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

ABSTRACT: A novel peroxisome proliferator-activated receptor (PPAR) ?/? dual agonist 5c was developed with an EC50 of 8 nM for PPAR?, 5 nM for PPAR?, and >300-fold selectivity against PPAR? (EC50 = 2939 nM), respectively. Further ADME and pharmacokinetic studies indicated 5c possessed distinguished in vitro and in vivo profiles. The excellent in vivo efficacy of compound 5c was demonstrated by the rat primary biliary cirrhosis (PBC) model.

SUBMITTER: Jiang Z 

PROVIDER: S-EPMC6627728 | biostudies-literature | 2019 Jul

REPOSITORIES: biostudies-literature

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

Jiang Zhigan Z   Liu Xing X   Yuan Zhiliang Z   He Haiying H   Wang Jing J   Zhang Xiao X   Gong Zhen Z   Hou Lijuan L   Shen Liang L   Guo Fengxun F   Zhang Jiliang J   Wang Jianhua J   Xu Deming D   Liu Zhuowei Z   Li Haijun H   Chen Xiaoxin X   Long Chaofeng C   Li Jian J   Chen Shuhui S  

ACS medicinal chemistry letters 20190624 7

A novel peroxisome proliferator-activated receptor (PPAR) α/δ dual agonist <b>5c</b> was developed with an EC<sub>50</sub> of 8 nM for PPARα, 5 nM for PPARδ, and >300-fold selectivity against PPARγ (EC<sub>50</sub> = 2939 nM), respectively. Further ADME and pharmacokinetic studies indicated <b>5c</b> possessed distinguished <i>in vitro</i> and <i>in vivo</i> profiles. The excellent <i>in vivo</i> efficacy of compound <b>5c</b> was demonstrated by the rat primary biliary cirrhosis (PBC) model. ...[more]

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