Uses
A cell-permeable, renal outer medullary potassium (ROMK) blocker that is shown to inhibit inward rectifier potassium channel, K
ir2.1 (IC
50 = 1.8 µM and 290 nM, at pH 7.4 and pH 8.5, respectively). It exhibits little selectivity against other members of the K
ir2.x family, but has no effect on K
ir1.1 (IC
50 >300 µM) and displays weak activity for K
ir4.1 and K
ir7.1 (IC
50 = 76 µM and 33 µM, respectively). It is reported to be assayed in 218 MLPCN HTS campaigns, demonstrating activity in only two assays that are not based on K
ir2.1. Furthermore, it displays a relatively clean profile in a radioligand binding panel of 68 GPCRs, ion channels and transporters.
