Purity >98%. The estrogen-related receptors (ERRs) are orphan nuclear receptors with homology to the estrogen receptor family and are expressed in tissues with high metabolic demand. Binding of peroxisome proliferator-activated receptor Gamma-coactivator 1Alpha (PGC-1Alpha) to this class of receptors is known to potentiate ERR activity. GSK4716 is an ERRBeta/Gamma agonist (IC50 = 2 μM) that can activate the receptor with similar potency as the protein ligand, PGC-1Alpha. It is more than 50-fold selective for binding to ERRBeta/Gamma compared with the estrogen receptors. This compound has been used to demonstrate the contribution of ERR receptor activity to the regulation of mitochondrial activity in skeletal muscle during exercise.