Shelf life (days): 1460.0
Formulation: A solid
Formal Name: dZ-[[4-[2-(dimethylamino)ethoxy]phenyl](4-hydroxyphenyl)methylene]-benzenebutanol
Purity: ≥95%
Formula Markup: C27H31NO3
Formula Weight: 417.5
CAS Number: 877387-37-6
Notes: GSK5182 is an inverse agonist of estrogen-related receptor γ (ERRγ; IC50 = 77 nM in a reporter assay) and a derivative of (Z)-4-hydroxy tamoxifen (Item No. 14854).{68867} It selectively binds to ERRγ over ERα, ERRα, and ERRβ (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.{68868} 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.{68869} GSK5182 (10 µM) inhibits fibrinogen secretion induced by the cannabinoid 1 (CB1) receptor agonist ACEA (arachidonoyl 2'-chloroethylamide; Item No. 91054) in AML12 hepatocytes.{68870} 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.{68871}
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