2-hydroxy Flutamide
货号：
15271-5mg 基本售价：
910.0 元 规格：
5 mg
产品信息
概述| 货号 | 15271-5mg |
| 描述 | 2-hydroxy Flutamide is the major metabolite formed during the metabolism of the non-steroidal antiandrogen flutamide by cytochrome P450 (CYP) isoforms CYP1A2 and CYP3A4.1 Through competitive inhibition of the binding of testosterone to the nuclear androgen receptor (AR; IC50 = ~300-900), 2-hydroxy flutamide blocks the expression of AR target genes and prevents androgen-dependent stabilization of the AR.2 Compared to flutamide, 2-hydroxy flutamide is a more potent antiandrogen in vivo, demonstrating a higher binding affinity for the AR (0.1% binding affinity relative to dihydrotestosterone) and, thus, is the predominant contributor to the therapeutic effects of flutamide in the treatment of prostate cancer.3 |
| 别名 | Hydroxyniphtholide;SCH 16423; |
性能| 供应商 | Cayman |
| 应用文献 |
1.Shet, M.S.,McPhaul, M.,Fisher, C.W., et al. Metabolism of the antiandrogenic drug (flutamide) by human CYP1A2. Drug Metabolism and Disposition 25(11), 1298-1303 (1997).
2.Kolvenbag, G.J.C.M.,Furr, B.J.A. and Blackledge, G.R.P. Receptor affinity and potency of non-steroidal antiandrogens: Translation of preclinical findings into clinical activity. Prostate Cancer Prostatic Dis. 1(6), 307-314 (1998).
3.Gao, W.,Kim, J. and Dalton, J.T. Pharmacokinetics and pharmacodynamics of nonsteroidal androgen receptor ligands. Pharmaceutical Research 23(8), 1641-1658 (2006).
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| 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 | 292.2 |
| 分子式 | C11H11F3N2O4 |
| CAS号 | 52806-53-8 |
| 稳定性 | ≥ 2 years |
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