(E/Z)-4-Hydroxytamoxifen

SKU: orb1300507

Description

Afimoxifene, the (E/Z)-4-hydroxylated metabolite of tamoxifen, is a selective estrogen receptor modulator (SERM) used in research. It is applied in studies of estrogen-dependent conditions such as breast cancer, gynecomastia, and mastalgia, utilizing both in vitro and in vivo experimental models.

Research Area

Metabolism Research

Key Properties

• CAS Number: 68392-35-8
• MW: 387.51
• Purity: 99.97% (May vary between batches)
• Formula: C₂₆H₂₉NO₂
• SMILES: CC\C(=C(/c1ccc(O)cc1)c1ccc(OCCN(C)C)cc1)c1ccccc1
• Target: Estrogen/progestogen Receptor,Drug Metabolite,Endogenous Metabolite,Estrogen Receptor/ERR
• Solubility: DMSO:60 mg/mL (154.83 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.16 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  ER:
• In Vitro:
  4-OHT is a potent activator of ER and has been shown to have a higher affinity for estrogen receptors compared to tamoxifen. It has significant dose and time-dependent direct effects to alter the contractile function of isolated adult rat cardiac myocytes. 4-HT activates on-target modification frequency for intein-Cas9 variants
• Cell Research:
  Cell lines: Adult Rat and Mouse Cardiac MyocytesConcentrations: 0, 0.5, 1, 3, 5, and 10 μMIncubation Time: 15-45 minMethod:For sarcomere length measurements, cells are covered in Tyrode's containing 4OHT, allowed to reach 36 ± 1°C, and then stimulated at 0.2 Hz.
• Animal Research:
  Animal Models: Sprague-Dawley ratsFormulation: dissolved in 200 μl tricaprylinDosages: 21 mg/kg, 54 μmol/kgAdministration: oral administration

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Estrogen Receptor, EstrogenReceptor, Estrogen Receptor/ERR, ERR, ER, Endogenous Metabolite, Inhibitor, (E/Z) 4 Hydroxytamoxifen, (E/Z)4Hydroxytamoxifen, (E/Z)-4-Hydroxytamoxifen, 4-Hydroxytamoxifen, Afimoxifene, progestogen Receptor, progestogenReceptor

Compound Identifiers

PubChem CID

449459