| 货号 | 16924-1g |
| 描述 | The aryl hydrocarbon receptor (AhR) is a ligand-activated transcription factor that promotes the expression of phase I and II xenobiotic chemical metabolizing enzyme genes, including the cytochrome P450 (CYP) isoforms CYP1A1 and CYP1A2.1 α-Naphthoflavone is a flavone that modulates xenobiotic metabolism at several points. It antagonizes AhR, blocking the expression of phase I and II genes at nanomolar concentrations, although it can agonize AhR at higher concentrations (10 µM).2,3 α-Naphthoflavone inhibits CYP19 (aromatase), CYP1A1, CYP1A2, and CYP1B1 (IC50s = 500, 60, 6, and 5 nM, respectively), whereas it activates CYP3A4 (Kd = 7.4 µM).4,5,6 Dietary α-naphthoflavone can contribute to carcinogenesis in the presence of synthetic estrogens.7 |
| 别名 | 7,8-Benzoflavone;NSC 407011; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Denison, M.S., and Nagy, S.R. Activation of the aryl hydrocarbon receptor by structurally diverse exogenous and endogenous chemicals. Annual Reviews of Pharmacology and Toxicology 43, 309-334 (2003). 2.Smith, K.J.,Murray, I.A.,Tanos, R., et al. Identification of a high-affinity ligand that exhibits complete aryl hydrocarbon receptor antagonism. Journal of Pharmacology and Experimental Therapeutics 338(1), 318-327 (2011). 3.Wilhelmsson, A.,Whitelaw, M.L.,Gustafsson, J.A., et al. Agonistic and antagonistic effects of α-naphthoflavone on dioxin receptor function. Role of the basic region helix-loop-helix dioxin receptor partner factor Arnt. J.Biol.Chem 269(29), 19028-19033 (1994). 4.Bruno, R.D., and Njar, V.C.O. Targeting cytochrome P450 enzymes: A new approach in anti-cancer drug development. Bioorganic & Medicinal Chemistry 15(15), 5074-5060 (2007). 5.Campbell, D.R., and Kurzer, M.S. Flavonoid inhibition of aromatase enzyme activity in human preadipocytes. Journal of Steroid Biochemistry and Molecular Biology 46, 381-388 (1993). 6.Sineva, E.V.,Rumfeldt, J.A.O.,Halpert, J.R., et al. A large-scale allosteric transition in cytochrome P450 3A4 revealed by luminescence resonance energy transfer (LRET). PLoS One 8(12), 1-13 (2013). 7.Metzler, M.,Blaich, G., and Tritscher, A.M. Role of metabolic activation in the carcinogenicity of estrogens: Studies in an animal liver tumor model. Environmental Health Perspectives 88, 117-121 (1990). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 272.3 |
| 分子式 | C19H12O2 |
| CAS号 | 604-59-1 |
| 稳定性 | ≥ 2 years |
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