Ethinylestradiol (Synonyms: Ethynyl estradiol; 17α-Ethynylestradiol)

Name: Ethinylestradiol
Brand: MedChemExpress
SKU: HY-B0216
Rating: 5.0 (5 reviews)

Cat. No.: HY-B0216 Purity: 99.96%: Data Sheet
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Ethinylestradiol is an orally active steroidal estrogen. Ethinylestradiol is widely used in research on menopausal symptoms, gynecological conditions, and certain hormone-sensitive cancers.

For research use only. We do not sell to patients.

CAS No. : 57-63-6

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
500 mg	In-stock	Estimated Time of Arrival: December 31
1 g	In-stock	Estimated Time of Arrival: December 31
5 g	In-stock	Estimated Time of Arrival: December 31
10 g	Get quote
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Based on 5 publication(s) in Google Scholar

Other Forms of Ethinylestradiol:

5 Publications Citing Use of MCE Ethinylestradiol

In Vivo Efficacy Study

Histological Imaging/Staining

ELISA

RT-PCR

: 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.

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Biological Activity
Purity & Documentation
References
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Description

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 μM Compound: EE2	Cytotoxicity against HEK293 cells Cytotoxicity against HEK293 cells	[PMID: 18973326]
HEK293	IC₅₀	2.2 μM 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 μM 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 μM 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 μM 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 μM 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 μM 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 nM 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 μM 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]

In Vitro

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.

In Vivo

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.

Clinical Trial

Molecular Weight

296.40

Formula

C₂₀H₂₄O₂

CAS No.

57-63-6

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

Steroids

Initial Source

Endogenous metabolite

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

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
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (8.43 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.
Protocol 4

Add each solvent one by one: 10% EtOH 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 EtOH 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 5

Add each solvent one by one: 10% EtOH 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 EtOH 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:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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.

Purity & Documentation

Purity: 99.96%

Select Batch:

Data Sheet (280 KB) SDS (479 KB)

COA (250 KB) HNMR (269 KB) LCMS (89 KB)

Handling Instructions (2659 KB)

References

[1]. Kuhl H. Pharmacology of estrogens and progestogens: influence of different routes of administration. Climacteric. 2005 Aug;8 Suppl 1:3-63. [Content Brief]

[2]. Arnal J F, et al. Ethinylestradiol does not enhance the expression of nitric oxide synthase in bovine endothelial cells but increases the release of bioactive nitric oxide by inhibiting superoxide anion production[J]. Proceedings of the National Academy of Sciences, 1996, 93(9): 4108-4113.

[3]. Notch EG, et al. 17alpha-Ethinylestradiol hinders nucleotide excision repair in zebrafish liver cells. Aquat Toxicol. 2009 Dec 13;95(4):273-8. [Content Brief]

[4]. Bertolotti M, et al. Effect of hypocholesterolemic doses of 17 alpha-ethinyl estradiol on cholesterol balance in liver and extrahepatic tissues. J Lipid Res. 1996 Aug;37(8):1812-22. [Content Brief]

[5]. Mandrup KR, et al. Effects of perinatal ethinyl estradiol exposure in male and female Wistar rats. Reprod Toxicol. 2013 Dec;42:180-91. [Content Brief]

Complete Stock Solution Preparation Table

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

Ethinylestradiol Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ethinylestradiol57-63-6Ethynyl estradiol 17α-EthynylestradiolEnvironmental PollutantsEstrogen Receptor/ERREndogenous MetaboliteEnvironmental Contaminantssteroidal estrogenorally activeRFL6 cellsBAEC cellsInhibitorinhibitorinhibit

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Ethinylestradiol (Synonyms: Ethynyl estradiol; 17α-Ethynylestradiol)

Customer Review

Other Forms of Ethinylestradiol:

Ethinylestradiol Related Antibodies

5 Publications Citing Use of MCE Ethinylestradiol

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View All Estrogen Receptor/ERR Isoform Specific Products:

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Biological Activity

Purity & Documentation

References

Customer Review

Ethinylestradiol Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Ethinylestradiol Related Classifications

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