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  3. Ethinylestradiol

エチニルエストラジオール  (Synonyms: Ethinylestradiol; Ethynyl estradiol; =17α-Ethynylestradiol)

製品番号: HY-B0216 純度: 99.96%
COA 取扱説明書 Technical Support

Ethinylestradiol is an orally active steroidal estrogen. Ethinylestradiol is widely used in research on menopausal symptoms, gynecological conditions, and certain hormone-sensitive cancers.

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CAS 番号 : 57-63-6

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10 mM * 1 mL in DMSO
ready for reconstitution
USD 33 在庫あり
Solution
10 mM * 1 mL in DMSO USD 33 在庫あり
Solid
500 mg $30 在庫あり
1 g $58 在庫あり
5 g $184 在庫あり
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カスタマーレビュー

Based on 5 publication(s) in Google Scholar

Other Forms of Ethinylestradiol:

Top Publications Citing Use of Products

    Ethinylestradiol purchased from MedChemExpress. Usage Cited in: Environ Health (Wash). 2025 Jan 10;3(4):414-424.

    Ethinylestradiol (EE2, 1-100 ng/L; 7 day) reduced the fertility of female zebrafish in a concentration-dependent manner.

    Ethinylestradiol purchased from MedChemExpress. Usage Cited in: Environ Health (Wash). 2025 Jan 10;3(4):414-424.

    Representative histological images of ovarian (upper) and testicular (lower) tissues from different groups. Ethinylestradiol (EE2, 1–100 ng/L) exposure for 7 days simultaneously inhibited oogenesis and spermatogenesis in zebrafish.

    Ethinylestradiol purchased from MedChemExpress. Usage Cited in: Environ Health (Wash). 2025 Jan 10;3(4):414-424.

    Temporal alterations in VTG concentrations in the liver, blood, and mucus of male zebrafish after exposure to 100 ng/L Ethinylestradiol (EE2) for 1, 2, 4, or 7 days. The results showed that only 100 ng/L EE2 suppressed liver VTG expression by 0.64-fold after 7 days of exposure, whereas blood VTG concentration started to decrease at exposure days 4 and 7 by 0.39- and 0.40-fold, respectively. In contrast, mucus VTG in male zebrafish significantly increased in abundance by 1.99-fold within 1 day of EE2 exposure, but it began to decrease at 2, 4, and 7 days of EE2 exposure by 0.45-, 0.71-, and 0.55-fold, respectively.

    Ethinylestradiol purchased from MedChemExpress. Usage Cited in: Food Biosci. 2025 Jul.

    HE staining was used to evaluate structural changes in liver tissue. The results depicted disorganized hepatocytes in the Ethinylestradiol (EE, 10 mg/kg; s.c.; 5 days) group, characterized by nuclear wrinkling and large cell gaps. Notably, liver injury was significantly mitigated by sesamol and UDCA treatment.

    Ethinylestradiol purchased from MedChemExpress. Usage Cited in: Food Biosci. 2025 Jul.

    Ethinylestradiol (EE, 10 mg/kg; s.c.; 5 days) induced liver enlargement in mice, resulting in a white appearance.

    Ethinylestradiol purchased from MedChemExpress. Usage Cited in: Food Biosci. 2025 Jul.

    Ethinylestradiol (EE, 10 mg/kg; s.c.; 5 days) induced collagen deposition in mice, but sesamol treatment reduced this, as shown by Sirius red staining.

    Ethinylestradiol purchased from MedChemExpress. Usage Cited in: Food Biosci. 2025 Jul.

    Ethinylestradiol (EE, 10 mg/kg; s.c.; 5 days) induced liver fibrosis in mice, accompanied by upregulation of fibrosis-related proteins such as TGF-β and α-SMA at the protein level.

    Ethinylestradiol purchased from MedChemExpress. Usage Cited in: Food Biosci. 2025 Jul.

    Ethinylestradiol (EE, 10 mg/kg; s.c.; 5 days) induced liver fibrosis in mice, accompanied by elevated mRNA levels of fibrosis-related proteins including TGF-β and α-SMA.

    Estrogen Receptor/ERR アイソフォーム固有の製品をすべて表示:

    Endogenous Metabolite アイソフォーム固有の製品をすべて表示:

    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    Ethinylestradiol is an orally active steroidal estrogen. Ethinylestradiol is widely used in research on menopausal symptoms, gynecological conditions, and certain hormone-sensitive cancers[1].

    Cellular Effect
    Cell Line Type Value Description References
    HEK293 EC50
    3 3
    Compound: EE2
    Cytotoxicity against HEK293 cells
    Cytotoxicity against HEK293 cells
    [PMID: 18973326]
    HEK293 IC50
    2.2 3
    Compound: ethinyl estradiol
    Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
    Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
    [PMID: 23241029]
    HEK293 IC50
    21.1 3
    Compound: ethinyl estradiol
    Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
    Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
    [PMID: 23241029]
    HEK293 IC50
    20.2 3
    Compound: ethinyl estradiol
    Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
    Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
    [PMID: 23241029]
    HEK293 IC50
    20.2 3
    Compound: ethinyl estradiol
    Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
    Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
    [PMID: 23241029]
    HEK293 IC50
    21 3
    Compound: Ethinylestradiol
    Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method
    Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method
    [PMID: 21030469]
    HEK293 IC50
    2.2 3
    Compound: ethinyl estradiol
    Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
    Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
    [PMID: 23241029]
    HEK293 IC50
    21.1 3
    Compound: ethinyl estradiol
    Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
    Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
    [PMID: 23241029]
    HEK293 IC50
    21 3
    Compound: Ethinylestradiol
    Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method
    Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method
    [PMID: 21030469]
    HEK293 IC50
    3 3
    Compound: 5; EE2
    Inverse agonist activity at GAL4 fused-human CAR-LBD transfected HEK293 cells after 24 hrs by luciferase reporter gene assay
    Inverse agonist activity at GAL4 fused-human CAR-LBD transfected HEK293 cells after 24 hrs by luciferase reporter gene assay
    [PMID: 26717202]
    HEK293 IC50
    44 3
    Compound: Ethinylestradiol
    Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method
    Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method
    [PMID: 21030469]
    HEK293 IC50
    44 3
    Compound: Ethinylestradiol
    Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method
    Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method
    [PMID: 21030469]
    MDA-MB-231 IC50
    32.9 3
    Compound: EED
    Cytotoxicity against ERalpha and ERbeta-deficient human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against ERalpha and ERbeta-deficient human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 23786452]
    HEK293 IC50
    3 3
    Compound: 5; EE2
    Inverse agonist activity at GAL4 fused-human CAR-LBD transfected HEK293 cells after 24 hrs by luciferase reporter gene assay
    Inverse agonist activity at GAL4 fused-human CAR-LBD transfected HEK293 cells after 24 hrs by luciferase reporter gene assay
    [PMID: 26717202]
    MCF7 IC50
    20 1
    Compound: EE2
    Inhibition of SULT1A1 in human MCF7 cells assessed as 17beta-estradiol sulfation
    Inhibition of SULT1A1 in human MCF7 cells assessed as 17beta-estradiol sulfation
    [PMID: 22593037]
    MDA-MB-231 IC50
    32.9 3
    Compound: EED
    Cytotoxicity against ERalpha and ERbeta-deficient human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against ERalpha and ERbeta-deficient human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 23786452]
    HEK293 EC50
    3 3
    Compound: EE2
    Cytotoxicity against HEK293 cells
    Cytotoxicity against HEK293 cells
    [PMID: 18973326]
    HEK293 IC50
    2.2 3
    Compound: ethinyl estradiol
    Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
    Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
    [PMID: 23241029]
    HEK293 IC50
    20.2 3
    Compound: ethinyl estradiol
    Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
    Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
    [PMID: 23241029]
    HEK293 IC50
    21 3
    Compound: Ethinylestradiol
    Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method
    Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method
    [PMID: 21030469]
    HEK293 IC50
    21.1 3
    Compound: ethinyl estradiol
    Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
    Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
    [PMID: 23241029]
    HEK293 IC50
    3 3
    Compound: 5; EE2
    Inverse agonist activity at GAL4 fused-human CAR-LBD transfected HEK293 cells after 24 hrs by luciferase reporter gene assay
    Inverse agonist activity at GAL4 fused-human CAR-LBD transfected HEK293 cells after 24 hrs by luciferase reporter gene assay
    [PMID: 26717202]
    HEK293 IC50
    44 3
    Compound: Ethinylestradiol
    Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method
    Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method
    [PMID: 21030469]
    MCF7 IC50
    20 1
    Compound: EE2
    Inhibition of SULT1A1 in human MCF7 cells assessed as 17beta-estradiol sulfation
    Inhibition of SULT1A1 in human MCF7 cells assessed as 17beta-estradiol sulfation
    [PMID: 22593037]
    MDA-MB-231 IC50
    32.9 3
    Compound: EED
    Cytotoxicity against ERalpha and ERbeta-deficient human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against ERalpha and ERbeta-deficient human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 23786452]
    体外実験

    Ethinylestradiol (0.01-10 nM, 24-48 h) increases cGMP formation in RFL6 cells[2].
    Ethinylestradiol (0.01-10 nM, 6-48 h) reduces superoxide anion production in BAEC cells in dose- and time-dependent manner[2].
    Ethinylestradiol (1-100 nM, 24 h) decreases mRNA (XPC and XPA) abundance and NER capacity in zebrfish liver cells[3].

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

    体内実験

    Ethinylestradiol (5 mg/kg, s.c., 5 days) increases synthesis and expression of low density lipoprotein-receptor in the liver of female Sprague-Dawley rats at pharmacological doses[4].
    Ethinylestradiol (0-50 μg/kg, i.g., daily, 21 days) can have adverse effects on the reproductive development of nulliparous female Wistar rats[5].

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

    Animal Model: Female Sprague-Dawley rats[4]
    Dosage: 5 mg/kg
    Administration: Subcutaneous injection (s.c.), 5 days
    Result: Decreases plasma cholesterol levels and cholesterol content.
    Increased low density lipoprotein tissue spaces and clearance rates in the liver.
    Enhanced the hepatic expression of low density lipoprotein-receptor protein and mRNA.
    Increased cholesterol synthesis in several extrahepatic tissues, such as adrenals, ovaries, small bowel, and spleen.
    Animal Model: Nulliparous female Wistar rats[5]
    Dosage: 0-50 μg/kg
    Administration: i.g., daily, 21 days
    Result: Increased number of nipples and reduced ovary weight in female offspring.
    Induced malformations of female genitalia.
    Deepened the width of urethral slits in adult rats.
    Increased the expression of estrogen-regulated gene in ventral prostate of prepubertal male offspring in a dose-dependent manner.
    Decreased ventral prostate weight at 15μg/kg in prepubertal male offspring.
    臨床実験
    分子量

    296.40

    分子式

    C20H24O2

    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    OC1=CC=C2C(CC[C@]3([H])[C@]2([H])CC[C@@]4(C)[C@@]3([H])CC[C@]4(C#C)O)=C1

    Structure Classification
    Initial Source
    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 100 mg/mL (337.38 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : ≥ 100 mg/mL (337.38 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.3738 mL 16.8691 mL 33.7382 mL
    5 mM 0.6748 mL 3.3738 mL 6.7476 mL
    10 mM 0.3374 mL 1.6869 mL 3.3738 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

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    一般には略語で表示されます:C1V1 = C2V2

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    体内:

    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: ≥ 2.5 mg/mL (8.43 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.
    • Protocol 2

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

      Solubility: ≥ 2.5 mg/mL (8.43 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
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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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    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.
    純度とドキュメンテーション

    純度: 99.96%

    参考文献

    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 / Ethanol 1 mM 3.3738 mL 16.8691 mL 33.7382 mL 84.3455 mL
    5 mM 0.6748 mL 3.3738 mL 6.7476 mL 16.8691 mL
    10 mM 0.3374 mL 1.6869 mL 3.3738 mL 8.4345 mL
    15 mM 0.2249 mL 1.1246 mL 2.2492 mL 5.6230 mL
    20 mM 0.1687 mL 0.8435 mL 1.6869 mL 4.2173 mL
    25 mM 0.1350 mL 0.6748 mL 1.3495 mL 3.3738 mL
    30 mM 0.1125 mL 0.5623 mL 1.1246 mL 2.8115 mL
    40 mM 0.0843 mL 0.4217 mL 0.8435 mL 2.1086 mL
    50 mM 0.0675 mL 0.3374 mL 0.6748 mL 1.6869 mL
    60 mM 0.0562 mL 0.2812 mL 0.5623 mL 1.4058 mL
    80 mM 0.0422 mL 0.2109 mL 0.4217 mL 1.0543 mL
    100 mM 0.0337 mL 0.1687 mL 0.3374 mL 0.8435 mL
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    • Molarity Calculator

    • Dilution Calculator

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

    一般には略語で表示されます:C1V1 = C2V2

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    Inquiry Information

    製品名:
    Ethinylestradiol
    製品番号:
    HY-B0216
    数量:
    MCE 日本正規代理店: