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概述
Vardenafil HCl Trihydrate是一种新型PDE抑制剂，作用于PDE5和PDE1，IC50分别为0.7和180 nM。
Information
Vardenafil HCl Trihydrate (BAY38-9456) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.
In vitro
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.
In vivo
Vardenafil dose-dependently potentiates erectile responses to intravenously administered sodium nitroprusside in rabbit. [1] 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 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.
Cell Data
cell lines：
Concentrations：
Incubation Time：
Powder Purity:≥99%
规格
别名
伐地那非盐酸盐三水合物
英文别名
BAY38-9456 | 2-(2-ethoxy-5-(4-ethylpiperazin-1-ylsulfonyl)phenyl)-5-methyl-7-propylimidazo[1,5-f][1,2,4]triazin-4(3H)-one hydrochloride trihydrate
规格或纯度
10mM in DMSO
英文名称
Vardenafil HCl Trihydrate
生化机理
盐酸伐地那非三水合物（BAY38-9456）是一种新型 PDE 抑制剂，对 PDE5 和 PDE1 的 IC50 分别为 0.7 和 180 nM。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
EC号
685-133-8
分子类型
小分子
Isomeric SMILES
CCCC1=NC(=C2N1N=C(NC2=O)C3=C(C=CC(=C3)S(=O)(=O)N4CCN(CC4)CC)OCC)C.O.O.O.Cl
关联CAS
PubChem CID
分子量
579.11
高级数据
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 74 mg/mL (200.34 mM); Water: Insoluble; Ethanol: Insoluble;
安全和危险性（GHS）
象形图
信号词
警告
危险声明
H302: 吞食有害
预防措施声明
P501: 将内容物/容器送到批准的废物处理厂处理
P264: 处理后要彻底洗手。
P270: 使用本产品时，请勿进食、饮水或吸烟。
P330: 漱口
P301+P317: 如果被吞咽：请寻求医疗帮助。
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
此产品的引用文献
溶液计算器
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危险品化学品经营许可证（带存储）