MLN-4760 是一种有效、选择性的人 ACE2 抑制剂，IC50 值为 0.44 nM，对其选择性是对其他相关蛋白的 5000 多倍，包括人睾丸 ACE (IC50，>100 μM) 和牛 carboxypeptidase A (IC50，27 μM) ACE2 (Cell-free assay); CPDA (Cell-free assay) 0.44 nM; 27 μM In vitro conversion from angiotensin II to angiotensin-(1–7) by mouse ACE2 is blocked by MLN-4760 (10 μM). MLN-4760 inhibits both human and mouse ACE2 activity. In huMNCs, MLN-4760-B (an isomer of MLN-4760) detects 63% ACE2 with 28-fold selectivity over ACE. In huCD34+ cells, MLN-4760-B detects 38% of ACE2 activity with 63-fold selectivity. In mu-heart and muMNCs, MLN-4760-B is 100- and 228-fold selective for ACE2, respectively. In muLin- cells, MLN-4760-B detects 25% ACE2 activity with a pIC50 of 6.3. The racemic mixture and MLN-4760-A shows lower efficacy and poor selectivity for ACE2 in MNCs and mu-heart. In vivo MLN-4760 blocks ACE2 activity, thus significantly reverses the elevation of carotid Ang-(1-7) level and the decline of carotid Ang II level induced by NaHS in mice. The anti-atherosclerotic property of NaHS is also significantly abolished by treatment with MLN-4760. Cell Research(from reference) Cell lines：mononuclear cells (MNCs), huCD34+ cells, mu-lineage-depleted (muLin-) cells Concentrations：0.01 nM to 300 μM Incubation Time：1 h, 4 h