货号 | 14930-100mg |
描述 | Selective inhibitors of phosphodiesterase 5 (PDE5), which specifically hydrolyzes cGMP, are used to study signaling through the guanylate cyclase activator nitric oxide and to mediate smooth muscle relaxation and vasodilation triggered by cGMP.1 Vardenafil is a potent inhibitor of PDE5 (IC50 = 0.2-1.2 nM) that less effectively blocks the activities of PDE6, PDE1, and PDE11 (IC50s = 2, 230, and 130 nM, respectively).2,3,4 PDE5 inhibitors, including vardenafil, have applications in several conditions, including erectile dysfunction, pulmonary arterial hypertension, and lower urinary tract dysfunction.5,6,7 |
供应商 | Cayman |
应用文献 | |
1.Rotella, D.P. Phosphodiesterase 5 inhibitors: Current status and potential applications. Nature Reviews.Drug Discovery 1, 674-682 (2002). 2.Card, G.L.,England, B.P.,Suzuki, Y., et al. Structural basis for the activity of drugs that inhibit phosphodiesterases. Structure 12(12), 2233-2247 (2004). 3.Boyle, C.D.,Xu, R.,Asberom, T., et al. Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED. Bioorganic & Medicinal Chemistry Letters 15(9), 2365-2369 (2005). 4.Smith, W.B., II,McCaslin, I.R.,Gokce, A., et al. PDE5 inhibitors: Considerations for preference and long-term adherence. International Journal of Clinical Practice 67(8), 768-780 (2013). 5.Galiè, N.,Negro, L. and Simonneau, G. The use of combination therapy in pulmonary arterial hypertension: New developments. Eur.Respir.Rev. 18(113), 148-153 (2009). 6.DeNinno, M.P. Future directions in phosphodiesterase drug discovery. Bioorganic & Medicinal Chemistry Letters 22(22), 6794-6800 (2012). 7.Yamaguchi, O. Latest treatment for lower urinary tract dysfunction: Therapeutic agents and mechanism of action. Int.J.Urol. 20(1), 28-39 (2013). | |
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 | 579.1 |
分子式 | C23H32N6O4S • HCl [3H2O] |
CAS号 | 330808-88-3 |
稳定性 | ≥ 2 years |
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