AE-3763

AE-3763 is a peptide-based human neutrophil elastase inhibitor with an IC50 of 29 nM.

Signaling Pathways >> Metabolic Enzyme/Protease >> Elastase

Research Areas >> Cardiovascular Disease

Research Areas >> Inflammation/Immunology

IC50: 29 nM (Human neutrophil elastase)[1]

AE-3763 exhibits potent in vitro inhibitory activity against human neutrophil elastase as well as extremely high solubility and stability in water[1].

Edema and leukocytes infiltration into the lung are significantly inhibited by 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 in mice, the results of a preliminary study have shown no overt toxic effect even at the high dose of 300 mg/kg, iv[1].

Mice[1] 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. Animal’s survival rate is observed up to 24 h after shock induction[1].

[1]. Inoue Y, et al. Development of a highly water-soluble peptide-based human neutrophil elastase inhibitor; AE-3763 for treatment of acute organ injury. Bioorg Med Chem. 2009 Nov 1;17(21):7477-86.

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