GSK5182

GSK5182 is an inverse agonist of estrogen-related receptor gamma (ERRgamma, IC50 = 77 nM in a reporter assay) and a derivative of (Z)-4-hydroxy tamoxifen (Cay-14854). It selectively binds to ERRgamma over ERalpha, ERRalpha, and ERRbeta (IC50s = 0.11, 2, >10, and >10 µM, respectively). GSK5182 enhances radioiodine uptake and membrane localization of the sodium/iodide symporter (NIS) in BHT-101 and CAL-62 anaplastic thyroid cancer cells. It inhibits osteoclastogenesis induced by RANKL and macrophage colony-stimulating factor (M-CSF) in primary mouse bone marrow-derived macrophages (BMDMs) and induces apoptosis in osteoclasts when used at a concentration of 10 µM. GSK5182 (10 µM) inhibits fibrinogen secretion induced by the cannabinoid 1 (CB1) receptor agonist ACEA (arachidonoyl 2'-chloroethylamide, Cay-91054) in AML12 hepatocytes. In vivo, GSK5182 (40 mg/kg) decreases blood glucose levels in a pyruvate tolerance test in a mouse model of high-fat diet-induced obesity.Formal Name: deltaZ-[[4-[2-(dimethylamino)ethoxy]phenyl](4-hydroxyphenyl)methylene]-benzenebutanol. CAS Number: 877387-37-6. Molecular Formula: C27H31NO3. Formula Weight: 417.5. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Sparingly soluble: 1-10 mg/ml, Ethanol: Slightly soluble: 0.1-1 mg/ml. SMILES: OC1=CC=C(/C(C2=CC=C(OCCN(C)C)C=C2)=C(CCCO)/C3=CC=CC=C3)C=C1. InChi Code: InChI=1S/C27H31NO3/c1-28(2)18-20-31-25-16-12-23(13-17-25)27(22-10-14-24(30)15-11-22)26(9-6-19-29)21-7-4-3-5-8-21/h3-5,7-8,10-17,29-30H,6,9,18-20H2,1-2H3/b27-26-. InChi Key: ZVSFNBNLNLXEFQ-RQZHXJHFSA-N.