Endoxifen E-isomer hydrochloride  ≥98% (HPLC)

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包装规格:1mg 5mg 25mg 100mg in glass bottle
溶解性:溶于DMSO(≥ 30 mg/mL)
产品描述:一种他莫西芬(Tamoxifen)代谢产物,一种有效的选择性雌激素反应调节剂(SERM)。Endoxifen (E-isomer hydrochloride) is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM). Target: Estrogen Receptor/ERR Endoxifen is considered a prodrug, since it has a much higher potency for the estrogen receptor than its parent drug. Endoxifen inhibits the hERG channel protein trafficking to the plasma membrane in a concentration-dependent manner with Endoxifen being more potent than Tamoxifen. Endoxifen is also shown to be a more potent inhibitor of estrogen target genes when ERβ is expressed. Additionally, low concentrations of Endoxifen observed in Tamoxifen treated patients with deficient CYP2D6 activity (20 to 40 nM) markedly inhibit estrogen-induced cell proliferation rates in the presence of ERβ, whereas much higher Endoxifen concentrations are needed when ERβ is absent.
保存条件:-20℃