Identification of a subtype selective human PPARα agonist through parallel-array synthesis
Copyright policy )Identification of a subtype selective human PPARα agonist through parallel-array synthesis
Using solid-phase, parallel-array synthesis, a series of urea-substituted thioisobutyric acids was synthesized and assayed for activity on the human PPAR subtypes. GW7647 (3) was identified as a potent human PPARalpha agonist with approximately 200-fold selectivity over PPARgamma and PPARdelta, and potent lipid-lowering activity in animal models of dyslipidemia. GW7647 (3) will be a valuable chemical tool for studying the biology of PPARalpha in human cells and animal models of disease.
- Research Triangle Park Foundation United States
- GlaxoSmithKline (United States) United States
Phenylurea Compounds, Receptors, Cytoplasmic and Nuclear, Hyperlipidemias, Dietary Fats, Butyrates, Cricetinae, Drug Design, Animals, Hypolipidemic Agents, Transcription Factors
Phenylurea Compounds, Receptors, Cytoplasmic and Nuclear, Hyperlipidemias, Dietary Fats, Butyrates, Cricetinae, Drug Design, Animals, Hypolipidemic Agents, Transcription Factors
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