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|
|Related Estrogen Receptor Products|
Quinestrol is a synthetic estrogen that has the potential to be used in breast and prostate cancer related research.
Giredestrant (GDC-9545) is a potential "best-in-class" selective estrogen receptor inhibitor (SERD). Giredestrant can competitively bind with Estradiol in the ER ligand binding domain and induce conformational changes. Giredestrant has antitumor activity.
Zuclomiphene citrate is a cis isomer of clomiphene citrate. Zuclomiphene citrate has an anti-estrogen effect and inhibits the secretion of luteinizing hormone (LH) more than trans isomers. Zuclomiphene citrate is also an oral active cholesterol lowering agent.
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.
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