Tamoxifen Citrate (Nolvadex) is an estrogen receptor antagonist with an IC50 of 31 μM for the MCF-7 cells. In some tissues such as the endometrium, it behaves as an agonist, hence tamoxifen may be characterized as a mixed agonist/antagonist.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO 50 mg/mL|
Effects of tamoxifen citrate on postoperative intra-abdominal adhesion in a rat model
Turgut Karaca, et al. Int J Surg. 2013;11(1):68-72. PMID: 23211136.
Tamoxifen-citrate counteracts the antitumor effects of cytotoxic drugs in vitro
V Hug, et al. J Clin Oncol. 1985 Dec;3(12):1672-7. PMID: 4067614.
|Related Estrogen Receptor Products|
27-Hydroxycholesterol is a selective estrogen receptor modulator, and it is also an agonist of the liver X receptor.
SAR439859 (Amcenestrant) is an orally active, nonsteroidal and selective degrader of estrogen receptor, it is also a potent antagonist of ER with EC50 of 0.2 nM for ERα degradation.
4-Hydroxytamoxifen is a selective estrogen receptor modulator.
Methylpiperidino pyrazole (MPP) is an agonist for estrogen receptor α and lacks any ligand functionality with estrogen receptor (ER)β.
|Endoxifen E-isomer hydrochloride
Endoxifen E-isomer hydrochloride is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM).
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