Abstract:
:A novel peroxisome proliferator-activated receptor (PPAR) α/δ dual agonist 5c was developed with an EC50 of 8 nM for PPARα, 5 nM for PPARδ, and >300-fold selectivity against PPARγ (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.
journal_name
ACS Med Chem Lettjournal_title
ACS medicinal chemistry lettersauthors
Jiang Z,Liu X,Yuan Z,He H,Wang J,Zhang X,Gong Z,Hou L,Shen L,Guo F,Zhang J,Wang J,Xu D,Liu Z,Li H,Chen X,Long C,Li J,Chen Sdoi
10.1021/acsmedchemlett.9b00189subject
Has Abstractpub_date
2019-06-24 00:00:00pages
1068-1073issue
7issn
1948-5875journal_volume
10pub_type
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