Estriol is a G-protein coupled estrogen receptor antagonist. It is one of the three main estrogens produced by the human body. It can be a weak or strong estrogen depending on if it is given acutely or chronically when given to immature animals, but is an antagonist when given in combination with estradiol. It may play a role in the development of breast cancer, but based on in vitro research does appear to act as an antagonist to the G-protein coupled estrogen receptor
|Cell lines||SkBr3 cells|
|Preparation method||For the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, culturing cells in 96-well plates under 200 μL of growth medium and at an initial density of 10,000 cells per well. Washing cells once they have attached and further incubated in medium which contains 2.5% charcoal-stripped FBS with the indicated treatment. Changing the medium every 2 days (with treatment). Where applicable,transfecting 200 ng of the indicated plasmids every 2 days before treatments using Fugene6 Reagent, as recommended by the manufacturer. Following 6 days of incubation, adding the assay mixture (10µL per well) which contains 1mg/mL 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) 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.|
|Incubation time||6 days|
|Animal models||mPTEN+/- and wild-type mice|
|Formulation||Estriol is dissolved in ethanol and corn oil.|
|Administration||Administrated via s.c.SkBr3 细胞|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 45 mg/mL|
|Related Estrogen Receptor Products|
Relugolix, also known as TAK-385, is a luteinizing hormone-releasing hormone (LH-RH) receptor antagonist with an IC50 of 0.12 nM.
Elagolix Soidum is a potent, selective, orally active, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) with Kd value of 54 pM.
GDC-0810 (Brilanestrant, ARN-81) is an orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM.
Tamoxifen is a estrogen receptor partial agonist/antagonist.
GSK 4716 is a selective agonist with estrogen-related receptors ERRβ and ERRγ.
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