Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Dofetilide (UK 68789) 是一种具有口服活性、有效的且特异性的IKr 阻滞剂,作为 III 类抗心律失常药物。Dofetilide 可用于心血管疾病研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 155 | 现货 | ||
5 mg | ¥ 319 | 现货 | ||
10 mg | ¥ 558 | 现货 | ||
25 mg | ¥ 987 | 现货 | ||
50 mg | ¥ 1,570 | 现货 | ||
100 mg | ¥ 2,220 | 现货 | ||
200 mg | ¥ 3,730 | 现货 | ||
500 mg | ¥ 5,960 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 317 | 现货 |
产品描述 | Dofetilide (UK 68789) is a sulfonamide class III antiarrhythmic agent and potassium channel blocker. Dofetilide selectively blocks cardiac ion channels of the rapid component of the delayed rectifier potassium current Ikr. This antiarrhythmic agent prolongs cardiac action potential duration and effective refractory period due to delayed repolarization without affecting conduction velocity. This results in a normal sinus rhythm. Dofetilide is used in the treatment of atrial fibrillation and flutter. |
体外活性 | Dofetilide blocks HERG currents in excised macro patches of Xenopus oocytes. [1] Dofetilide (1 μM) reduces the amplitude of IKr to 61% of control currents in guinea pig cardiomyocytes, as measured by 200-ms test pulses and analysis of the deactivating tail currents of IKr. [2] Dofetilide increases apico-basal disparity of repolarization, due to a more marked increase of ERPs in the apex than in the base in the intact canine heart. [3] |
体内活性 | Dofetilide (100 mg/kg, i.v.) does not suppress automaticity arrhythmias induced by two-stage coronary ligation and epinephrine or the coronary ligation and reperfusion arrhythmias, but suppresses the reentry arrhythmia induced by PES in dogs with old myocardial infarction (MI). Dofetilide also shows antiarrhythmic effect in some dogs with digitalis arrhythmia. Dofetilide increases QT interval and shows negative chronotropic effect like that of other class III drugs, but is different in antiarrhythmic profiles from those of other class III agents such as D-sotalol, E-4031, and MS-551 in that it does not prevent the occurrence of ventricular fibrillation (VF) immediately after coronary reperfusion and has some antiarrhythmic effects on digitalis arrhythmia. [4] Dofetilide causes increased resorptions and the same stage-dependent malformations in Sprague-Dawley rats. [5] |
别名 | UK 68789, UK-68798, Tikosyn, 多非利特 |
分子量 | 441.56 |
分子式 | C19H27N3O5S2 |
CAS No. | 115256-11-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 44.2 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2647 mL | 11.3235 mL | 22.647 mL | 56.6174 mL |
5 mM | 0.4529 mL | 2.2647 mL | 4.5294 mL | 11.3235 mL | |
10 mM | 0.2265 mL | 1.1323 mL | 2.2647 mL | 5.6617 mL | |
20 mM | 0.1132 mL | 0.5662 mL | 1.1323 mL | 2.8309 mL | |
50 mM | 0.0453 mL | 0.2265 mL | 0.4529 mL | 1.1323 mL | |
100 mM | 0.0226 mL | 0.1132 mL | 0.2265 mL | 0.5662 mL |
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。
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。
Dofetilide 115256-11-6 Membrane transporter/Ion channel Potassium Channel cardiovascular UK68798 UK68789 potent specific class antiarrhythmic UK 68789 UK-68798 orally UK-68789 Inhibitor Tikosyn inhibit KcsA UK 68798 III agent 多非利特 inhibitor