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Elafibranor

Elafibranor (GFT505) 是过氧化物酶体增殖物激活受体-α (PPAR-α) 和过氧化物酶体增殖物激活受体-δ (PPAR-δ) 的激动剂，EC50 值分别为 45 和 175 nM。

CAS号

923978-27-2

分子式

C22H24O4S

主要靶点

PPAR

仅限科研使用

Cat No : CM06120

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Synonyms

GFT505

验证数据展示

  • CAS No.: 923978-27-2

    Elafibranor
    CAS#: 923978-27-2

产品信息

Elafibranor is an agonist of the peroxisome proliferator-activated receptor-α (PPAR-α) and peroxisome proliferator-activated receptor-δ (PPAR-δ) with EC50 values of 45 and 175 nM, respectively.

CAS号 923978-27-2
分子式 C22H24O4S
主要靶点 PPAR
主要通路 DNA损伤和修复|代谢
分子量 384.49
纯度 99.50%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 GFT505

靶点活性

PPAR-δ:175 nM (EC50)|PPAR-α:45 nM (EC50)

体内活性

GFT505 improves insulin sensitivity and early studies indicate it may be useful in non-alcoholic fatty liver disease which is being tested in a Phase IIb study. 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 insulin sensitivity, glucose homeostasis, and lipid metabolism and reduces inflammation. 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 GFT505. GFT505 does not induce cardiac adverse effects of PPARγ-activating agonists in monkeys

体外活性

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

溶解度

DMSO:33 mg/mL

参考文献

1.Liu ZM,etal.Early investigational drugs targeting PPAR-α for the treatment of metabolic disease.Expert Opin Investig Drugs. 2015 May;24(5):611-21.
2.Ratziu V,etal.Elafibranor, an Agonist of the Peroxisome Proliferator-Activated Receptor-α and -δ, Induces Resolution of Nonalcoholic Steatohepatitis Without Fibrosis Worsening. Gastroenterology. 2016 May;150(5):1147-1159.
3.Hanf R,etal.The dual peroxisome proliferator-activated receptor alpha/delta agonist GFT505 exerts anti-diabetic effects in db/db mice without peroxisome proliferator-activated receptor gamma-associated adverse cardiac effects.Diab Vasc Dis Res. 2014 Nov;11(6):440-7.

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