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PF-03716556 is a potent, and selective acid pump antagonist for the treatment of gastroesophageal reflux disease. PF-03716556 demonstrated 3-fold greater inhibitory activity than revaprazan. PF-03716556 did not display any species differences, exhibiting highly selective profile including the canine kidney Na(+),K(+)-ATPase. Kinetics experiments revealed that PF-03716556 has a competitive and reversible mode of action.