Powder: -20°C for 3 years | In solvent: -80°C for 2 years
Vesnarinone HCl 是一种具有口服活性的 phosphodiesterase 3 (PDE3) 抑制剂。Vesnarinone HCl 可对钙离子和钾离子进行调节, 增加钙通量,减少钾通量。Vesnarinone HCl 是一种新的正性肌力化合物,可增强心肌收缩力,可用于心力衰竭的研究。
产品描述 | Vesnarinone HCl is an orally active phosphodiesterase 3 (PDE3) inhibitor.Vesnarinone HCl modulates calcium and potassium ions, increasing calcium flux and decreasing potassium flux.Vesnarinone HCl is a new positive inotropic compound that enhances myocardial contractility and can be be used in heart failure studies. |
靶点活性 | PDE3A:10.7 μM, PDE3B:13.2 μM, ERG1:1.1 μM |
体外活性 | Vesnarine (60 and 100 μg/mL; 48 h) in a dose-dependent manner to inhibit cell growth.[3] Vesnarine (60 μg/mL; 48 h) induces G1 phase arrest and cell apoptosis.[3] Vesnarine (60 μg/mL; 0, 12, 24, and 48 h) increased the expression of p21 mRNA and slightly decreased the p21 protein.[3] |
体内活性 | Vesnarinone (3-300 μM) increases contractile tension in isolated ventricular muscles of dogs, cats, rabbits, and guinea pig in a dose-dependent manner.[5] Vesnarinone (Oral and i.v.) administration of vesnarinone increases right ventricular pressure with no effect on heart rate in dog models of tricuspid insufficiency- and pulmonary stenosis-induced congestive heart failure. It also increases contractility and coronary flow while decreasing heart rate in a guinea pig model of aortic stenosis-induced congestive heart failure. Formulations containing vesnarinone have been used for the treatment of congestive heart failure.[6] |
别名 | Vesnarinone HCl(81840-15-5 Free base), OPC-8212 HCl |
分子量 | 431.91 |
分子式 | C22H26ClN3O4 |
CAS No. | T3465L |
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
( < 1 mg/mL refers to the product slightly soluble or insoluble )
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
Vesnarinone HCl T3465L Membrane transporter/Ion channel Metabolism Calcium Channel Potassium Channel PDE Vesnarinone HCl(81840-15-5 Free base) OPC-8212 HCl Inhibitor inhibitor inhibit