GW 542573X

GW 542573X is an activator of small-conductance calcium-activated potassium channel KCa2.1/SK1. It increases current in an inside-out patch clamp assay using HEK293 cells expressing the human channel (EC50 = 8. µM). GW 542573X is selective for KCa2.1/SK1 over KCa2.2/SK2, KCa2.3/SK3, and intermediate-conductance calcium-activated potassium channel KCa3.1/IK in whole-cell patch clamp assays using HEK293 cells expressing the human channels at 10 µM, as well as the voltage-gated sodium channel Nav1. N-type voltage-gated calcium channel Cav2. voltage-gated potassium channel Kv1. purinergic P2X2/3 receptor, and alpha7 nicotinic acetylcholine receptor (nAChR) at 30 µM. In vivo, GW 542573X (15 mg/kg) decreases freezing time in contextual fear but not cued fear memory tests in mice when administered prior to the conditioning period.. Solulibility: DMSO: Sparingly soluble: 1-10 mg/ml: Ethanol: Sparingly soluble: 1-10 mg/ml, PBS (pH 7.2): Soluble: =10 mg/ml.