A cell-permeable, renal outer medullary potassium (ROMK) blocker that is shown to inhibit inward rectifier potassium channel, Kir2.1 (IC50=1.8uM and 290nM, 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 >300uM) and displays weak activity for Kir4.1 and Kir7.1 (IC50=76uM and 33uM, 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.
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
