Network Version
Elafibranor Data Sheet
| Product Name: | Elafibranor |
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|---|---|---|
| CAS No.: | 923978-27-2 | |
| Cat. No.: | HY-16737 | |
| MWt: | 384.49 | |
| Formula: | C22H24O4S | |
| Purity : | >98% | |
| Solubility: | DMSO : ≥ 33 mg/mL | |
| Mechanisms: | Target: Inflammation/Immunology Metabolic Disease | |
| Biological Activity: | ||
| Elafibranor (GFT505) is a PPARα/δ agonist with EC50s of 45 and 175 nM, respectively. Elafibranor can be used for the study of primary biliary cholangitis[1]. IC50 & Target:EC50: 45 nM (PPAR-α), 175 nM (PPAR-δ)[1] In Vitro:Elafibranor (GFT505) is being developed as a dual PPAR-α/PPAR-δ agonist for the inhibition of T2DM and non-alcoholic fatty liver disease. Elafibranor has an active metabolite, GFT1007, and both have potent agonist activity for PPAR-α and to a lesser extent for PPAR-δ[1]. In Vivo:Elafibranor is well tolerated and does not cause weight gain or cardiac events, but does produce a mild, reversible increase in serum creatinine. Elafibranor improves glucose homeostasis, and lipid metabolism and reduces inflammation[2]. Elafibranor (GFT505) treatment improves glucose control and plasma lipids in diabetic db/db mice. A significant dose-dependent reduction of hepatic expression of the key gluconeogenic enzymes glucose 6-phosphatase (G6Pase), PEPCK, and fructose 1,6-bisphosphatase 1 (FBP1) is observed with Elafibranor. Elafibranor does not induce cardiac adverse effects of PPARγ-activating agonists in monkeys[3]. | ||
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