GW501516 is a selective agonist (activator) of the PPARδ receptor. It displays high affinity (Ki = 1 nM) and potency (EC50 = 1 nM) for PPARδ with > 1,000 fold selectivity over PPARα and PPARγ. In rats, binding of GW501516 to PPARδ recruits the coactivator PGC-1α. The PPARδ/co-activator complex in turn up regulates the expression of proteins involved in energy expenditure. Furthermore, in rats treated with GW501516, increased fatty acid metabolism in skeletal muscle and protection against diet-induced obesity and type II diabetes was observed. In obese rhesus monkeys, GW501516 increased high-density lipoprotein (HDL) and lowered very-low-density lipoprotein (VLDL).
Molar Mass: 453.498 g/mol