Cat. No.: HY-15731

Estetrol

고객리뷰

Based on 1 Customer Validation

Estetrol, an orally active estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol binds ERα as well as ERβ (with a fourfold lower affinity). Estetrol increases eNOS expression/activity and NO synthesis in endothelial cells. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast. Estetrol can be used in contraception and menopausal hormone research.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity: 99.76%
CAS No.: 15183-37-6
화학식: C₁₈H₂₄O₄
분자량:304.39

보관:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Estetrol Chemical Structure

CAS No.: 15183-37-6

사이즈

가격

재고

수량

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
용액&용해도
- In Vitro
- In Vivo
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

Estrogen receptor^[1]

All Estrogen Receptor/ERR Isoforms :

All Endogenous Metabolite Isoforms :

All NO Synthase Isoforms :

In Vitro

Estetrol (0.1-10 nM, 48 h) increases eNOS expression/activity and NO synthesis via ERs in HUVEC cells^[2].
Estetrol (E4) (1 nM-1 μM) induces ERE transcriptional activity (Gene: AF‐1 and AF‐2) in HeLa and HepG2 cells, but has lower ERα binding affinity compared with E2^[3].
Estetrol (0.1-10 nM, 48 h) blocks the E2-induced cytoskeleton remodeling and movement of breast cancer cells (T47-D cell)^[4].

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

In Vivo

Estetrol (0.6 and 6 mg/kg/day, mixed in diet, 12 weeks) induces an atheroprotective effect in mice, with an ERα‐dependent manner^[3].
Estetrol (0.03-3.0 mg/kg, p.o., twice daily for four consecutive days) inhibits ovulation in rats^[5].

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

Animal Model:

Four‐week‐old ovariectomized ERα^+/+LDL‐r^−/− or ERα^−/−LDL‐r^−/− mice were switched to atherogenic diet from the age of 6-18 weeks^[1]
Dosage:

0.6 or 6 mg/kg/day
Administration:

mixed in atherogenic diet, 12 weeks
Result:

Decreased total plasma cholesterol at 6 mg/kg/day in ERα^+/+LDLr^−/− but not in ERα^−/−LDLr^−/− mice.
Prevented lipid deposition in ovariectomized ERα^+/+LDLr^−/− mice.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 15183-37-6
Appearance Solid
분자량 304.39
화학식 C₁₈H₂₄O₄
Color White to off-white
SMILES

OC1=CC=C2C(CC[C@]3([H])[C@]2([H])CC[C@@]4(C)[C@@]3([H])[C@@H](O)[C@@H](O)[C@@H]4O)=C1
Structure Classification
- Phenols
- Monophenols
- Steroids
Initial Source
- Endogenous metabolite
선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

용액&용해도

In Vitro:

DMSO : 100 mg/mL (328.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.2853 mL

16.4265 mL

32.8530 mL

5 mM

0.6571 mL

3.2853 mL

6.5706 mL

10 mM

0.3285 mL

1.6427 mL

3.2853 mL

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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: ≥ 2.5 mg/mL (8.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (8.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (8.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (418 KB)
- English - EN (418 KB)
- Français - FR (418 KB)
- Deutsch - DE (418 KB)
- Norwegian - NO (418 KB)
- Español - ES (418 KB)
- Swedish - SV (418 KB)
- Italian - IT (418 KB)
- Korean - KR (418 KB)
- Portuguese - PT (418 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Valéra MC, et al. Effect of estetrol, a selective nuclear estrogen receptor modulator, in mouse models of arterial and venous thrombosis. Mol Cell Endocrinol. 2018 Dec 5;477:132-139. [Content Brief]

[2]. Montt-Guevara MM, et al. Estetrol Modulates Endothelial Nitric Oxide Synthesis in Human Endothelial Cells. Front Endocrinol (Lausanne). 2015 Jul 22;6:111. [Content Brief]

[3]. Abot A, et al. The uterine and vascular actions of estetrol delineate a distinctive profile of estrogen receptor α modulation, uncoupling nuclear and membrane activation. EMBO Mol Med. 2014 Oct;6(10):1328-46. [Content Brief]

[4]. Giretti MS, et al. Effects of Estetrol on Migration and Invasion in T47-D Breast Cancer Cells through the Actin Cytoskeleton. Front Endocrinol (Lausanne). 2014 May 26;5:80. [Content Brief]

[5]. Coelingh Bennink HJ, et al. Ovulation inhibition by estetrol in an in vivo model. Contraception. 2008 Mar;77(3):186-90. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.2853 mL	16.4265 mL	32.8530 mL	82.1326 mL
	5 mM	0.6571 mL	3.2853 mL	6.5706 mL	16.4265 mL
	10 mM	0.3285 mL	1.6427 mL	3.2853 mL	8.2133 mL
	15 mM	0.2190 mL	1.0951 mL	2.1902 mL	5.4755 mL
	20 mM	0.1643 mL	0.8213 mL	1.6427 mL	4.1066 mL
	25 mM	0.1314 mL	0.6571 mL	1.3141 mL	3.2853 mL
	30 mM	0.1095 mL	0.5476 mL	1.0951 mL	2.7378 mL
	40 mM	0.0821 mL	0.4107 mL	0.8213 mL	2.0533 mL
	50 mM	0.0657 mL	0.3285 mL	0.6571 mL	1.6427 mL
	60 mM	0.0548 mL	0.2738 mL	0.5476 mL	1.3689 mL
	80 mM	0.0411 mL	0.2053 mL	0.4107 mL	1.0267 mL
	100 mM	0.0329 mL	0.1643 mL	0.3285 mL	0.8213 mL

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Estetrol

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Drug Repurposing Compound Library

All Estrogen Receptor/ERR Isoforms

All Endogenous Metabolite Isoforms

All NO Synthase Isoforms

Biological Activity

Chemical Information

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

Estetrol Related Classifications

HY-15731 Related Classifications