货号 | 14938-50mg |
描述 | 5α-Reductase catalyzes the NADPH-dependent reduction of Δ4,5 double bonds in several steroid substrates, including testosterone, which is converted to dihydrotestosterone, the primary mediator of prostate growth.1 The 5α-reductase enzymes responsible for the reduction of testosterone to dihydrotestosterone exists 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 Finasteride is a 4-azasteroid analog of testosterone that competitively blocks type II 5α-reductase activity (IC50 = 4.2 nM) with 100-fold greater affinity than for the type I enzyme.2 It has been used in the treatment of benign prostatic hyperplasia, decreasing human prostatic dihydrotestosterone levels by 70-90% and reducing prostatic size.2 However, at 10 μM finasteride has also been shown to induce the expression of Nrf2 and HO-1 proteins in androgen refractory prostrate PC-3 cells, which has been implicated in increased high-grade prostate tumor formation.3 Also, at 0.1 μM finasteride can inhibit testosterone-induced type I procollagen and TGF-β1 expression in human scalp dermal fibroblasts in a model of androgenic alopecia.4 |
别名 | MK-906;Propecia®;Proscar®; |
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.Yun, D.K.,Lee, J. and Keum, Y.S. Finasteride increases the expression of hemoxygenase-1 (HO-1) and NF-E2-related factor-2 (Nrf2) proteins in PC-3 cells: Implication of finasteride-mediated high-grade prostate tumor occurence. Biomol.Ther.(Seoul) 21(1), 49-53 (2013). 4.Yoo, H.G.,Kim, J.S.,Lee, S.R., et al. Perifollicular fibrosis: Pathogenetic role in androgenetic alopecia. Biological and Pharmaceutical Bullentin 29(6), 1246-1250 (2006). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥95% |
计算分子量 | 372.5 |
分子式 | C23H36N2O2 |
CAS号 | 98319-26-7 |
稳定性 | ≥ 2 years |
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