Art. -Nr.: HY-116865

Equilenin

Name: Equilenin
Brand: MedChemExpress
SKU: HY-116865
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Equilenin is a B-ring unsaturated estrogen discovered in pregnant mare urine and is one of the major components of Premarin, a drug commonly used for estrogen replacement therapy. Equilenin binds to estrogen receptors in the body and exerts effects similar to endogenous estrogens. Equilenin weakly binds to and activates the aryl hydrocarbon receptor (AhR) to induce CYP1A1 expression. Equilenin exhibits high affinity for sex hormone-binding globulin (SHBG/SBP) and is metabolized by CYP1A1/1B1 to 4-hydroxy and 17β-dihydro derivatives. Equilenin is used in breast cancer-related research.

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Reinheit : 95.0%
CAS. Nr.: 517-09-9
Formel: C₁₈H₁₈O₂
Molecular Weight:266.33

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Equilenin Chemical Structure

CAS. Nr.: 517-09-9

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Protokoll (3)
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Endogenous Metabolite Isoform-spezifische Produkte anzeigen :

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen :

In Vitro

Equilenin (10-300 μM; 1 h) directly binds to AhR in C57BL mice, and at high concentrations inhibits specific [³H]B (a) P binding by approximately 50%^[1].
Equilenin binds to SBP with an equilibrium association constant of approximately 6 × 10⁷ M^-1, which is strong enough to competitively displace the natural steroid DHT from the binding site^[2].
Equilenin (1-30 μM; 24 h) induces CYP1A1 mRNA expression in HepG2 cells in a concentration-dependent manner^[1].
Equilenin (1-30 μM; 24 h) activates transcription through the xenobiotic response element (XRE) in HepG2 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

Real Time qPCR^[1]

View Protocol

Cell Line:

HepG2 cells
Concentration:

1, 1, 3, 10 or 30 μM
Incubation Time:

24 h
Result:

Induced CYP1A1 mRNA in a concentration-dependent manner, reaching an approximate 15-fold induction at 30 μM compared to control.

In Vivo

Equilenin (1-20 mg/kg/day; i.p.; for 3 consecutive days) dose-dependently induces CYP1A activity and CYP1A protein expression in the liver of C57BL mice^[1].
Equilenin (1-20 mg/kg/day; i.p.; intraperitoneal injection; 3 consecutive days) significantly induces CYP1A activity and protein expression in the liver of DBA2 mice at high doses^[1].
Equilenin (1-10 mg/L; immersion; 2 h) causes significant developmental toxicity and teratogenicity in developing medaka embryos, including malformations, mortality, and delayed hatching, accompanied by alterations in multiple gene expression pathways^[4].

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

Animal Model:

C57BL mice (6 weeks old at time of arrival, acclimatized for 1 week before use)^[1]
Dosage:

1 mg/kg/day; 20 mg/kg/day
Administration:

i.p.; repeatedly over 3 days
Result:

Significantly increased the activity of the CYP1A-dependent drug-metabolizing enzyme, ethoxyresorufin O-deethylation (EROD), at 20 mg/kg/day.
Increased expression of CYP1A protein in liver microsomes.
Showed an induction potency slightly more than half of that by B(a)P at the same dose.

Animal Model:

DBA2 mice (6 weeks old)^[1]
Dosage:

1 mg/kg/day; 20 mg/kg/day
Administration:

i.p.; daily for 3 days
Result:

Significantly increased EROD activity at 20 mg/kg/day.
Significantly increased CYP1A protein expression compared to controls at 20 mg/kg/day.

Animal Model:

NIES strain (embryos collected from 6-month-old adults)^[4]
Dosage:

1 mg/L; 10 mg/L
Administration:

immersion; 2 h
Result:

Reduced normal embryogenesis to 33% at 10 mg/L.
Increased deformity incidence to 17% at 1 mg/L and 33.3% at 10 mg/L.
Delayed hatching occurred at 8.3% for all test solutions.
Achieved 25% mortality at 10 mg/L.
Altered gene expression with 3855 differentially expressed genes (375 upregulated, 3480 downregulated) at 10 mg/L.

Chemical Information

CAS. Nr. 517-09-9
Appearance Solid
Molecular Weight 266.33
Formel C₁₈H₁₈O₂
SMILES

O=C1CC[C@]2([H])[C@@]1(CCC3=C2C=CC4=CC(O)=CC=C34)C
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (375.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.7547 mL

18.7737 mL

37.5474 mL

5 mM

0.7509 mL

3.7547 mL

7.5095 mL

10 mM

0.3755 mL

1.8774 mL

3.7547 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Protokoll

All Molecular Biology Signal Pathway Related Animals and Diseases

RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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.
Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (292 KB)
SDS (605 KB)
- English - EN (605 KB)
- Français - FR (605 KB)
- Deutsch - DE (605 KB)
- Norwegian - NO (605 KB)
- Español - ES (605 KB)
- Swedish - SV (605 KB)
- Italian - IT (605 KB)
- Korean - KR (605 KB)
- Portuguese - PT (605 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Jinno A, et al. Induction of cytochrome P450-1A by the equine estrogen equilenin, a new endogenous aryl hydrocarbon receptor ligand. The Journal of steroid biochemistry and molecular biology. 2006 Jan;98(1):48-55.

[2]. Ross JB, et al. Equilenin: a specific fluorescent probe for steroid-protein interactions in sex steroid-binding protein. FEBS letters. 1982 Nov 29;149(2):240-4.

[3]. Spink DC, et al. Metabolism of equilenin in MCF-7 and MDA-MB-231 human breast cancer cells. Chemical research in toxicology. 2001 May;14(5):572-81. [Content Brief]

[4]. Uchida M, et al. Developmental toxicity and transcriptome analysis of equine estrogens in developing medaka (Oryzias latipes) using nanosecond pulsed electric field incorporation. Comparative biochemistry and physiology. Toxicology & pharmacology : CBP. 2023 Apr;266:109547.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	3.7547 mL	18.7737 mL	37.5474 mL	93.8685 mL
	5 mM	0.7509 mL	3.7547 mL	7.5095 mL	18.7737 mL
	10 mM	0.3755 mL	1.8774 mL	3.7547 mL	9.3869 mL
	15 mM	0.2503 mL	1.2516 mL	2.5032 mL	6.2579 mL
	20 mM	0.1877 mL	0.9387 mL	1.8774 mL	4.6934 mL
	25 mM	0.1502 mL	0.7509 mL	1.5019 mL	3.7547 mL
	30 mM	0.1252 mL	0.6258 mL	1.2516 mL	3.1290 mL
	40 mM	0.0939 mL	0.4693 mL	0.9387 mL	2.3467 mL
	50 mM	0.0751 mL	0.3755 mL	0.7509 mL	1.8774 mL
	60 mM	0.0626 mL	0.3129 mL	0.6258 mL	1.5645 mL
	80 mM	0.0469 mL	0.2347 mL	0.4693 mL	1.1734 mL
	100 mM	0.0375 mL	0.1877 mL	0.3755 mL	0.9387 mL

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Equilenin

Alle Endogenous Metabolite Isoform-spezifische Produkte anzeigen

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen