Estetrol
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.
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- Pureza: 99.76%
- No. CAS: 15183-37-6
- Fòrmula: C18H24O4
- Peso molecular:304.39
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
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Actividad biológica
Estrogen receptor[1]
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.
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.
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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]
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Dosage:0.6 or 6 mg/kg/day
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Administration:mixed in atherogenic diet, 12 weeks
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 15183-37-6
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Appearance Solid
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Peso molecular 304.39
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Fòrmula C18H24O4
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Color White to off-white
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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
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Structure Classification
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Initial Source
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (277 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
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, 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 |
Estetrol Related Classifications
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