4-Hydroxytamoxifen Overview
4-Hydroxytamoxifen is a biologically active metabolite of tamoxifen and a well-studied selective estrogen receptor modulator (SERM). It demonstrates significantly higher estrogen receptor binding affinity than its parent compound, making it a preferred molecule for direct estrogen receptor interaction studies in controlled laboratory environments.
Due to its defined pharmacological profile and receptor specificity, 4-Hydroxytamoxifen is widely referenced in estrogen signaling research and molecular biology models.
Chemical Structure and Identification
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Chemical Name: 4-Hydroxytamoxifen
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Alternative Names: 4-OHT, Afimoxifene, Hydroxytamoxifen
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CAS Number: 82413-23-8
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Molecular Formula: C₂₆H₂₉NO₂
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Molecular Weight: 387.51 g/mol
The defining structural feature of 4-Hydroxytamoxifen is the phenolic hydroxyl group, which enhances estrogen receptor affinity and alters receptor conformational behavior compared to tamoxifen.
Chemical and molecular data are verified using PubChem reference standards.
Mechanism of Action
4-Hydroxytamoxifen acts as a selective estrogen receptor modulator by binding to estrogen receptors and inducing a unique receptor conformation. This interaction influences transcriptional regulation by modifying co-activator and co-repressor recruitment.
Its activity is characterized by:
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High-affinity binding to estrogen receptors
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Competitive antagonism of endogenous estrogens
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Tissue-dependent modulation of estrogen signaling
Because it does not require metabolic conversion, 4-Hydroxytamoxifen is commonly used in experimental models requiring direct receptor engagement.
Research Applications
4-Hydroxytamoxifen is utilized in a wide range of laboratory research applications, including:
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Estrogen receptor signaling studies
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Hormone-responsive gene expression models
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ER-positive cell line research
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Inducible gene recombination systems
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Comparative SERM activity evaluation
Its consistency and potency make it a standard reference compound in estrogen-related research.
Physical and Chemical Properties
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Form: Solid compound
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Solubility: Typically dissolved in DMSO or ethanol for laboratory preparation
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Stability: Sensitive to light and oxidative conditions
Appropriate storage and handling procedures are required to maintain compound integrity.
Research Use Disclaimer
4-Hydroxytamoxifen is provided strictly for laboratory research use only (RUO).
Not intended for human consumption, clinical use, veterinary use, or diagnostic applications.
All research involving this compound must comply with applicable regulations and institutional guidelines.
Final Summary
4-Hydroxytamoxifen is a high-affinity estrogen receptor modulator with a clearly defined chemical structure and extensive research background. Its direct receptor activity and reproducible behavior make it an essential tool in estrogen signaling and hormone-related laboratory studies.
| CAS Number | 82413-23-8 |
| Other Names | T4-hydroxytamoxifen, 4Hydroxytamoxifen, 4-Hydroxy-Tamoxifen |
| IUPAC Name | 4-[(Z)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-1-phenylbut-1-en-2-yl]phenol |
| Molecular Formula | C26H29NO2 |
| Molecular Weight | 387.5 g/mol |
| Dry-Fill Capsule Concentration | NA |
| Liquid Concentration And Solution | 0.5mg/ml (Transdermal Gel) Ethanol, DMSO, PEG400, Propylene Glycol, Carbomer 940, Distilled Water, Menthol Crystals |
| Aliquot Concentration And Solution | NA |
