VU0240551 is a K+/Cl- cotransporter 2 (KCC2) inhibitor (IC50 = 568 nM).1 It selectively inhibits KCC2 over Na+/K+/Cl- cotransporter 1 (NKCC1; IC50 = >50 ?M) but does inhibit the activity of adenosine A1 and A3 receptors, as well as inhibits activity of L-type calcium channels at the benzothiazepine site and human ether-a-go-go-related gene (hERG) potassium channels by greater than 50% in a panel of 68 receptors, ion channels, and transporters at 10 ?M. VU0240551 decreases potassium ion uptake by 70% in HEK293 cells expressing KCC2 when used at a concentration of 1 ?M.
1.Delpire, E., Days, E., Lewis, L.M., et al.Small-molecule screen identifies inhibitors of the neuronal K-Cl cotransporter KCC2Proc. Natl. Acad. Sci. USA106(13)5383-5388(2009)