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Vardenafil dihydrochloride

Vardenafil dihydrochloride

产品编号 T4480   CAS 224789-15-5
别名: Levitra, Vardenafil Hydrochloride, 二盐酸伐地那非

Vardenafil dihydrochloride (Levitra) 是一种新型 PDE 抑制剂,对 PDE5 和 PDE1 的 IC50 分别为 0.7 和 180 nM。

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Vardenafil dihydrochloride Chemical Structure
Vardenafil dihydrochloride, CAS 224789-15-5
规格 价格/CNY 货期 数量
25 mg ¥ 457 待询
50 mg ¥ 822 待询
100 mg ¥ 1,480 待询
200 mg ¥ 2,624 待询
1 mL * 10 mM (in DMSO) ¥ 784 待询

Vardenafil dihydrochloride 的其他形式现货产品:

Vardenafil hydrochloride Vardenafil hydrochloride trihydrate Vardenafil
其他形式的 Vardenafil dihydrochloride:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
产品目录号及名称: Vardenafil dihydrochloride (T4480)
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参考文献
产品描述 Vardenafil dihydrochloride (Levitra) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.
靶点活性 PDE5:0.7 nM (Cell-free), PDE1:180 nM (Cell-free)
体外活性 Vardenafil specifically inhibits the hydrolysis of cGMP by PDE5 with an IC50 of 0.7 nM (6.6 nM). Vardenafil significantly enhances the SNP-induced relaxation of human trabecular smooth muscle at 3 nM (10 nM). Vardenafil also significantly potentiates both ACh-induced and transmural electrical stimulation-induced relaxation of trabecular smooth muscle. Vardenafil (100 mM) increases cyclic GMP levels in rat hippocampal slices. Vardenafil, tadalafil, and Sildenafil each competitively inhibit cGMP hydrolysis by phosphodiesterase-5 (PDE5), thereby fostering cGMP accumulation and relaxation of vascular smooth muscle.
体内活性 Vardenafil dose-dependently potentiates erectile responses to intravenously administered sodium nitroprusside in rabbit. Vardenafil (3 mg/kg, p.o.) results in an improved object discrimination performance in rats. Vardenafil (30 mg/L, p.o.) increases both iNOS and proliferating cell nuclear antigen expression (SM cell replication) in rats, with normalization of the dynamic infusion cavernosometry drop rate and SM/collagen ratio. Vardenafil induces powerful preconditioning-like cardioprotective effect against ischemia/reperfusion injury through the opening of mitochondrial K(ATP) channels in the heart of rabbit. Vardenafil protects the ischemic myocardium against reperfusion injury through a mechanism dependent on mitochondrial K(ATP) channel opening.
别名 Levitra, Vardenafil Hydrochloride, 二盐酸伐地那非
分子量 561.52
分子式 C23H34Cl2N6O4S
CAS No. 224789-15-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: 10 mg/mL (17.27 mM)

Ethanol: 16 mg/mL (27.6 mM)

DMSO: 93 mg/mL (160.6 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / Ethanol / DMSO 1 mM 1.7809 mL 8.9044 mL 17.8088 mL 44.522 mL
5 mM 0.3562 mL 1.7809 mL 3.5618 mL 8.9044 mL
10 mM 0.1781 mL 0.8904 mL 1.7809 mL 4.4522 mL
Ethanol / DMSO 20 mM 0.089 mL 0.4452 mL 0.8904 mL 2.2261 mL
DMSO 50 mM 0.0356 mL 0.1781 mL 0.3562 mL 0.8904 mL
100 mM 0.0178 mL 0.089 mL 0.1781 mL 0.4452 mL

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TargetMol Library Books参考文献

1. Saenz d T I, et al. The phosphodiesterase inhibitory selectivity and the in vitro and in vivo potency of the new PDE5 inhibitor vardenafil[J]. International Journal of Impotence Research, 2001, 13(5):282. 2. Prickaerts J, et al. Effects of two selective phosphodiesterase type 5 inhibitors, sildenafil and vardenafil, on object recognition memory and hippocampal cyclic GMP levels in the rat[J]. Neuroscience, 2002, 113(2):351-361. 3. Blount M A, et al. Binding of tritiated sildenafil, tadalafil, or vardenafil to the phosphodiesterase-5 catalytic site displays potency, specificity, heterogeneity, and cGMP stimulation[J]. Molecular Pharmacology, 2004, 66(1):144-152. 4. Ferrini M G, et al. Vardenafil prevents fibrosis and loss of corporal smooth muscle that occurs after bilateral cavernosal nerve resection in the rat[J]. Urology, 2006, 68(2):429-435. 5. Salloum F N, et al. Sildenafil and Vardenafil but not Nitroglycerin Limit Myocardial Infarction through Opening of Mitochondrial KATP Channels when Administered at Reperfusion following Ischemia in Rabbits[J]. Journal of Molecular & Cellular Cardiology, 2007, 42(2):453-458.
Deltasonamide 2 hydrochloride Thioquinapiperifil dihydrochloride Sulmazole Carbodenafil Isomazole Balipodect Pomiferin Vardenafil hydrochloride

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

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