Estetrol

Estetrol, an orally active estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol binds ERα as well as ERβ (with a fourfold lower affinity). Estetrol increases eNOS expression/activity and NO synthesis in endothelial cells. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast. Estetrol can be used in contraception and menopausal hormone research^[1][2][3][4]. IC50 & Target:Estrogen receptor^[1] In Vitro:Estetrol (0.1-10 nM, 48 h) increases eNOS expression/activity and NO synthesis via ERs in HUVEC cells^[2].
Estetrol (E4) (1 nM-1 μM) induces ERE transcriptional activity (Gene: AF‐1 and AF‐2) in HeLa and HepG2 cells, but has lower ERα binding affinity compared with E2^[3].
Estetrol (0.1-10 nM, 48 h) blocks the E2-induced cytoskeleton remodeling and movement of breast cancer cells (T47-D cell)^[4].
In Vivo:Estetrol (0.6 and 6 mg/kg/day, mixed in diet, 12 weeks) induces an atheroprotective effect in mice, with an ERα‐dependent manner^[3].
Estetrol (0.03-3.0 mg/kg, p.o., twice daily for four consecutive days) inhibits ovulation in rats^[5].