Endoxifen (E-isomer)
产品编号: DC9959
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应用领域
Endoxifen (E-型异构体)盐酸盐是Tamoxifen代谢产物, 是有效的选择性雌激素反应调节剂（SERM）。
| Cas No.: |
1197194-61-8 |
| 名称: |
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| 别名: |
E-Endoxifen |
| SMILES: |
OC1=CC=C(/C(C2=CC=C(OCCNC)C=C2)=C(C3=CC=CC=C3)/CC)C=C1.[H]Cl |
| 分子式: |
C25H28ClNO2 |
| 分子量: |
409.95 |
| 纯度: |
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| 保存条件: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: |
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| In Vitro: |
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| References: |
Endoxifen (E-isomer hydrochloride) is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM).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. |
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| Animal Administration: |
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| References: |
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MSDS
COA
| LOT NO. |
DOWNLOAD |
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| 2018-0101 |
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