| 货号 | 14024-10mg |
| 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 Tadalafil is a potent inhibitor of PDE5 (IC50 = 1-5 nM) that also blocks the activity of PDE11 (IC50 = 10-33 nM), which hydrolyzes both cAMP and cGMP.2,3 The IC50 values for tadalafil against other isoforms of PDE are in the micromolar range.2,3 The pharmacokinetics of tadalafil are highlighted by its prolonged duration of effect.4 PDE5 inhibitors, including tadalafil, have applications in several conditions, including erectile dysfunction, pulmonary arterial hypertension, and lower urinary tract dysfunction.5,6,7,8,9 |
| 别名 | Adcirca;Cialis®; |
| 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.Curran, M.P. Tadalafil: In the treatment of signs and symptoms of benign prostatic hyperplasia with or without erectile dysfunction. Drugs & Aging 29(9), 771-781 (2012). 8.Udeoji, D.U. and Schwartz, E.R. Tadalafil as monotherapy and in combination regimens for the treatment of pulmonary arterial hypertension. Ther.Adv.Respir.Dis. 7(1), 39-49 (2013). 9.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 | 389.4 |
| 分子式 | C22H19N3O4 |
| CAS号 | 171596-29-5 |
| 稳定性 | ≥ 2 years |
| 本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。 |