MilliporeSigma™ Calbiochem™ GIRK Activator, ML297

Description

• A blood-brain barrier-permeable, non-toxic phenyl-pyrazolylurea compound that acts as a direct, potent, fast, and reversible activator of GIRK1 (G-protein activated inward-rectifying K + channel containing subunit 1) containing channels (EC 50 = 162, 914, and 887nM in Thallium influx assay for GIRK1/2, GIRK1/3, and GIRK1/4 expressed in HEK-293 cell lines)
• Its action does not require the presence of an activated G i GPCR
• Shown to be inactive towards GIRK2, GIRK2/3, K ir 2.1, K V 7.4 and GABA A , and weakly active against a panel of 61 other receptors, ion channels, enzymes, transporters, and proteins even at higher concentration (∽10μM)
• Exhibits desirable pharmacokinetic properties with good solubility (17.5μM), predicted hepatic clearance (88 ml/min/kg), and T max of 640nM and 130nM in plasma and brain, respectively
• Shown to reduce locomotor function and seizure frequency in electroshock- and chemically-induced murine epilepsy models (60mg/kg, i.p).