MLN-4760 (MLN4760) is a potent, selective inhibitor of angiotensin-converting enzyme (ACE)-related carboxypeptidase ACE2 with IC50 of 0.44 nM (hACE2).
MLN-4760 displays >5,000-fold selectivity over related enzymes including human testicular ACE (IC50>100 uM) and bovine carboxypeptidase A (IC50=27 uM).
MLN-4760 exacerbated the Ang II-dependent formation of ROS and abolished the generation of Ang-(1-7) from Ang II.
MLN-4760 exacerbates cardiac hypertrophy and fibrosis in Ren-2 hypertensive rats.
