Ethynyl estradiol is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills. EE is hormonally effective by activating the estrogen receptor and thus is an estrogen. It finds its most common use in the estrogen-progestin combination preparations of oral contraceptives.
|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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