GI-530159 (ICA-069771) is a novel potent, selective, mechano-sensitive K2P channel (TERK) opener with EC50 of 1 uM for TERK1.
GI-530159 shows no activator effects on other potassium channels TASK2, KCNQ1, KCNQ2, KCNQ3 using Rb+ efflux assays or against NaV1.2, NaV1.7 and NaV1.8 (EC50>100 uM).
GI-530159 enhances TREK2 channels at 1 uM about 42 ± 6 %, but without effect on TRAAK and TASK3 channels.
GI-530159 shows a significant reduction in firing frequency and a small hyperpolarization of resting membrane potential in cultured rat DRG neurones.
