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Estriol

Name: Estriol
Brand: Selleck Chemicals
SKU: S2466
Rating: 5 (1 reviews)

Synonyms: NSC-12169

Catalog No.S2466 Purity: 99.34%

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

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

Estriol Related Products

Related Targets	Estrogen receptor Progesterone receptor ERR	Click to Expand
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Signaling Pathway

Estrogen/progestogen Receptor Signaling Pathway

Choose Selective Estrogen/progestogen Receptor Inhibitors

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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References

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Chemical Information & 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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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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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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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