产品
编 号:F522199
分子式:C22H24O4S
分子量:384.49
产品类型
结构图
CAS No: 923978-27-2
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产品详情
生物活性:
Elafibranor (GFT505) is a PPARα/δ agonist with EC50s of 45 and 175 nM, respectively.
体内研究:
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.
体外研究:
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.