LUF7244, a selective allosteric modulator of K v 11.1 channels, effectively suppresses early afterdepolarizations and holds potential for anti-arrhythmia research [1].

LUF7244, at concentrations ranging from 0 to 10 μM, specifically targets and binds to Kv11.1 channels in HEK293 cells, thereby enhancing the IKv11.1 by preventing its inactivation in a dose-responsive manner [1]. In cardiomyocytes within the same concentration range, LUF7244 significantly shortens the action potential duration (APD) by about 50% and mitigates dofetilide-induced early afterdepolarizations (EAD) in isolated ventricular cardiomyocytes from both SR and CAVB dogs [1]. At a concentration of 10 μM, LUF7244 does not affect the currents I_KIR2.1, I_Nav1.5, I_Ca-L, and I_Ks, but it notably increases I_Kr twofold [1].

LUF7244, administered intravenously at a dosage of 2.5 mg/kg over 15 minutes, effectively reduces repolarization parameters and exhibits antiarrhythmic properties, mitigating dofetilide-induced Torsades de Pointes (TdP) arrhythmias in dogs with chronic atrioventricular block (CAVB) [1].