Agonist API GW501516 white powder

GW 501516 is an agonist of PPARδ with EC50 value of 1.1 nM.
GW501516 is shown to be the most potent and selective PPARα agonists known with an EC 50 of 1. 1 nM against PPARα and 1000-fold selectivity over the other human subtypes, PPARα and -γ. GW501516 exerts anti-inflammatory effects in mouse cultured proximal tubular (mProx)cells. GW501516 inhibits palmitate- and TNFα-induced increases in MCP-1 mRNA expression in a dose-dependent manner.
GW501516 causes impaired bone formation, leading to decreased BMD and deterioration of bone properties in OVX rats. GW501516 attenuates interstitial inflammation and proximal tubular cell damage in a protein-overload mouse nephropathy model. GW501516 treatment enhances running endurance and the proportion of succinate dehydrogenase (SDH)-positive muscle fibres in both trained and untrained mice.