GW501516 is a selective PPARd agonist with a Ki affinity of 1.1 nM in a human binding assay. In a cell-based transfection assay, GW501516 induces expression of GAL4-responsive reporter gene at an EC50 of 1.2 nM. At doses up to 1 uM, GW501516 does not promote adipocyte differentiation, bind to RXRa, or have activity toward other nuclear or non-nuclear receptors. (1) GW501516 incrases expression of the reverse cholesterol transporter ATP-binding cassette A1 and induces apolipoprotein A1-specific cholesterol efflux. (1)

GW501516 is also reported to be a PPARb agonist with anti-inflammatory activity and decreases IFN-g-induced upregulation of TNF-a and iNOS. Concurrently, GW501516 increase IL-6 mRNA expression. (2)