Potent and selective PPARdelta (NR1C2) agonist, EC50=1.2 nM and 1000-fold selective over other PPAR subtypes.1 Induces apolipoprotein A1-mediated cholesterol efflux in vitro.1 Improves hematopoietic stem cell maintenance.2 Prevents downregulation of AMPK caused by a high-fat diet in liver and increases fatty acid oxidation.3 Upregulates human Sirt1 via Sp1 activation.4 Along with exercise, GW-501516 synergistically increases running endurance.5
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