General description

A cell-permeable, renal outer medullary potassium (ROMK) blocker that is shown to inhibit inward rectifier potassium channel, K_ir2.1 (IC₅₀ = 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 (IC₅₀ >300 µM) and displays weak activity for K_ir4.1 and K_ir7.1 (IC₅₀ = 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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Lindsley, C.W., et al. 2011. ACS Chem. Biol.6, 845.

Packaging

5 mg in Glass bottle

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)