tcsc0438 GW 501516

GW 501516 is a PPARδ agonist with an EC₅₀ of 1.1 nM.

IC50 & Target: EC50: 1.1 nM (PPARδ)^[1]

In Vitro: GW 501516 is shown to be the most potent and selective PPARα agonists known with an EC₅₀ of 1.1 nM against PPARα and 1000-fold selectivity over the other human subtypes, PPARα and-γ^[1]. GW 501516 exerts anti-inflammatory effects in mouse cultured proximal tubular (mProx) cells. GW 501516 inhibits palmitate- and TNFα-induced increases in MCP-1 mRNA expression in a dose-dependent manner^[3].

In Vivo: GW 501516 causes impaired bone formation, leading to decreased BMD and deterioration of bone properties in OVX rats^[2]. GW 501516 attenuates interstitial inflammation and proximal tubular cell damage in a protein-overload mouse nephropathy model^[3]. GW 501516 treatment enhances running endurance and the proportion of succinate dehydrogenase (SDH)-positive muscle fibres in both trained and untrained mice^[4].