2. Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. Estrogen Receptor/ERR Endogenous Metabolite
  4. Estriol

Estriol (Oestriol), an orally active estrogen, is a ERα and ERβ agonist. Estriol is a potent GPR30 antagonist in estrogen receptor-negative breast cancer cells. Estriol can ameliorate disease severity through immunomodulatory mechanisms that decrease tissue inflammation. Estriol has powerful proconvulsant effects.

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Estriol Chemical Structure

Estriol Chemical Structure

CAS No. : 50-27-1

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Based on 3 publication(s) in Google Scholar

Other Forms of Estriol:

Estriol Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

Estriol (Oestriol), an orally active estrogen, is a ERα and ERβ agonist. Estriol is a potent GPR30 antagonist in estrogen receptor-negative breast cancer cells. Estriol can ameliorate disease severity through immunomodulatory mechanisms that decrease tissue inflammation. Estriol has powerful proconvulsant effects[1][2][3].

IC50 & Target

Human Endogenous Metabolite

 

In Vitro

Estriol (Oestriol) binds to both ER and GPR30, however it can exhibit ER agonism or GPR30 antagonism depending on the receptor expression profile in the different cancer cell contexts[1].
Estriol (1-80 μM; for 7 days) reduces cell number of 17β-estradiol stimulated HCC1806 cells very clearly down to 16% at 80 μM[2].
Estriol (100 μM; pretreated for 30 minutes) completely prevented activation of cyclin D1 expression by 17β-estradiol[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Estriol Related Antibodies

Cell Viability Assay[2]

Cell Line: GPR30 positive (HCC1806) and a GPR30 negative TNBC cell line (MDA-MB-231)
Concentration: 1, 10, 20, 40, 60, 80 μM
Incubation Time: For 7 days
Result: Reduced cell number of 17β-estradiol stimulated HCC1806 cells very clearly down to 16±12% (p < 0.01) at 80 μM whereas in MDA-MB-231 cells was reduced to only 61±10% at the highest applied concentration.

Cell Cycle Analysis[2]

Cell Line: HCC1806 cells
Concentration: 100 μM
Incubation Time: Pretreated for 30 minutes
Result: Completely prevented activation of cyclin D1 expression by 17β-estradiol (10 nM; 10 min or 20 minutes).
In Vivo

Estriol (Oestriol ; 0.005, 0.01 mg/kg; IP; daily; for 5 weeks) enhances the percentage incidence of seizures[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Swiss Albino mice weighing between 25 and 35 g[3]
Dosage: 0.005, 0.01 mg/kg
Administration: IP; daily; for 5 weeks
Result: Reduced the time for induction of kindling from 5 weeks to 3 and 2 weeks for male and female mice respectively and enhanced the percentage incidence of seizures.
Clinical Trial
Molecular Weight

288.38

Formula

C18H24O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@]1([C@H]2O)[C@](C[C@H]2O)([H])[C@@](CCC3=C4C=CC(O)=C3)([H])[C@]4([H])CC1
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (866.91 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4676 mL 17.3382 mL 34.6765 mL
5 mM 0.6935 mL 3.4676 mL 6.9353 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (7.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (7.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.68%

COA (247 KB) HNMR (255 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4676 mL 17.3382 mL 34.6765 mL 86.6912 mL
5 mM 0.6935 mL 3.4676 mL 6.9353 mL 17.3382 mL
10 mM 0.3468 mL 1.7338 mL 3.4676 mL 8.6691 mL
15 mM 0.2312 mL 1.1559 mL 2.3118 mL 5.7794 mL
20 mM 0.1734 mL 0.8669 mL 1.7338 mL 4.3346 mL
25 mM 0.1387 mL 0.6935 mL 1.3871 mL 3.4676 mL
30 mM 0.1156 mL 0.5779 mL 1.1559 mL 2.8897 mL
40 mM 0.0867 mL 0.4335 mL 0.8669 mL 2.1673 mL
50 mM 0.0694 mL 0.3468 mL 0.6935 mL 1.7338 mL
60 mM 0.0578 mL 0.2890 mL 0.5779 mL 1.4449 mL
80 mM 0.0433 mL 0.2167 mL 0.4335 mL 1.0836 mL
100 mM 0.0347 mL 0.1734 mL 0.3468 mL 0.8669 mL
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Estriol Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Estriol50-27-1OestriolEstrogen Receptor/ERREndogenous MetaboliteERαERβGPR30breast cancer cellstissue inflammationproconvulsantInhibitorinhibitorinhibit

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