Description: Bazedoxifene (also known as TSE-424; WAY140424), a novel third generation selective estrogen receptor modulator (SERM) with IC50s of 26 and 99 nM for ERα and ERβ, respectively, has been developed to have favorable effects on bone and the lipid profile while minimizing stimulation of uterine or breast tissues. Bazedoxifene does not stimulate ERα mediated transcriptional activity and acts as an antagonist to estradiol in cultured breast cancer (bMCF-7) cells. Similar results are seen in other cell lines including CHO (ovarian), HepG2 (hepatic) or GTI-7 (neuronal) with bazedoxifene having no ERα agonist activity and acting as an antagonist to estradiol action.
References: Clin Interv Aging. 2007 Sep; 2(3): 299–303; Endocrinology. 2005 Sep;146(9):3999-4008.
Related CAS #: 198480-56-7 (HCl); 198481-32-2 (free base); 198481-33-3 (acetate)