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Pemafibrate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Pemafibrate图片
CAS NO:848259-27-8
规格:98%
分子量:490.55
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
Pemafibrate is a potent PPARα agonist, with EC50s of 1 nM, 1.10 uM and 1.58 uM for h-PPARα, h-PPARγ and h-PPARδ, respectively, and possesses lipid-lowering effect.
CAS:848259-27-8
分子式:C28H30N2O6
分子量:490.55
纯度:98%
存储:Store at -20°C

Background:

Pemafibrate is a potent PPARα agonist, with EC50s of 1 nM, 1.10 uM and 1.58 uM for h-PPARα, h-PPARγ and h-PPARδ, respectively, and possesses lipid-lowering effect.


Pemafibrate is a potent PPARα agonist, with EC50s of 1 nM, 1.10 uM and 1.58 uM for h-PPARα, h-PPARγ and h-PPARδ, respectively. Pemafibrate is more than 1000 fold selective towards PPARα than PPARγ and PPARδ[1].


Pemafibrate (3 mg/kg, p.o.) increases plasma h-apoA-I in human apoA-I (h-apoA-I) transgenic mice, and shows higher levels of plasma h-apoA-I than fenofibrate at 300 mg/kg[1]. Pemafibrate (0.03 mg/kg) decreases levels of triglycerides and aspartate aminotransferase (AST) in PEMA-L (db/db) mice. Pemafibrate (0.1 mg/kg) not only shows such effects but increases liver weight in PEMA-H (db/db) mice. Pemafibrate enhances the pathogenesis in a rodent model of nonalcoholic steatohepatitis (NASH). Pemafibrate significantlly reduces the grade of hepatocyte ballooning in PEMA-H mice. Furthermore, Pemafibrate modulates lipid turnover and induces uncoupling protein 3 (UCP 3) expression in the liver[2]. Pemafibrate (K-877, 0.0005%) contained in high-fat diet (HFD) inhibits the body weight gain in mice. Pemafibrate significantly decreases the abundance of triglyceride (TG)-rich lipoproteins, including remnants, in postprandial plasma of mice. Pemafibrate also decreases intestinal mRNA expression of ApoB and Npc1l1[3].


参考文献:
[1]. Yamazaki Y, et al. Design and synthesis of highly potent and selective human peroxisome proliferator-activated receptor alpha agonists. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4689-93. Epub2007 May 24.
[2]. Honda Y, et al. Pemafibrate, a novel selective peroxisome proliferator-activated receptor alpha modulator, improves the pathogenesis in a rodent model of nonalcoholic steatohepatitis. Sci Rep. 2017 Feb 14;7:42477.
[3]. Sairyo M, et al. A Novel Selective PPARα Modulator (SPPARMα), K-877 (Pemafibrate), Attenuates Postprandial Hypertriglyceridemia in Mice. J Atheroscler Thromb. 2018 Feb 1;25(2):142-152.