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GW501516 is a selective agonist of the PPARδ receptor that displays high affinity and potency for PPARδ with > 1,000 fold selectivity over PPARα and PPARγ. In rats, binding of GW501516 to PPARδ recruits the coactivator PGC-1α . It was initially discovered during a research collaboration between GSK and Ligand Pharmaceuticals that began in 1992 The drug entered into clinical development as a drug candidate for metabolic and cardiovascular diseases, but was abandoned in 2007 because animal testing showed that the drug caused cancer to develop rapidly in several organs
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