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Elafibranor
- GFT505
- Soluble in 0.1N NaOH(aq) and DMSO
- MF: C22H24O4S
- MW: 384.49
Description
The dual PPARα/δ agonist Elafibrinor (GFT505) (EC50 values of 45 nM and 175 nM for PPARα and PPARδ, respectively) is a liver-targeted insulin-sensitizer that is a drug candidate for the treatment of type 2 diabetes, nonalcoholic fatty liver disease (NAFLD) and nonalcoholic steatohepatitis (NAS). In animals, its protective effects are mediated by both PPAR-α-dependent and -independent mechanisms.
More Information
| Parent CAS No. | 923978-27-2 |
|---|---|
| Chemical Name | (E)-2-(2,6-Dimethyl-4-(3-(4-(methylthio)phenyl)-3-oxoprop-1-enyl)phenoxy)-2-methylpropanoic acid |
| SMILES | C1C=C(C(=O)/C=C/C2C=C(C)C(OC(C)(C)C(=O)O)=C(C)C=2)C=CC=1SC |
| MFCD | N.A. |
| InChi | InChI=1S/C22H24O4S/c1-14-12-16(13-15(2)20(14)26-22(3,4)21(24)25)6-11-19(23)17-7-9-18(27-5)10-8-17/h6-13H,1-5H3,(H,24,25)/b11-6+ |
| InChiKey | AFLFKFHDSCQHOL-IZZDOVSWSA-N |
| CID | 9864881 |
| Short Description | PPAR α/δ agonist |
References
- B Cariou et al. Effects of the new dual PPAR α/δ agonist GFT505 on lipid and glucose homeostasis in abdominally obese patients with combined dyslipidemia or impaired glucose metabolism. Diabetes Care. 2011 Sep;34(9):2008-14.
- B Cariou et al. Dual Peroxisome Proliferator–Activated Receptor α/δ Agonist GFT505 Improves Hepatic and Peripheral Insulin Sensitivity in Abdominally Obese Subjects. Diabetes Care. 2013 Oct; 36(10): 2923–2930.
- B Staels 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 Dec;58(6):1941-52.
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