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].

Product Specifications

CAS Number

15183-37-6

UNSPSC

12352005

Hazard Statement

H351, H360, H362

Target

Endogenous Metabolite; Estrogen Receptor/ERR; NO Synthase

Related Pathways

Immunology/Inflammation; Metabolic Enzyme/Protease; Vitamin D Related/Nuclear Receptor

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease; Cancer

Purity

99.76

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

OC1=CC=C2C(CC[C@]3([H])[C@]2([H])CC[C@@]4(C)[C@@]3([H])[C@@H](O)[C@@H](O)[C@@H]4O)=C1

Molecular Formula

C18H24O4

Molecular Weight

304.39

Precautions

H351, H360, H362

References & Citations

[1]Valéra MC, et al. Effect of estetrol, a selective nuclear estrogen receptor modulator, in mouse models of arterial and venous thrombosis. Mol Cell Endocrinol. 2018 Dec 5;477:132-139.|[2]Montt-Guevara MM, et al. Estetrol Modulates Endothelial Nitric Oxide Synthesis in Human Endothelial Cells. Front Endocrinol (Lausanne) . 2015 Jul 22;6:111.|[3]Abot A, et al. The uterine and vascular actions of estetrol delineate a distinctive profile of estrogen receptor α modulation, uncoupling nuclear and membrane activation. EMBO Mol Med. 2014 Oct;6 (10) :1328-46.|[4]Giretti MS, et al. Effects of Estetrol on Migration and Invasion in T47-D Breast Cancer Cells through the Actin Cytoskeleton. Front Endocrinol (Lausanne) . 2014 May 26;5:80.|[5]Coelingh Bennink HJ, et al. Ovulation inhibition by estetrol in an in vivo model. Contraception. 2008 Mar;77 (3) :186-90.