Elafibranor|923978-27-2|(GFT505)-陌孚医药/Medlife

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Elafibranor (Synonyms: GFT505)

目录号: PL10066 纯度: ≥99%

CAS No. :923978-27-2

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中文名称	Elafibranor
中文别名	GFT505;2-[2,6-二甲基-4-[(1E)-3-[4-(甲硫基)苯基]-3-氧代-1-丙烯-1-基]苯氧基]-2-甲基丙酸
英文名称	Elafibranor
英文别名	GFT505;elafibranor E;GFT-505;Elafibranor(GFT505);Elafibranor;Elafibranor [USAN];2J3H5C81A5;Elafibranor (USAN);(E)-2-(2,6-dimethyl-4-(3-(4-(methylthio)phenyl)-3-oxoprop-1-enyl)phenoxy)-2-methylpropanoic acid;Elafibranor [INN];GFT 505;2-[2,6-dimethyl-4-[(E)-3-(4-methylsulfanylphenyl)-3-oxoprop-1-enyl]phenoxy]-2-methylpropanoic acid;BCP19067;s3720;DB05187;SB16790;(E)-2-(2,6-dimethyl-4-(3-(4-(methylthio)phenyl)-3-oxoprop-1-en-1-yl)phenoxy)-2-methylpropanoic acid;2-{2,6-dimethyl-4-[(1E)-3-[4-(methylsulfanyl)phenyl]-3-oxoprop-1-en-1-yl]phenoxy}-2-methylpropanoic acid;SureCN815512;S;2-[2,6-Dimethyl-4-[(1E)-3-[4-(methylthio)phenyl]-3-oxo-1-propen-1-yl]phenoxy]-2-methylpropanoic acid (ACI);(E)-1-[4-(Methylthio)phenyl]-3-[3,5-dimethyl-4-[(carboxydimethylmethyl)oxy]phenyl]prop-2-en-1-one
Cas No.	923978-27-2
分子式	C₂₂H₂₄O₄S
分子量	384.49
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

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

生物活性

Elafibranor (GFT505) is a PPARα/δ agonist with EC 50 s of 45 and 175 nM, respectively.

性状

Solid

IC50 & Target[1][2]

PPAR-α 45 nM (EC50) PPAR-δ 175 nM (EC

体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Liu ZM, et al. 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, et al. 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.

溶解度数据	In Vitro: DMSO : ≥ 33 mg/mL (85.83 mM)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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