| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| 100mg | |||
| Other Sizes |
| Targets |
4-Hydroxyestrone targets estrogen receptors (ERalpha and ERbeta) but with lower binding affinity compared to 17beta-estradiol. It modulates angiogenesis during corpus luteum formation. It is also involved in catechol estrogen-mediated DNA damage and may be associated with an increased risk of cancer.
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| ln Vitro |
4-Hydroxyestrone exhibits strong neuroprotective effects against oxidative damage in vitro. It shows little estrogenic activity but can be oxidized to form reactive quinones that bind to DNA, contributing to genotoxicity. It also regulates the angiogenic process during corpus luteum formation.
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| ln Vivo |
In vivo, 4-Hydroxyestrone provides effective protection against kainic acid-induced hippocampal oxidative damage in rats compared to 17beta-estradiol. It is found in the early and mid-luteal phases and may be involved in hormone-dependent cancer risk.
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| Enzyme Assay |
This cell-free assay is performed using purified recombinant human estrogen receptors (ERalpha and ERbeta). 4-Hydroxyestrone (0.1 nM - 10 uM) is incubated with 3H-estradiol (1 nM) in binding buffer for 16-24 hours at 4degC. Bound radioactivity is separated by charcoal adsorption or filtration, and IC50/Ki values are calculated. Alternatively, a fluorescence polarization-based competitive binding assay is used.
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| Cell Assay |
Human cancer cell lines (e.g., MCF-7 breast cancer cells) are treated with 4-Hydroxyestrone (0.1-100 uM) for 24-72 hours. Cell proliferation is assessed by MTT. For DNA damage studies (comet assay), cells are treated for 2-6 hours. Apoptosis is measured by caspase-3 activation or Annexin V staining. Metabolism of 4-OHE1 in cells can be followed by HPLC-MS.
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| Animal Protocol |
Female rats are administered 4-Hydroxyestrone by subcutaneous injection (doses 0.5-5 mg/kg). Hippocampal oxidative damage is induced by kainic acid. After treatment (1-7 days), brain tissues are harvested for lipid peroxidation (MDA), glutathione levels, and antioxidant enzyme activity. Corpus luteum angiogenesis is assessed by CD31 staining. Catechol estrogen quinone-DNA adducts can be quantified by 32P-postlabeling.
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| ADME/Pharmacokinetics |
Metabolism / Metabolites
Known metabolites of 4-hydroxyestrone include estrone 4-O-glucuronide and 4-methoxyestrone. 4-Hydroxyestrone is a known metabolite of estrone. 4-Hydroxyestrone is an endogenous metabolite, not a drug. Levels vary during the menstrual cycle (early to mid-luteal phase). It circulates at low concentrations (picomolar to nanomolar range) and is inactivated by catechol-O-methyltransferase (COMT) to 4-methoxyestrone, a process that can be affected by COMT polymorphisms. |
| Toxicity/Toxicokinetics |
This endogenous metabolite is not a toxic compound per se but may contribute to estrogen-mediated genotoxicity and carcinogenesis in susceptible individuals. It is a research-grade biochemical used to study estrogen metabolism, hormone-dependent cancers, and neuroprotection. Not for human consumption.
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| References | |
| Additional Infomation |
4-Hydroxyestrone is a 4-hydroxy steroid, a product of estrone with a hydroxyl group replaced at the 4-position. It possesses estrogenic activity, is a metabolic product found in human urine, and is also a carcinogen. It is a 4-hydroxy steroid, a 17-oxosteroid, a 3-hydroxy steroid, a phenolic steroid, and a catecholamine compound. Its function is related to estrone. 4-Hydroxyestrone is a metabolite formed during the liver metabolism of estrone via the hydroxylation of the 4-carbon by cytochrome P450 (CYP) family enzymes, and possesses potential carcinogenic activity. The mechanism of 4-hydroxyestrone's pro-tumorigenic action is not yet fully understood, but this metabolite exhibits higher estrogenic activity compared to its parent compound. Furthermore, the oxidation of 4-hydroxyestrone produces compounds containing free radicals, which can remove purines from DNA, leading to mutations and potentially inducing tumors.
This is a research-grade endogenous steroid metabolite, not a drug. It is used as a reference standard for estrogen metabolism studies and biomarker research. Molecular formula: C18H22O3; molecular weight: 286.37. Purity: ≥90% (HPLC). Solubility: methanol (10 mg/mL). Storage: -20degC. |
| Molecular Formula |
C18H22O3
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|---|---|
| Molecular Weight |
286.36548
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| Exact Mass |
286.157
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| CAS # |
3131-23-5
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| Related CAS # |
4-Hydroxyestrone-d4;81586-98-3;4-Hydroxyestrone-13C6
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| PubChem CID |
9971251
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.241g/cm3
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| Boiling Point |
468.2ºC at 760mmHg
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| Melting Point |
260-263ºC
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| Flash Point |
251.1ºC
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| Index of Refraction |
1.61
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| LogP |
3.523
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
21
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| Complexity |
448
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C[C@]12CC[C@H]3[C@H]([C@@H]1CCC2=O)CCC4=C3C=CC(=C4O)O
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| InChi Key |
XQZVQQZZOVBNLU-QDTBLXIISA-N
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| InChi Code |
InChI=1S/C18H22O3/c1-18-9-8-11-10-4-6-15(19)17(21)13(10)3-2-12(11)14(18)5-7-16(18)20/h4,6,11-12,14,19,21H,2-3,5,7-9H2,1H3/t11-,12-,14+,18+/m1/s1
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| Chemical Name |
(8R,9S,13S,14S)-3,4-dihydroxy-13-methyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-17-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4920 mL | 17.4599 mL | 34.9199 mL | |
| 5 mM | 0.6984 mL | 3.4920 mL | 6.9840 mL | |
| 10 mM | 0.3492 mL | 1.7460 mL | 3.4920 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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