A selective agonist for PPARδ (peroxisome proliferator-activated receptorδ) (EC50 = 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. MW: 453.5. Purity ≥98% by HPLC