MLN-4760 是选择性的人ACE2抑制剂，IC50=0.44 nM，对人ACE2的选择性是其他相关蛋白的 5000 多倍，包括人睾丸 ACE (IC50，>100 μM) 和牛 Carboxypeptidase A (IC50，27 μM)。

MLN-4760 is an angiotensin-converting (ACE2) inhibitor(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 displays 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 an ACE of 4.4±0.1, 6.2±0.1 in murine heart and mononuclear cells (MNCs), respectively. MLN-4760 potently quenches the cleavage of the 7-Mca-YVADAPK(Dnp) in rhACE2[2].

MLN-4760 (100 μM, intracerebroventricular infusion for five days) obviously worsens neurological function at 4 h and 3 d post-stroke. However, without obviously increasing infarct volume[3].

305335-31-3

C19H23Cl2N3O4

428.31

DMSO:199 mg/mL(464.62 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years