MK-0448

MK-0448 is a potent, specific I(Kur) current/Kv1.5 channel inhibitor with IC50 of 8.6 nM, potently inhibits IKur in human atrial myocytes with IC50 of 10.8 nM; also demonstrates a potent effect on currents associated with other Kv1.x and Kv2.x subunits, such as Kv1.7 and Kv2.1, with IC50 of 72 and 61 nM, respectively; displays >70-fold concentration than inhibition of IKur; significantly causes prolongation of the atrial refractory period in normal anesthetized dogs. Heart Arrhythmia Phase 1 Clinical

References 1. Pavri BB, et al. Circ Arrhythm Electrophysiol. 2012 Dec;5(6):1193-201. 2. Loose S, et al. Front Pharmacol. 2014 Mar 4;5:26. 3. Wolkenberg SE, et al. Bioorg Med Chem Lett. 2017 Feb 15;27(4):1062-1069. View Related Products by Target Potassium Channel Heart Arrhythmia