Estetrol (E4, 15α-Hydroxyestriol) is an estrogen steroid hormone produced exclusively during pregnancy by the fetal liver. Estetrol is a selective estrogen receptor modulator (SERM) with potent estrogenic effects on vaginal mucosa, bone and brain, neutral effect on liver, and anti-estrogen effects on breast tissue. Estetrol has higher affinity for ERα over ERβ. Estetrol is being studied for its potential as a contraceptive, a drug for meopausal symptoms, and an anticancer agent.
| Molecular Weight | 304.38 |
| Formula | C18H24O4 |
| CAS Number | 15183-37-6 |
| Form | Solid |
| Solubility (25°C) | DMSO: 20 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.
[1] Franca Fruzzetti, et al. Estetrol: A New Choice for Contraception
[2] Anne Gallez, et al. Estetrol and Mammary Gland: Friends or Foes?
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