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Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis.

P J Brown·L W Stuart·K P Hurley·M C Lewis·D A Winegar·J G Wilson·W O Wilkison·O R Ittoop·T M Willson
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Abstract

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.

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AnimalsButyratesCricetinaeDietary FatsDrug DesignHyperlipidemiasHypolipidemic AgentsPhenylurea CompoundsReceptors, Cytoplasmic and NuclearTranscription FactorsJournal Article

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P J Brown, L W Stuart, K P Hurley, M C Lewis, D A Winegar, J G Wilson, W O Wilkison, O R Ittoop, T M Willson. 2001-05-07. Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis.. https://doi.org/10.1016/s0960-894x(01)00188-3

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