Information Elafibranor (GFT505) is an agonist of theperoxisome proliferator-activated receptor-α(PPAR-alpha)andperoxisome proliferator-activated receptor-δ(PPAR-δ). It improves insulin sensitivity, glucose homeostasis, and lipid metabolism and reduces inflammation. Targets PPARα ; PPARδ In vitro GFT505 is a novel PPAR modulator that shows a preferential activity on PPAR-α and concomitant activity on PPAR-δ. In vivo 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.
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Elafibranor
CAS number：923978-27-2 molecular formula：C22H24O4S
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| Chinese alias | - | ||
| English alias | BIM-0018283.P001 | CHEBI:31581 | AS-57112 | 4-(2-acetamino-ethyl)-phenol | CCG-268462 | Elafibranor | ZHB93288 | 2-[2,6-dimethyl-4-[(~{E})-3-(4-methylsulfanylphenyl)-3-oxidanylidene-prop-1-enyl]phenoxy]-2-methyl-propanoic acid | Q15409440 | s3720 | D11208 | ||
| CAS number | 923978-27-2 | molecular formula | C22H24O4S |
| molecular weight | 384.49 g/mol | Exact mass | - |
| PSA | 88.900 Ų | logp | 5.477 |
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