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Elafibranor

CAS No. : 923978-27-2

MCE 国际站：Elafibranor

产品活性：Elafibranor (GFT505) 是 PPARα/δ 的激动剂，EC₅₀ 分别为 45 和 175 nM。

研究领域：Cell Cycle/DNA Damage  |  Vitamin D Related/Nuclear Receptor

作用靶点：PPAR

In Vitro: Elafibranor (GFT505) is being developed as a dual PPAR-α/PPAR-δ agonist for the treatment 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.

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. 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.

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