产品描述:
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 γ-coactivator 1α (PGC-1α) to this class of receptors is known to potentiate ERR activity.{12071} GSK4716 is an ERRβ/γ agonist (IC50 = 2 µM) that can activate the receptor with similar potency as the protein ligand, PGC-1α.{28181} It is more than 50-fold selective for binding to ERRβ/γ compared with the estrogen receptors.{28181} This compound has been used to demonstrate the contribution of ERR receptor activity to the regulation of mitochondrial activity in skeletal muscle during exercise.{28182}