RPR260243 is a potent, selective hERG potassium channel (Kv11.1) activator that dramatically slows current deactivation at 1-30 uM.
RPR260243-modified HERG currents is inhibited by dofetilide (IC50=58 nM), has little effect on HERG current amplitude and no significant effects on steady-state activation parameters or on channel inactivation processes, and no activator-like effects on other voltage-dependent ion channels, including the erg3 K+ channel.
RPR260243 completely reverses the action potential-prolonging effects of dofetilide in guinea pig myocytes.
