(E/Z)-4-Hydroxytamoxifen
CAS No. : 68392-35-8
(Synonyms: Afimoxifene; 4-OHT)
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|---|---|---|
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| 10mg | $90 | In-stock |
| 50mg | $260 | In-stock |
| 100mg | $400 | In-stock |
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| Cat. No. : | HY-16950A |
| M.Wt: | 387.51 |
| Formula: | C26H29NO2 |
| Purity: | >98 % |
| Solubility: | DMSO : 83.33 mg/mL (ultrasonic) |
(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][4].
In Vitro:(E/Z)-4-Hydroxytamoxifen (10 μM, 0-90 min) oxidized by CYP2D6 represents a minor route of Tamoxifen metabolism, and then is converted to 3,4- dihydroxytamoxifen and Endoxifen (HY-18719E)[3].
In Vivo:(E/Z)-4-Hydroxytamoxifen (20.9 mg/kg, gavage or i.p., daily for 7 days) reduces the body weight and induces a significant increase in ethoxyresorufin O-deethylase activity in rats[3].
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