V-161 is a potent, specific E. hirae Na+-transporting V-ATPase (EhV-ATPase) inhibitor with IC50 of 144 nM, blocks the function of Na+-transporting V-ATPase and preferentially inhibits the growth of enterococci.
V-161 binds to the interface of the c-ring and a-subunit, constituting the Na+ transport pathway in the membrane, thereby halting its rotation.
V-161 significantly suppresses VRE colonization in the small intestine of mice, having no effect on bacteria lacking this enzyme or on human cells.
V-161 inhibits vancomycin-resistant Enterococcus faecium (VRE).
V-161 inhibits the growth of E. hirae under alkaline conditions (>pH 7.5) with MIC of 4 ug/mL for both E. hirae and VRE (pH 8.5), but not under neutral or acidic conditions (V-161 selectively blocks bacterial V-ATPase function, but not human kidney cells.
V-161 significantly suppresses VRE colonization in the mouse small intestine.