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Beschreibung

A cell-permeable, renal outer medullary potassium (ROMK) blocker that is shown to inhibit inward rectifier potassium channel, Kir2.1 (IC50 = 1.8 µ,M and 290 nM, at pH 7.4 and pH 8.5, respectively). It exhibits little selectivity against other members of the Kir2.x family, but has no effect on Kir1.1 (IC50 >300 µ,M) and displays weak activity for Kir4.1 and Kir7.1 (IC50 = 76 µ,M and 33 µ,M, respectively). It is reported to be assayed in 218 MLPCN HTS campaigns, demonstrating activity in only two assays that are not based on Kir2.1. Furthermore, it displays a relatively clean profile in a radioligand binding panel of 68 GPCRs, ion channels and transporters.