Equilenin
Based on 1 Customer Validation
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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- Pureté : 95.0%
- CAS No.: 517-09-9
- Formule: C18H18O2
- Masse moléculaire:266.33
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
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.
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Cell Line:HepG2 cells
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Concentration:1, 1, 3, 10 or 30 μM
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Incubation Time:24 h
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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.; 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.
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Animal Model:C57BL mice (6 weeks old at time of arrival, acclimatized for 1 week before use)[1]
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Dosage:1 mg/kg/day; 20 mg/kg/day
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Administration:i.p.; repeatedly over 3 days
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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.
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Animal Model:DBA2 mice (6 weeks old)[1]
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Dosage:1 mg/kg/day; 20 mg/kg/day
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Administration:i.p.; daily for 3 days
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Result:Significantly increased EROD activity at 20 mg/kg/day.
Significantly increased CYP1A protein expression compared to controls at 20 mg/kg/day.
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Animal Model:NIES strain (embryos collected from 6-month-old adults)[4]
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Dosage:1 mg/L; 10 mg/L
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Administration:immersion; 2 h
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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
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CAS No. 517-09-9
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Appearance Solid
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Masse moléculaire 266.33
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Formule C18H18O2
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SMILES
O=C1CC[C@]2([H])[C@@]1(CCC3=C2C=CC4=CC(O)=CC=C34)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocole
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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.
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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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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.
Pureté et documentation
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Fiche technique (292 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
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, 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 |
Equilenin Related Classifications
HY-116865 Related Classifications
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Keywords
- Equilenin
- 517-09-9
- Endogenous Metabolite
- Aryl Hydrocarbon Receptor
- Cytochrome P450
- medaka embryos
- dihydrotestosterone
- 17β-dihydroequilenin
- aryl hydrocarbon receptor
- ethoxyresorufin O-deethylase
- CYP1A1
- cytochrome P450 1B1
- sex steroid-binding protein
- catechol O-methyltransferase
- cytochrome P450 1A1
- Inhibitor
- inhibitor
- inhibit