2-Methoxyestrone
Based on 3 publication(s) in Google Scholar
2-Methoxyestrone is an estrogen metabolite with antimitotic activity. 2-Methoxyestrone acts as a liver-specific prohormone that undergoes demethylation to form active 2-hydroxyestrogens, and it can also interconvert with 2-Methoxyestradiol (HY-12033) via the 17β-hydroxysteroid dehydrogenase pathway. In the presence of all-trans retinoic acid, 2-Methoxyestrone exerts a strong, concentration-dependent inhibitory effect on cell growth. 2-Methoxyestrone delays the progression of pulmonary hypertension in rats, alleviates right ventricular and pulmonary vascular remodeling, and relieves proliferative pulmonary hypertension in rats. 2-Methoxyestrone can be used in studies related to proliferative pulmonary hypertension.
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- Reinheit: 95.81%
- CAS. Nr.: 362-08-3
- Formel: C19H24O3
- Molecular Weight:300.39
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) 2-Methoxyestrone
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Biologische Aktivität
Beschreibung
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | GI50 |
21.3 μM
Compound: 1
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Inhibition of the growth of human breast cancer MCF-7 cells done for 2 hr at 37 degree C with compound
Inhibition of the growth of human breast cancer MCF-7 cells done for 2 hr at 37 degree C with compound
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[PMID: 16078843] |
| Sf9 | IC50 |
11 μM
Compound: 6
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Displacement of [3H]17beta-estradiol from human ERalpha expressed in SF9 cells
Displacement of [3H]17beta-estradiol from human ERalpha expressed in SF9 cells
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[PMID: 19836949] |
In Vitro
2-Methoxyestrone (2ME1) exhibits no or only weak antimitotic activity in hPASMC, hLF and HeLa cells when used alone, but in the presence of Retinoic acid (HY-14649), potently inhibits the growth of these cell types in a concentration-dependent manner[1].
2-Methoxyestrone (2-MeOE1) exhibits extremely low relative binding affinity for alpha-fetoprotein in the serum of 3-hour-old rats; it also shows extremely low relative binding affinity for estrogen receptors in an in vitro receptor-binding system[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
2-Methoxyestrone (20 μg/kg/h; administered continuously via implanted osmotic minipumps) attenuates pulmonary arterial hypertension and right ventricular remodeling induced by SU5416 (HY-10374) combined with hypoxia in intact female rats and ovariectomized female rats[1].
2-Methoxyestrone (2-MeOE1) is abundant in the plasma of neonatal rats and localizes in the liver. It exhibits extremely low binding affinity for alpha-fetoprotein and estrogen receptors, lacks uterotrophic activity, and exerts estrogen-like effects on liver-derived serum lipids and plasma renin substrate[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 362-08-3
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Appearance Solid
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Molecular Weight 300.39
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Formel C19H24O3
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Color White to off-white
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SMILES
C[C@]1([C@](CC2)([H])[C@]3([H])CCC4=C(C=C(OC)C(O)=C4)[C@@]3([H])CC1)C2=O
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Structure Classification
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Cell Metab
Sensing steroid hormone 17α-hydroxypregnenolone by GPR56 enables protection from ferroptosis-induced liver injury. [Abstract]2024 Nov 5;36(11):2402-2418.e10. PMID: 39389061 -
Nat Chem Biol
2022 Nov;18(11):1196-1203. PMID: 35982227 -
Proc Natl Acad Sci U S A
2022 Apr 12;119(15):e2117004119. PMID: 35394864
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 50 mg/mL (166.45 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, 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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.32 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.
In Vivo Dissolution Calculator
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.
Reinheit & Dokumentation
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Data Sheet (289 KB)
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SDS (563 KB)
- English - EN (563 KB)
- Français - FR (563 KB)
- Deutsch - DE (563 KB)
- Norwegian - NO (563 KB)
- Español - ES (563 KB)
- Swedish - SV (563 KB)
- Italian - IT (563 KB)
- Korean - KR (563 KB)
- Portuguese - PT (563 KB)
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Handling Instructions (2659 KB)
Verweise
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 | 3.3290 mL | 16.6450 mL | 33.2901 mL | 83.2251 mL |
| 5 mM | 0.6658 mL | 3.3290 mL | 6.6580 mL | 16.6450 mL | |
| 10 mM | 0.3329 mL | 1.6645 mL | 3.3290 mL | 8.3225 mL | |
| 15 mM | 0.2219 mL | 1.1097 mL | 2.2193 mL | 5.5483 mL | |
| 20 mM | 0.1665 mL | 0.8323 mL | 1.6645 mL | 4.1613 mL | |
| 25 mM | 0.1332 mL | 0.6658 mL | 1.3316 mL | 3.3290 mL | |
| 30 mM | 0.1110 mL | 0.5548 mL | 1.1097 mL | 2.7742 mL | |
| 40 mM | 0.0832 mL | 0.4161 mL | 0.8323 mL | 2.0806 mL | |
| 50 mM | 0.0666 mL | 0.3329 mL | 0.6658 mL | 1.6645 mL | |
| 60 mM | 0.0555 mL | 0.2774 mL | 0.5548 mL | 1.3871 mL | |
| 80 mM | 0.0416 mL | 0.2081 mL | 0.4161 mL | 1.0403 mL | |
| 100 mM | 0.0333 mL | 0.1665 mL | 0.3329 mL | 0.8323 mL |