product name Estriol
Description: Estriol (also called NSC-12169) is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells. Estriol’s efficacy is due to the interference between estradiol-induced positive cooperative binding and receptor dimerization, as well as the binding of hER complexes to ERE. 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.
References: Mol Cell Endocrinol. 2010 May 14;320(1-2):162-70; Lab Invest. 2006 Mar;86(3):286-96.
288.39
Formula
C18H24O3
CAS No.
50-27-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 57 mg/mL (197.6 mM)
Water: <1 mg/mL
Ethanol: 10 mg/mL (34.7 mM)
Solubility (In vivo)
5% DMSO+95% Corn oil: 10 mg/mL
Synonyms
NSC-12169
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19419283
| In Vitro |
In vitro 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 Alzheimers disease-associated low-order Aβ oligomer formation, and among them, estriol shows the strongest in vitro activity. Kinase Assay: Cell Assay: 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 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. |
| Animal model | mPTEN+/- and wild-type mice |
| Formulation & Dosage | Dissolved in ethanol and corn oil; 4 μg/g/day; s.c. administration |
| References | Mol Cell Endocrinol. 2010 May 14;320(1-2):162-70; Lab Invest. 2006 Mar;86(3):286-96. |
