1189700-56-8

White Crystalline Solid

Labeled Dofitilide, intended for use as an internal standard for the quantification of Dofitilide by GC- or LC-mass spectrometry.

Potassium channel blocker

Dofetilide-d₄ is intended for use as an internal standard for the quantification of dofetilide by GC- or LC-MS. Dofetilide is a class III antiarrhythmic agent that prolongs cardiac action potential duration by selectively inhibiting the rapidly activating inward rectifying component of net delayed rectifier K⁺ current (IC₅₀ = 31.5 nM in guinea pig cardiomyocytes). However, at 1 μM, dofetilide has pro-arrhythmic activity, inducing early afterdepolarizations (prolonged repolarization) in cell models and Torsade de Pointes in a rabbit screen for proarrhythmic properties when administered at a dose of 10 mg/kg. Formulations containing dofetilide have been used in the treatment of highly symptomatic atrial fibrillation and the conversion of flutter to normal sinus rhythm.

Store at -20°C

[1] N K JURKIEWICZ  M C S. Rate-dependent prolongation of cardiac action potentials by a methanesulfonanilide class III antiarrhythmic agent. Specific block of rapidly activating delayed rectifier K+ current by dofetilide.[J]. Circulation research, 1993, 72 1: 75-83. DOI: 10.1161/01.res.72.1.75
[2] L NALOS. Comparison of the IKr blockers moxifloxacin, dofetilide and E-4031 in five screening models of pro-arrhythmia reveals lack of specificity of isolated cardiomyocytes[J]. British Journal of Pharmacology, 2011, 165 2: 467-478. DOI: 10.1111/j.1476-5381.2011.01558.x
[3] ALBERT DUNNINK. Ventricular remodelling is a prerequisite for the induction of dofetilide-induced torsade de pointes arrhythmias in the anaesthetized, complete atrio-ventricular-block dog.[J]. Europace, 2012, 14 3: 431-436. DOI: 10.1093/europace/eur311