| In Vitro | In vitro activity: Elafibranor (also known as GFT505) is being developed as a dual PPAR-α/PPAR-δ agonist for the treatment of T2DM and non-alcoholic fatty liver disease. GFT505 has an active metabolite, GFT1007, and both have potent agonist activity for PPAR-α and to a lesser extent for PPAR-δ
Kinase Assay: Elafibranor is a PPARα/δ agonist with EC50s of 45 and 175 nM, respectively. GFT505 is being developed as a dual PPAR-α/PPAR-δ agonist for the treatment of T2DM and non-alcoholic fatty liver disease. GFT505 has an active metabolite, GFT1007, and both have potent agonist activity for PPAR-α and to a lesser extent for PPAR-δ. |
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| In Vivo | Elafibranor (also known as 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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| Animal model | hApoE2 KI and hApoE2 KI/PPAR-α KO mice |
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| Formulation & Dosage | Formulated in 0.1% Tween 80 and 1% carboxymethyl cellulose in 98.9% distilled water; 30 mg/kg; P.O. |
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| References | Gastroenterology. 2016 May;150(5):1147-1159.e5; Expert Opin Investig Drugs. 2015 May;24(5):611-21. |
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