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.
For research use only. We do not sell to patients.
- Purity : 95.81%
- CAS No.: 362-08-3
- Formula: C19H24O3
- Molecular Weight:300.39
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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HY-12033
2-MethoxyestradiolApoptotic & Antiangiogenic Agent -
HY-124489
2-Hydroxyestradiol17β-Estradiol Metabolite -
HY-113344
16α-HydroxyestroneEndogenous Metabolite -
HY-B0141
EstradiolHuman Endogenous Metabolite -
HY-B0234
EstroneEndogenous Metabolite -
HY-107850
PregnanediolProgesterone Metabolite -
HY-N2370
24-HydroxycholesterolLXR Activator -
HY-113252R
2-Methoxyestrone (Standard)Reference Standard
Publications Citing Use of MedChemExpress (MCE) 2-Methoxyestrone
MoreAll Endogenous Metabolite Isoforms
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Biological Activity
Description
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. Further protocols information, click here.
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 No. 362-08-3
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Appearance Solid
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Molecular Weight 300.39
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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
Solvent & Solubility
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Protocols
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Protocol for Cell Counting and Cell Density Analysis
Cell counting and cell-density analysis estimate the number of cells in a known volume or field area. Manual hemocytometer counting uses a chamber of defined geometry to convert counted cells into cells/mL, while automated counters and image-analysis workflows detect cell objects from optical, brightfield, fluorescence, impedance, or digital-image features. Trypan blue viability counting is based on dye exclusion: viable cells with intact membranes exclude dye, while non-viable cells with compromised membranes stain blue. The readout is total cell density, viable-cell density, dead-cell density, and percent viability. Cell density can also be estimated from microscopy images by counting objects per image area, from flow cytometry using calibrated volume or reference particles, or from in situ microscopy in bioreactors after calibration against reference methods such as hemocytometer or flow cytometry.
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
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Somatic Cell Culture
A method of simulating the in vivo environment in vitro to maintain the cell growth, differentation and main functions.
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CCK-8/WST-8 Cell Proliferation Assay
The CCK-8/WST-8 assay is based on the reduction of the water-soluble tetrazolium salt WST-8 to a water-soluble formazan product by cellular dehydrogenases in metabolically active cells, where the generated formazan amount is proportional to the number of living cells and is quantified by measuring absorbance in the visible range, providing a colorimetric readout for cell viability and proliferation assessment. This class of tetrazolium-based assays improves upon earlier MTT-based systems by producing a water-soluble formazan, eliminating the need for organic solubilization steps and enabling direct spectrophotometric measurement in culture medium.
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Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
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Cell Counting-Based Growth Curve Assay
Cell counting-based growth curve assays quantify cell proliferation by directly measuring changes in viable cell number over time using manual or automated counting methods such as hemocytometer-based counting or instrument-assisted cell enumeration, enabling construction of growth curves that reflect population expansion dynamics in response to culture conditions. A widely used approach is trypan blue exclusion with hemocytometer counting, where membrane-compromised (non-viable) cells take up the dye, allowing discrimination between viable and non-viable cells while simultaneously enabling total cell number quantification. Repeated sampling across time points allows estimation of proliferation rate, growth phases, and comparative growth kinetics between experimental conditions.
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MTT Cell Proliferation Assay
The MTT assay is a colorimetric endpoint assay for estimating viable cell number, cell growth, cytotoxicity, or cell activation in cultured mammalian cells. Living cells reduce the yellow tetrazolium salt MTT into purple/blue formazan, while dead cells do not generate the same signal; the resulting color can be quantified with a multiwell spectrophotometer. MTT reduction is commonly interpreted as a readout of metabolic activity that often correlates with viable cell number, but it should not be treated as a direct cell-counting method unless the assay is optimized for the cell type and experimental condition. Studies show that MTT reduction can involve mitochondrial and non-mitochondrial reducing systems, and formazan may accumulate in intracellular lipid droplets rather than simply marking mitochondria.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
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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)
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 | 3.3290 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 |
2-Methoxyestrone Related Classifications
HY-113252 Related Classifications
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