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.
| Molecular Weight | 296.4 |
| Formula | C20H24O2 |
| CAS Number | 57-63-6 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| 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.
[2] Amy L Lee. Segesterone Acetate and Ethinyl Estradiol Vaginal Ring (Annovera) for Contraception
[4] Andrea J Rapkin, et al. Drospirenone/ethinyl estradiol
[5] J W Goldzieher, et al. Pharmacokinetics of ethinyl estradiol and mestranol
| Related Estrogen Receptor Products |
|---|
| hFSH-β-(33-53) TFA
hFSH-β-(33-53) TFA, a thiol-containing peptide which corresponds to a second FSH receptor-binding domain, is a FSHR (follicle-stimulating hormone receptor) antagonist. hFSH-β-(33-53) TFA inhibits binding of FSH to receptor and is a partial agonist of estradiol synthesis in Sertoli cells. |
| Yp537
Yp537 is an estrogen receptor (ER) inhibitor that blocks dimerization of the human estrogen receptor. |
| Palazestrant
Palazestrant is a novel, orally active, estrogen receptor antagonist and selective estrogen receptor degrader. It can be used in studies related to ER+/HER2+ breast cancer. |
| Acolbifene hydrochloride
Acolbifene hydrochloride is an active metabolite of EM800 and an orally available, selective estrogen receptor modulator (SERM) that inhibits estradiol-induced ERα (IC50 = 2 nM) and ERβ (IC50 = 0.4 nM) transcriptional activity, has significant anti-estrogenic effects on the mammary gland and uterus, and has anticancer activity. possesses anticancer activity. |
| Acolbifene
Acolbifene is an active metabolite of EM800 and an orally active pure anti-estrogen and selective estrogen receptor (ER) antagonist that inhibits estradiol-induced ERα (IC50 = 2 nM) and ERβ (IC50 = 0.4 nM) transcriptional activity and has anticancer activity. |
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