A selective agonist for PPAR (peroxisome proliferator-activated receptor) (EC= 1. 1 nM), displaying 1000-fold selectivity over the other human subtypes. In macrophages, fibroblasts, and intestinal cells, GW501516 increases expression of the reverse cholesterol transporter ATP-binding cassette A1 and induces apolipoprotein A1-specific cholesterol efflux.
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