WAY-169916

WAY-169916 is a pathway-selective estrogen receptor (ER) ligand.¹ 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.²

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1. Chadwick, C.C., Chippari, S., Matelan, E., et al. Identification of pathway-selective estrogen receptor ligands that inhibit NF-κB transcriptional activity. Proc. Natl. Acad. Sci. U.S.A. 102(7), 2543-2548 (2005).

2. Booth, E.A., Marchesi, M., Knittel, A.K., et al. The pathway-selective estrogen receptor ligand WAY-169916 reduces infarct size after myocardial ischemia and reperfusion by an estrogen receptor dependent mechanism. J. Cardiovasc. Pharmacol. 49(6), 401-407 (2007).