Application

ML277 has been used as the KCNQ1 activator to treatcells in lung metastasisassay.

Biochem/physiol Actions

ML277 is a potent activator of KCNQ1 (Kv7.1) channels with >100-fold selectivity versus KCNQ2 and KCNQ4 and no activity against the hERG potassium channel up to 30 µM. KCNQ1 is a voltage-gated potassium channel required for repolarization phase of the cardiac action potential. Mutations in the KCNQ1 gene are associated with long QT syndrome (LQTS), a disorder in which the heart muscles take longer than normal to recover after each heart beat and can lead to dangerous arrhythmias such as atrial fibrillation. Activators of KCNQ1 channels could have potential use in treatments of LQTS. ML277 is the first selective and potent activator found, with an EC₅₀ of 260 nM.

Features and Benefits

This compound is featured on the Potassium Channels page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Packaging

5, 25 mg in glass bottle