ML-252 (hydrochloride)

ML-252 is a potent and selective inhibitor of the voltage-gated potassium channel subtype Kv7.2 (IC50 = 69 nM in a patch clamp assay). It is the (S)-enantiomer and is more potent than the (R)-enantiomer and the racemic mixture (IC50s = 944 and 160 nM, respectively). It is selective for Kv7.2 over other Kv channel subtypes, >68 G protein-coupled receptors, transporters, L- and N-type calcium channels, and KATP and hERG potassium channels though it does inhibit the melatonin MT1 receptor 61% when used at a concentration of 10 µM.