货号 | 14854-1mg |
描述 | (Z)-4-hydroxy Tamoxifen is a major phase I metabolite of tamoxifen (Item No. 13258), a well-known estrogen receptor antagonist in breast but partial estrogen receptor agonist in endometrium. (Z)-4-hydroxy Tamoxifen is a product of cytochrome P450 (CYP)2D6 and CYP2B6 activity.1,2,3 The (Z), or trans, isomer of 4-hydroxytamoxifen has at least a 100-fold higher affinity for estrogen receptors than tamoxifen.4 |
别名 | ICI 79280;trans-4-hydroxy Tamoxifen; |
供应商 | Cayman |
应用文献 | |
1.Crewe, H.K.,Notley, L.M.,Wunsch, R.M., et al. Metabolism of tamoxifen by recombinant human cytochrome P450 enzymes: Formation of the 4-hydroxy, 4-hydroxy and N-desmethyl metabolites and isomerization of trans-4-hydroxytamoxifen. Drug Metabolism and Disposition 30(8), 869-874 (2002). 2.Desta, Z.,Ward, B.A.,Soukhova, N.V., et al. Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: Prominent roles for CYP3A and CYP2D6. Journal of Pharmacology and Experimental Therapeutics 310(3), 1062-1075 (2004). 3.Dahmane, E.,Boccard, J.,Csajka, C., et al. Quantitative monitoring of tamoxifen in human plasma extended to 40 metabolites using liquid-chromatography high-resolution mass spectrometry: New investigation capabilities for clinical pharmacology. Analytical and Bioanalytical Chemistry 406(11), 2627-2640 (2016). 4.Katzenellenbogen, B.S.,Norman, M.J.,Eckert, R.L., et al. Bioactivities, estrogen receptor interactions, and plasminogen activator-inducing activities of tamoxifen and hydroxy-tamoxifen isomers in MCF-7 human breast cancer cells. Cancer Res. 44(1), 112-119 (1984). | |
运输条件 | Wet ice in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 387.5 |
分子式 | C26H29NO2 |
CAS号 | 68047-06-3 |
稳定性 | ≥ 2 years |
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