Vardenafil
产品说明书
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同义名 : | - |
| CAS号 : | 224785-90-4 | |
| 货号 : | A277692 | |
| 分子式 : | C23H32N6O4S | |
| 纯度 : | 98% | |
| 分子量 : | 488.603 | |
| MDL号 : | MFCD07773094 | |
| 存储条件： |
Pure form Keep in dark place,Inert atmosphere,Room temperature In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 25 mg/mL(51.17 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Vardenafil (VAR) is synthetic, highly selective, and potent inhibitor of phosphodiesterase-5 which competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. It is clinically approved for treatment of erectile dysfunction in men, including diabetic and postprostatectomy patients[3]. Vardenafil significantly enhanced the SNP-induced relaxation of human trabecular smooth muscle at 3 nM (10 nM). Vardenafil also significantly potentiated both ACh-induced and transmural electrical stimulation-induced relaxation of trabecular smooth muscle. The minimum concentration of vardenafil that significantly potentiated SNP-induced cGMP accumulation was 3 nM (30 nM). In vivo studies in rabbits showed that orally administered vardenafil dose-dependently potentiated erectile responses to intravenously administered SNP. The minimal effective dose that significantly potentiated erection was 0.1 mg/kg (1 mg/kg)[4]. Vardenafil suppresses ECM (extracellular matrix) generation alone and also exhibits significant synergistic suppression of ECM in combination with nintedanib in vitro[5]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00955929 | Penile Cancer ... 展开 >> Erectile Dysfunction Radical Prostatectomy 收起 << | Not Applicable | Active, not recruiting | August 2019 | United States, New York ... 展开 >> Memorial Sloan Kettering Cancer Center New York, New York, United States, 10065 收起 << |
| NCT02757807 | Erectile Dysfunction | Not Applicable | Unknown | December 2016 | United States, New York ... 展开 >> RMA Recruiting New York, New York, United States, 10025 Contact: Oren Fuerst, Ph.D. oren@eco-fusion.com 收起 << |
| NCT00906269 | Impotence Pro... 展开 >>static Neoplasms 收起 << | Phase 4 | Unknown | January 2013 | United States, Connecticut ... 展开 >> Hartford Hospital Recruiting Hartford, Connecticut, United States, 06106 Contact: James Graydon, MD 860-947-8500 jgraydo@harthosp.org 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.05mL 0.41mL 0.20mL |
10.23mL 2.05mL 1.02mL |
20.47mL 4.09mL 2.05mL |
| 参考文献 |
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