AE-3763 is a peptide-based human neutrophil elastase inhibitor (IC50: 29 nM).

Neutrophil elastase (human):29 nM

AE-3763 has potent inhibitory activity against human neutrophil elastase as well as extremely high solubility and stability in water.

Edema and leukocytes infiltration into the lung is significantly inhibited by the infusion of AE-3763. AE3763 significantly improves survival rate by 24 h in a mouse model of fatal shock associated with multiple organ dysfunction. AE-3763 dose-dependently prevents hemorrhage when given intravenously by infusion (ED50: 0.42 mg/kg/h) or by bolus injection (1.2 mg/kg). With regard to the toxicity of AE-3763 (300 mg/kg, i.v.) in mice, the results of a preliminary study have shown no overt toxic effect.

D-Galactosamine shock is induced in C3H/HeN mice (6-7 w, 22-25 g). AE-3763 (10 or 100 mg/kg) is administrated intraperitoneally six times at 2 h interval. Control animals receive the vehicle (PBS) instead of AE-3763. The animal survival rate is observed up to 24 h after shock induction.