Discovery of a Novel Selective Dual Peroxisome Proliferator-Activated Receptor α/δ Agonist for the Treatment of Primary Biliary Cirrhosis.

Zhigan Jiang,Xing Liu,Zhiliang Yuan,Haiying He,Jing Wang,Xiao Zhang,Zhen Gong,Lijuan Hou,Liang Shen,Fengxun Guo,Jiliang Zhang,Jianhua Wang,Deming Xu,Zhuowei Liu,Haijun Li,Xiaoxin Chen,Chaofeng Long,Jian Li,Shuhui Chen

ACS medicinal chemistry letters（2019）

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摘要

A novel peroxisome proliferator-activated receptor (PPAR) α/δ dual agonist was developed with an EC of 8 nM for PPARα, 5 nM for PPARδ, and >300-fold selectivity against PPARγ (EC = 2939 nM), respectively. Further ADME and pharmacokinetic studies indicated possessed distinguished and profiles. The excellent efficacy of compound was demonstrated by the rat primary biliary cirrhosis (PBC) model.

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关键词

Peroxisome proliferator-activated receptor (PPAR),dual agonist,primary biliary cirrhosis (PBC)

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