MLN-4760

MLN-4760 is a potent and selective human ACE2 inhibitor (IC₅₀, 0.44 nM), with excellent selectivity (>5000-fold) versus related enzymes including human testicular ACE (IC₅₀, >100 μM) and bovine carboxypeptidase A (CPDA; IC₅₀, 27 μM). IC50 & Target: IC50: 0.44 nM (Human ACE2), 27 μM (Bovine carboxypeptidase A)^[1] In Vitro: MLN-4760 is a potent and selective human ACE2 inhibitor (IC₅₀, 0.44 nM), with excellent selectivity (>5000-fold) versus related enzymes human testicular ACE (IC₅₀, >100 μM) and bovine carboxypeptidase A (CPDA; IC₅₀, 27 μM)^[1]. MLN-4760 effectively quenches cleavage of the 7-Mca-YVADAPK(Dnp) in rhACE2. MLN-4760 shows pIC₅₀ at rhACE2 of 8.5±0.1 and at rhACE of 4.4±0.2. MLN-4760 also shows pIC₅₀ at rhACE2 of 4.7±0.1, 6.9±0.1 and at ACE of 4.4±0.1, 6.2±0.1 in murine heart and mononuclear cells (MNCs), resepctively^[2]. In Vivo: MLN-4760 (100 μM, intracerebroventricular infusion for five days) significantly worsens neurological function at 4 h and 3 d post-stroke without significantly increasing infarct volume^[3].