GSK4716

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.Formal Name: 4-hydroxy-2-[[4-(1-methylethyl)phenyl]methylene]hydrazide benzoic acid. CAS Number: 101574-65-6. Molecular Formula: C17H18N2O2. Formula Weight: 282.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 16 mg/ml, Ethanol: 20 mg/ml, Ethanol:PBS (pH 7.2) (1:6): 0.14 mg/ml. lambdamax: 220, 309 nm. SMILES: OC1=CC=C(C(N/N=C/C2=CC=C(C(C)C)C=C2)=O)C=C1. InChi Code: InChI=1S/C17H18N2O2/c1-12(2)14-5-3-13(4-6-14)11-18-19-17(21)15-7-9-16(20)10-8-15/h3-12,20H,1-2H3,(H,19,21)/b18-11+. InChi Key: IKPPIUNQWSRCOZ-WOJGMQOQSA-N.