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伐地那非 /Vardenafil {[allProObj[0].p_purity_real_show]}

货号:A277692

Vardenafil是一种用于治疗勃起功能障碍的 PDE5 抑制剂。

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Vardenafil 化学结构 CAS号:224785-90-4
Vardenafil 化学结构
CAS号:224785-90-4
Vardenafil 3D分子结构
CAS号:224785-90-4
Vardenafil 化学结构 CAS号:224785-90-4
Vardenafil 3D分子结构 CAS号:224785-90-4
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Vardenafil 纯度/质量文件 产品仅供科研

货号:A277692 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 PDE PDE1 PDE10A PDE2 PDE3 PDE4 PDE5 PDE6 其他靶点 纯度
Doxofylline 99+%
Deltarasin +++

PDEδ , Kd: 38 nM

99+%
7-(2,3-Dihydroxypropyl)theophylline 98%
Aminophylline +

PDE, IC50: 0.12 mM

98+%
Anagrelide HCl 99%+
Irsogladine mAChR,AChR 99%
PF-8380 +++

Autotaxin, IC50: 2.8 nM

99%+
Dipyridamole 98%
Balipodect ++++

PDE10A, IC50: 0.3 nM

99%+
PF-2545920 ++++

PDE10A, IC50: 0.37 nM

97%
Luteolin +

PDE1, Ki: 15.0 μM

++

PDE2, Ki: 6.4 μM

+

PDE3, Ki: 13.9 μM

+

PDE4, Ki: 11.1 μM

+

PDE5, Ki: 9.5 μM

98%
Milrinone ++

PDE2, IC50: 5.2 μM

++

PDE3, IC50: 2.1 μM

ATPase 99%
Pimobendan ++

PDE3, IC50: 0.32 μM

98%
Cilostazol ++

PDE3, IC50: 0.2 μM

98%
Fenspiride HCl +

PDE3, pIC50: 3.44

+

PDE4, pIC50: 4.16

99% (HPLC)
(S)-(+)-Rolipram ++

PDE4, IC50: 0.75 μM

99% (HPLC)
Apremilast +++

PDE4, IC50: 74 nM

98%
GSK256066 ++++

PDE4B, IC50: 3.2 pM

98+%
Roflumilast ++++

PDE4A1, IC50: 0.7 nM

PDE4A4, IC50: 4.3 nM

99%
Rolipram +++

PDE4B, IC50: 130 nM

99%+
Cilomilast +++

LPDE4, IC50: 100 nM

HPDE4, IC50: 120 nM

99%
Avanafil ++++

PDE5, IC50: 1 nM

98%
Vardenafil HCl Trihydrate ++++

PDE5, IC50: 0.7 nM

98%
Tadalafil ++++

PDE5, IC50: 1.8 nM

98%
Icariin ++

PDE5, IC50: 0.432 μM

98%
Sildenafil +++

PDE6, IC50: 33 nM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Vardenafil 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].

Vardenafil 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 <<

Vardenafil 参考文献

[1]Goldstein I, Young JM, et al. Vardenafil, a new phosphodiesterase type 5 inhibitor, in the treatment of erectile dysfunction in men with diabetes: a multicenter double-blind placebo-controlled fixed-dose study. Diabetes Care. 2003 Mar;26(3):777-83.

[2]Saenz de Tejada I, Angulo J, et al. The phosphodiesterase inhibitory selectivity and the in vitro and in vivo potency of the new PDE5 inhibitor vardenafil. Int J Impot Res. 2001 Oct;13(5):282-90.

[3]Ashour AE, Rahman AF, Kassem MG. Vardenafil dihydrochloride. Profiles Drug Subst Excip Relat Methodol. 2014;39:515-44

[4]Saenz de Tejada I, Angulo J, Cuevas P, Fernández A, Moncada I, Allona A, Lledó E, Körschen HG, Niewöhner U, Haning H, Pages E, Bischoff E. The phosphodiesterase inhibitory selectivity and the in vitro and in vivo potency of the new PDE5 inhibitor vardenafil. Int J Impot Res. 2001 Oct;13(5):282-90

[5]Bourne MH Jr, Kottom TJ, Hebrink DM, Choudhury M, Leof EB, Limper AH. Vardenafil Activity in Lung Fibrosis and In Vitro Synergy with Nintedanib. Cells. 2021 Dec 11;10(12):3502

Vardenafil 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.05mL

0.41mL

0.20mL

10.23mL

2.05mL

1.02mL

20.47mL

4.09mL

2.05mL

Vardenafil 技术信息

CAS号224785-90-4
分子式C23H32N6O4S
分子量 488.603
别名
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place,Inert atmosphere,Room temperature

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
动物实验配方
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