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| 品牌 | absin | CAS | 115256-11-6 |
|---|---|---|---|
| 分子式 | C19H27N3O5S2 | 纯度 | 98% |
| 分子量 | 441.56 | 货号 | abs47028326 |
| 规格 | 5mg | 供货周期 | 现货 |
| 主要用途 | is a sulfonamide class III antiarrhythmi | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
Dofetilide 115256-11-6
| 产品描述 | |
| 描述 | Dofetilide 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. |
| 纯度 | 98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | 多非利特；UK 68789 |
| 外观 | white to off-white |
| 可溶性/溶解性 | DMSO : 44.2 mg/mL (100 mM) |
| 生物活性 | |
| 靶点 | Potassium channel |
| In vitro(体外研究) | Dofetilide blocks HERG currents in excised macro patches of Xenopus oocytes. 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. 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. |
| In vivo(体内研究) | 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. Dofetilide causes increased resorptions and the same stage-dependent malformations in Sprague-Dawley rats. |
| 参考文献 | |
| 参考文献 |
| 研究领域 | |
| 研究领域 | Cardiovascular Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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