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GW501516 is subtype-selective small-molecule agonist of peroxisome proliferator-activated receptor δ (PPARδ) with Ki value of 1.1nM [1].

GW501516 is discovered by combinatorial chemistry and structure-based drug design to use as an ideal chemical tool to study the function of the ubiquitously expressed PPARδ. In the cell-based transfection assay, it induces expression of a GAL4-responsive reporter gene with EC50 value of 1.2nM. GW501516 shows more than 1000-fold selective for PPARδ over other subtypes. PPARδ is expressed in many tissues that contribute to cholesterol flux, and is a RXR of partner. As an agonist of PPARδ, GW501516 is found to increase the expression of ABCA1 as well as the apoA1-specific cholesterol efflux. In primate model of human metabolic disease, GW501516 increases the level of HDLc and lowers the fasting triglycerides. GW501516 also produces fewer, yet larger, LDL and VLDL particles results in a less atherogenic lipid composition. Furthermore, GW501516 partially corrects the hyperinsulinemia in primates without adverse effects on glycemic control [1, 2

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