Formulation: A solid
Formal Name: 4-[1-(2-propen-1-yl)-7-(trifluoromethyl)-1H-indazol-3-yl]-1,3-benzenediol
Purity: ≥98%
Formula Markup: C17H13F3N2O2
Formula Weight: 334,3
Shelf life (days): 1460
CAS Number: 669764-18-5
Notes: WAY-169916 is a pathway-selective estrogen receptor (ER) ligand.{67096} It binds to human ERα and ERβ (IC50 = 3 nM for both) and inhibits IL-1β-induced NF-κB reporter activity in HAECT-1 cells expressing human ERα (IC50 = 93 nM), but not cells lacking ER expression, when used at concentrations up to 10 µM. WAY-169916 (1 µM) reduces increases in creatine kinase (CK) activity induced by the ER agonist 17β-estradiol (Item No. 10006315) in HAECT-1 cells. In vivo, WAY-169916 (10 mg/kg per day) reduces high-fat diet-induced hepatic NF-κB activity and inflammatory gene expression without increasing uterine weight in ovariectomized rats. It inhibits chronic diarrhea, as well as intestinal ulceration and inflammatory cell infiltration, in an HLA-B27 transgenic rat model of inflammatory bowel disease (IBD). WAY-169916 (1 mg/kg) reduces infarct size in an ovariectomized rabbit model of coronary artery occlusion-induced ischemia and reperfusion injury.{67097}
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