Tamoxifen

Estrogen agonist/antagonist

Estrogen receptor antagonist.

• Powerful estrogen antagonist as well as pronounced anti-angiogenetic reaction observed
• Agitate bottle before each administration
• Not for human consumption

Tamoxifen (also known as Nolvadex, Istubal, Valodex and Tamox) is an antagonist of estrogen receptors. It also shows promise for anovulatory disorders and reversal of gynecomastia. Tamoxifen administration alone has been shown to have anti-angiogenetic effects in various models which appear to be, at least in part, independent of tamoxifen's estrogen receptor antagonist properties. It is used as a research tool to trigger tissue-specific gene expression in many conditional expression constructs in genetically modified animals including a version of the Cre-Lox recombination technique.

It is metabolized in the liver by the cytochrome P450 isoform CYP2D6 and CYP3A4 into active metabolites such as 4-hydroxytamoxifen (afimoxifene) and N-desmethyl-4-hydroxytamoxifen (endoxifen)[29] which have 30-100 times more affinity with the estrogen receptor than tamoxifen itself. These active metabolites compete with estrogen in the body for binding to the estrogen receptor. In breast tissue, 4-hydroxytamoxifen acts as an estrogen receptor antagonist so that transcription of estrogen-responsive genes is inhibited.The scientific literature is complex with respect to the activity of tamoxifen, and care should be taken to establish whether tamoxifen, or the 4-hydroxy metabolite was used, especially in in vitro assays.

CAS Number 10540-29-1

THIS PRODUCT IS NOT INTENDED TO TREAT, CURE OR DIAGNOSE ANY CONDITION OR DISEASE AND IS NOT FOR HUMAN CONSUMPTION