Estriol

Catalog No.S2466 Synonyms: NSC-12169

Estriol Chemical Structure

Molecular Weight(MW): 288.39

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

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In DMSO USD 130 In stock
USD 97 In stock
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Biological Activity

Description Estriol is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.
Targets
ER [1]
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]

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]

Protocol

Cell Research:[1]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[4]
+ Expand
  • Animal Models: mPTEN+/- and wild-type mice
  • Formulation: Estriol is dissolved in ethanol and corn oil.
  • Dosages: 4 μg/g/day
  • Administration: Administrated via s.c.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 57 mg/mL (197.64 mM)
Ethanol 10 mg/mL (34.67 mM)
Water Insoluble
In vivo Add solvents individually and in order:
5% DMSO+95% Corn oil
10 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 288.39
Formula

C18H24O3

CAS No. 50-27-1
Storage powder
Synonyms NSC-12169

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03032848 Completed Vaginitis Atropic|Pelvic Organ Prolapse|Endometrial Hyperplasia Universidade Federal do Paraná November 26, 2013 Phase 4
NCT03044652 Recruiting Vulvovaginal Atrophy Dr. August Wolff GmbH & Co. KG Arzneimittel|proDERM Institut für Angewandte Dermatologische Forschung GmbH|Bremer Pharmacovigilance Service GmbH|GCP-Service International Ltd. & Co. KG November 2016 Phase 4
NCT02906111 Not yet recruiting Genital Prolapse Salvatore Caruso|Policlinico Universitario, Catania November 2016 Phase 4
NCT02967510 Recruiting Vaginal Atrophy ITF Research Pharma, S.L.U. October 2016 Phase 2
NCT02892214 Not yet recruiting Localized Provoked Vulvodynia Meir Medical Center October 2016 --
NCT02733731 Recruiting Atrophic Vaginitis First Affiliated Hospital, Sun Yat-Sen University February 2016 Phase 1

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Estrogen/progestogen Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID