SKA-121

A positive-gating modulator of IKCa1/KCa3.1 channels (EC50 = 109 nM); selective for KCa3.1 over KCa2.1, KCa2.2 and KCa2.3 (EC50s = 8,700, 6,800, and 4,400 nM, respectively), KCa1.1 as well as voltage-gated potassium and sodium channels; potentiates calcium-evoked KCa currents by approximately 7-fold (1 µM) as well as calcium-evoked and basal KCa currents; potentiates bradykinin-induced endothelium-dependent relaxation (EC50 = 7.9 nM) in large porcine coronary arteries ex vivo; lowers MAP ) by approximately 20 and 25 mm Hg in normo- and hypertensive mice (100 mg/kg)