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Elafibranor
- GFT505
- Soluble in 0.1N NaOH(aq) and DMSO
- MF: C22H24O4S
- MW: 384.49
Description
Elafibranor (GFT505) is an orally active dual agonist of PPARα and PPARδ, with reported EC50 values of 45 nM and 175 nM, respectively. Activation of these nuclear receptors modulates transcriptional programs involved in fatty-acid oxidation, lipid handling, glucose homeostasis and inflammatory signaling.
Elafibranor is used to investigate metabolic and hepatic PPAR biology in cellular and animal models, including insulin resistance, dyslipidemia, hepatic steatosis and steatohepatitis. Its effects can involve both PPARα-dependent and additional pathway components, so receptor-specific controls are valuable when interpreting complex in vivo responses.
Key Features
- Dual PPARα/PPARδ agonist
- EC50: 45 nM for PPARα and 175 nM for PPARδ
- Orally active metabolic modulator
- Regulates lipid oxidation and inflammatory pathways
Applications
- PPARα and PPARδ research
- Lipid and glucose metabolism studies
- Fatty-acid oxidation assays
- Hepatic steatosis and steatohepatitis models
- Insulin-sensitivity research
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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