Product Description: (E/Z)-4-Hydroxytamoxifen (Afimoxifene) is a racemic compound of (Z)-4-Hydroxytamoxifen and (E)-4-Hydroxytamoxifen isomers. (E/Z)-4-Hydroxytamoxifen is a selective estrogen receptor modulator with mixed estrogenic and antiestrogenic activity, which is also an active metabolite of Tamoxifen (HY-13757A). (E/Z)-4-Hydroxytamoxifen is an agonist of the G protein-coupled estrogen receptor (GPER) with relatively low affinity (100-1000 nM). (E/Z)-4-Hydroxytamoxifen is promising for research of cyclical mastalgia, such as breast pain, tenderness, and nodularity[1][2][3].
Applications: Cancer-programmed cell death
Formula: C26H29NO2
References: [1]Mansel R, et al. A phase II trial of Afimoxifene (4-hydroxytamoxifen gel) for cyclical mastalgia in premenopausal women. Breast Cancer Res Treat. 2007 Dec;106(3):389-97. /[2]Desta Z, et al. Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75./[3]Gamboa da Costa G, et al. DNA adduct formation and mutant induction in Sprague-Dawley rats treated with tamoxifen and its derivatives. Carcinogenesis. 2001 Aug;22(8):1307-15.
CAS Number: 68392-35-8
Molecular Weight: 387.51
Compound Purity: 99.62
Research Area: Cancer; Metabolic Disease
Solubility: DMSO : 83.33 mg/mL (ultrasonic)
Target: Adhesion G Protein-coupled Receptors (AGPCRs);Drug Metabolite;Estrogen Receptor/ERR
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