| 货号 | 15956-100mg |
| 描述 | 5α-reductase catalyzes the NADPH-dependent reduction of Δ4,5 double bonds in several steroid substrates, including testosterone (Item No. 15645), which is converted to dihydrotestosterone, the primary mediator of prostate growth.1 The 5α-reductase enzymes responsible for the reduction of testosterone to dihydrotestosterone exist as two forms: type I, which occurs in the skin, liver, and ventral prostate and type II, which is expressed in ventral prostate, epididymis, and other reproductive tissues.2 Dutasteride is a time-dependent, dual inhibitor of 5α-reductase (apparent Kis = 17 and 4.3 nM at 10 and 30 minute reaction times, respectively) that is frequently used in the treatment of benign prostatic hyperplasia.3,4 Compared to finasteride (Item No. 14938), a selective inhibitor of type II 5α-reductase, dutasteride has a greater terminal half-life (1 vs. 14 hours in rat, respectively) and is more effective at decreasing serum levels of dihydrotestosterone at single doses > 10 mg.4 Dutasteride has also been used as a strategy to reduce androgen levels related to prostate tumor burden on androgen receptor activity.5 |
| 别名 | Avodart®; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.George, F.W.,Russell, D.W. and Wilson, J.D. Feed-forward control of prostate growth: Dihydrotestosterone induces expression of its own biosynthetic enzyme, steroid 5α-reductase. Proceedings of the National Academy of Sciences of the United States of America 88(18), 8044-8047 (1991). 2.Flores, E.,Bratoeff, E.,Cabeza, M., et al. Steroid 5α-reductase inhibitors. Mini Rev.Med.Chem. 3(3), 225-237 (2003). 3.Makridakis, N. and Reichardt, J.K. Pharmacogenetic analysis of human steroid 5α reductase type II: Comparison of finasteride and dutasteride. Journal of Molecular Endocrinology 34(3), 617-623 (2005). 4.Bramson, H.N.,Hermann, D.,Batchelor, K.W., et al. Unique preclinical characteristics of GG745, a potent dual inhibitor of 5AR. Journal of Pharmacology and Experimental Therapeutics 282(3), 1496-1502 (1997). 5.Nacusi, L.P. and Tindall, D.J. Targeting 5α-reductase for prostate cancer prevention and treatment. Nat.Rev.Urol. 8(7), 378-384 (2011). | |
| 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 | 528.5 |
| 分子式 | C27H30F6N2O2 |
| CAS号 | 164656-23-9 |
| 稳定性 | ≥ 2 years |
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