101574-65-6

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. GSK4716 is an ERRβ/γ agonist (IC₅₀ = 2 μM) that can activate the receptor with similar potency as the protein ligand, PGC-1α. It is more than 50-fold selective for binding to ERRβ/γ 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.

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. GSK4716 is an ERRβ/γ agonist (IC50 = 2 μM) that can activate the receptor with similar potency as the protein ligand, PGC-1α. It is more than 50-fold selective for binding to ERRβ/γ 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.[Cayman Chemical]

ChEBI:GSK 4716 is a monoterpenoid.

Selective agonist at estrogen-related receptors ERR β and ERR γ . Displays selectivity over ERR α and the classical estrogen receptors.

Store at -20°C

[1] LIPING WANG. X-ray crystal structures of the estrogen-related receptor-gamma ligand binding domain in three functional states reveal the molecular basis of small molecule regulation.[J]. The Journal of Biological Chemistry, 2006: 37773-37781. DOI: 10.1074/jbc.m608410200
[2] SHAMINA M RANGWALA. Estrogen-related receptor gamma is a key regulator of muscle mitochondrial activity and oxidative capacity.[J]. The Journal of Biological Chemistry, 2010, 285 29: 22619-22629. DOI: 10.1074/jbc.m110.125401