |
1. Ratziu V, et al. Elafibranor, an Agonist of the Peroxisome Proliferator-Activated Receptor-α and -δ, Induces Resolution of Nonalcoholic Steatohepatitis Without Fibrosis Worsening. Gastroenterology. 2016, 150(5):1147-1159.e5. 2. Staels B, et al. Hepatoprotective effects of the dual peroxisome proliferator-activated receptor alpha/delta agonist, GFT505, in rodent models of nonalcoholic fatty liver disease/nonalcoholic steatohepatitis. Hepatology. 2013, 58(6):1941-52. 3. Boeckmans J, et al. Elafibranor restricts lipogenic and inflammatory responses in a human skin stem cell-derived model of NASH. Pharmacol Res. 2019 Jun;144:377-389. |
| 溶解性： |
Soluble in DMSO、Ethanol |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.601 ml |
13.004 ml |
26.009 ml |
| 5 mM |
0.52 ml |
2.601 ml |
5.202 ml |
| 10 mM |
0.26 ml |
1.3 ml |
2.601 ml |
| 50 mM |
0.052 ml |
0.26 ml |
0.52 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京