Estriol 50-27-1

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Molecular Weight:

288.39 Estriol is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.

Biological Activity

MTT assays using G-1 shows that, in SkBr3 cells, the proliferative
effect induced by 100 nM G-1 is abolished in the presence of 1 μM
estriol which acts as an antagonist of GPR30-dependent pathway. A cell-free transcription assay demonstrates that the antiestrogenic
activity exhibited by estriol is because of interferring with
estradiol-induced positive cooperative binding and receptor
dimerization, binding of hER complexes to ERE, as well as reducing
estradiol-dependent transcription in a dose-dependent manner.


A recent study shows that estrogen (estrone, estradiol, and estriol)
inhibits Alzheimer's disease-associated low-order Aβ oligomer formation,
and among them, estriol shows the strongest in vitro activity.


In mPTEN+/- mice, estriol treatments resulted in a 187.54% gain in the
relative ratio of uterine wet weight to body weight; estriol also
increases the ratio to 176.88% in wild-type mice.


Estriol
treatment (20 mg/kg ip), in vivo, sensitizes Kupffer cells to LPS via
mechanisms dependent on an increase in CD14 by elevated portal blood
endotoxin caused by increased gut permeability in rats; while one-half
of the rats given estriol intraperitoneally 24 hours before an injection
of a sublethal dose of LPS (5 mg/kg) died within 24 hours.

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Product Categories : Endocrinology & Hormones > Estrogen/progestogen Receptor Inhibitor