MLN-4760 is an effective and selective inhibitor of human ACE2 (IC50, 0.44 nM). It also has excellent selectivity (>5000-fold) versus related enzymes including human testicular ACE (IC50>100 μM) and bovine carboxypeptidase A (CPDA; IC50, 27 μM). MLN-4760 also enables to study the effect of reduced ACE2 activity on the lung’s susceptibility for Coronavirus disease (COVID) related acute respiratory distress syndrome (ARDS).