Formulation: A solid
Formal Name: 2-[4-[(1Z)-1,2-diphenyl-1-buten-1-yl]phenoxy]-N-methyl-ethanamine
Purity: ≥95%
Formula Markup: C25H27NO • HCl
Formula Weight: 394
Shelf life (days): 1460
CAS Number: 15917-65-4
Notes: N-Desmethyltamoxifen is an active metabolite of the estrogen receptor antagonist tamoxifen (Item Nos. 13258 / 11629).{28446} It is formed from tamoxifen by the cytochrome P450 (CYP) isoforms CYP2D6, CYP2C19, CYP3A5, or CYP3A4. N-Desmethyltamoxifen is an inhibitor of PKC (IC50 = 8 µM for the rat enzyme).{69735} It decreases iron (III) chloride and ascorbate-induced increases in thiobarbituric acid reactive substances (TBARS) in rat liver microsomes (IC50 = 17.5 µM).{69736} N-Desmethyltamoxifen induces relaxation in isolated and washed rat aortic rings (pD2 = 9), an effect that can be blocked with the selective estrogen receptor degrader ICI 182780 (fulvestrant; Item No. 10011269).{69737}