Home Endocrinology & Hormones Estrogen/progestogen Receptor antagonist Estriol For research use only.

Estriol

Synonyms: NSC-12169

Estriol (NSC-12169) is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.

Estriol Chemical Structure

Estriol Chemical Structure

CAS: 50-27-1

Selleck's Estriol has been cited by 1 publication

Purity & Quality Control

Batch: S246601 DMSO] 57 mg/mL] false] Ethanol] 10 mg/mL] false] Water] Insoluble] false Purity: 99.34%
99.34

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Biological Activity

Description Estriol (NSC-12169) is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.
Targets
ER [1]
In vitro
In vitro 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. [1] 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. [2] 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. [3]
Cell Research Cell lines SkBr3 cells
Concentrations ~100 nM
Incubation Time 6 days
Method For the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, cells are cultured in plastic 96-well plates under 200 μL of growth medium and at an initial density of 10,000 cells per well. Cells are washed once they have attached and further incubated in medium containing 2.5% charcoal-stripped FBS with the indicated treatment. The medium is changed every 2 days (with treatment). Where applicable, 200 ng of the indicated plasmids are transfected every 2 days before treatments using Fugene6 Reagent, as recommended by the manufacturer. Following 6 days of incubation, the assay mixture (10µL per well) containing 1mg/mL 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) is added to each well and incubated at 37 ◦C for 4 h in a 5% CO2 atmosphere. The yellow tetrazolium MTT, reduced by metabolically active cells, results in intracellular purple formazan, which is released after overnight incubation with 200 µL 1% sodium dodecyl sulfate in 0.01N HCL and quantified spectrophotometrically by reading absorbance at 570nm using an enzyme-linked immunosorbent assay plate reader.
In Vivo
In vivo 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. [4] 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. [5]
Animal Research Animal Models mPTEN+/- and wild-type mice
Dosages 4 μg/g/day
Administration Administrated via s.c.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05000424 Recruiting Quality of Life|Pregnancy Related Franklin Health Research November 1 2021 Not Applicable
NCT05012072 Recruiting Mental Health Wellness 1|Preterm Birth Microgen LLC August 1 2021 Not Applicable
NCT04305093 Completed Obesity; Endocrine|Hormone Disturbance Precision Analytical Inc. December 15 2019 --
NCT04267731 Completed Aging Well Vemico Ltd.|University of Roehampton December 1 2019 Not Applicable
NCT03116022 Unknown status Dyspareunia|Menopause|Sexual Dysfunction University of Sao Paulo June 1 2017 Phase 1

Chemical lnformation & Solubility

Molecular Weight 288.39 Formula

C18H24O3
CAS No. 50-27-1 SDF Download Estriol SDF
Smiles CC12CCC3C(C1CC(C2O)O)CCC4=C3C=CC(=C4)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 57 mg/mL ( (197.64 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble


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In vivo
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