Nolvados (Tamoxifen Citrate)

About the Product

Nolvados is a research compound from Driada Medical, containing Tamoxifen Citrate. Tamoxifen Citrate is a nonsteroidal, orally active agent classified as a selective estrogen receptor modulator (SERM) . Its chemical formula is C₃₂H₃₇NO₈, with a molecular weight of 563.64 g/mol .

The compound functions by competitively binding to estrogen receptors in target tissues . In breast tissue, it acts as a potent antagonist, blocking estrogen from stimulating cell growth . This anti-estrogenic profile is central to its research applications.

• Product Name: Nolvados (Tamoxifen Citrate)

• Brand: Driada Medical

• Form: Solution for research applications

• CAS Number: 54965-24-1

• For Research Use Only.

Research Applications & Mechanism of Action

• Selective Estrogen Receptor Modulator (SERM): Tamoxifen is a benchmark compound for studying estrogen receptor (ER) biology due to its tissue-specific effects . It acts as an antagonist in breast tissue, blocking estrogen-driven proliferation, but can exhibit agonist activity in other tissues such as bone and the endometrium . This complex pharmacology is valuable for investigating receptor dynamics and tissue-specific signaling.

• Cancer Research: As a model anti-estrogen, tamoxifen is widely used to study hormone-responsive cancers, particularly ER-positive breast cancer models. Research includes investigating mechanisms of acquired resistance and combination therapies .

• Gene Regulation & Apoptosis: Tamoxifen is a potent activator of the Hsp90 molecular chaperone ATPase and can induce autophagy and apoptosis, making it relevant for studying cell death and stress response pathways .

• Transgenic Model Generation: Tamoxifen is a critical tool for generating inducible gene knockout models. When used with CreER(T2) transgenic mice, tamoxifen administration enables temporal control of gene deletion, a cornerstone of modern functional genetics research .

• Hsp90 & Kinase Inhibition: Beyond its nuclear receptor activity, tamoxifen is a known inhibitor of protein kinase C (PKC) and an activator of the GPR30 receptor, demonstrating its utility in studying non-genomic signaling pathways .

Research & Scientific Background

• Mechanism: Tamoxifen competes with estradiol for estrogen receptor binding . In breast tissue, the tamoxifen-receptor complex recruits co-repressors, halting the transcription of estrogen-responsive genes required for cell proliferation .

• Metabolism: The compound is extensively metabolized, primarily by cytochrome P450 enzymes (CYP3A4, CYP2D6), to active metabolites including N-desmethyl tamoxifen and 4-hydroxytamoxifen . This metabolic profile is a key consideration in pharmacogenomic research.

• Pharmacokinetics: Following oral administration, tamoxifen has a terminal elimination half-life of approximately 5-7 days, with its major metabolite having a half-life of about 14 days . Steady-state concentrations are achieved after several weeks.