Dofetilide

SKU: orb1300735

Description

Dofetilide is a class III antiarrhythmic agent that selectively inhibits the IKr potassium channel, prolonging the cardiac action potential. It is used in research models of atrial fibrillation and flutter to study electrophysiology and delayed repolarization in both in vitro and in vivo settings.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 115256-11-6
• MW: 441.56
• Purity: >98%
• Formula: C₁₉H₂₇N₃O₅S₂
• SMILES: N(S(C)(=O)=O)C1=CC=C(CCN(CCOC2=CC=C(NS(C)(=O)=O)C=C2)C)C=C1
• Target: Ion channel
• Solubility: Soluble in DMSO (up to 25 mg/ml).

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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.

Storage & Handling

• Storage: RT
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Tikosyn

Compound Identifiers

PubChem CID

71329