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E-Endoxifen hydrochloride Chemical Structure

E-Endoxifen hydrochloride

Data Sheet For research use only. Not for human use.
Cat. No. :BCP18472CAS No. :1197194-61-8Purity:98%
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  • Chemical Properties&Biological Activity
CAS No. 1197194-61-8 Cat. No. BCP18472
Name E-Endoxifen hydrochloride
Synonyms Endoxifen E-isomer HCl;Endoxifen E-isomer hydrochloride;
SMILES
Chemical Name
Formula C25H28ClNO2 M. Wt 409.95
Purity 98% Storage Store at 4-8°C
Description Endoxifen E-isomer is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM).Endoxifen is considered a prodrug, since it has a much higher potency for the estrogen receptor than its parent drug. Endoxifen inhibits the hERG channel protein trafficking to the plasma membrane in a concentration-dependent manner with Endoxifen being more potent than Tamoxifen.Endoxifen is also shown to be a more potent inhibitor of estrogen target genes when ERβ is expressed. Additionally, low concentrations of Endoxifen observed in Tamoxifen treated patients with deficient CYP2D6 activity (20 to 40 nM) markedly inhibit estrogen-induced cell proliferation rates in the presence of ERβ, whereas much higher Endoxifen concentrations are needed when ERβ is absent.
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