Estriol Estrogen/progestogen Receptor antagonist

Cat.No.S2466

Estriol (NSC-12169) is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.
Estriol Estrogen/progestogen Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 288.39

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 57 mg/mL (197.64 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 288.39 Formula

C18H24O3

Storage (From the date of receipt)
CAS No. 50-27-1 Download SDF Storage of Stock Solutions

Synonyms NSC-12169 Smiles CC12CCC3C(C1CC(C2O)O)CCC4=C3C=CC(=C4)O

Mechanism of Action

Targets/IC50/Ki
ER
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. 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 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. 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.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/16402032/
  • [5] https://pubmed.ncbi.nlm.nih.gov/20826375/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05000424 Unknown status
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 Phase 2
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

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