| 常用名 | (Z)-4-羟基-N-去甲基他莫昔芬(异构体的混合物) | CAS号 | 112093-28-4 |
|---|---|---|---|
| 价格 | ¥需询单/1mg | 纯度 | 98.0% |
| 备货期 | 3天 | 库存 | 现货 |
| 产品详情(用途,包装等)
用途: Endoxifen Z-isomer is the most important Tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα). Endoxifen inhibits hERG tail currents at 50 mV in a concentration-dependent manner with IC50 values of 1.6 μM.IC50 value: 1.6 μM [1]Target: hERG Potassium Channel, Estrogen Receptor/ERREndoxifen Z-isomer 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. [1] Endoxifen is also shown to be a more potent inhibitor of estrogen target genes when ERβ is expressed. Additionally, low concentrations of Endoxifen Z-isomer 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 Z-isomer concentrations are needed when ERβ is absent.[2] 物理化学性质: CAS号:112093-28-4 常用中文名:(Z)-4-羟基-N-去甲基他莫昔芬(异构体的混合物) 常用英文名:Endoxifen (Z-isomer) 分子式:C25H27NO2 分子量:373.48700 密度:1.099g/cm3 沸点:519.327ºC at 760 mmHg 熔点:127-129°C 闪点:267.88ºC 储存条件:Amber Vial, -86°C Freezer, Under Inert Atmosphere |