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Description

A cell-permeable glycinyl hydrazone compound that acts as a potent, selective and reversible open-channel blocker of CFTR with intermediate speed (<1 min, 95% inhibition at 50 µ,M, Ki = 4.3 µ,M in CFTR-expressing FRT cells for apical membrane Cl- current) and exhibits desirable aqueous solubility. Shown to produce inwardly rectifying CFTR Cl- currents with reduced mean channel open time and suggested to directly interact with the channel pore at the extracellular side of the membrane. Displays minimal effects on P-glycoprotein and non-CFTR-mediated Cl- currents, and is effective in nasal and intestinal epithelia in vivo.