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AE-3763

Catalog No. T10254 CAS 291778-77-3

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

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AE-3763, CAS 291778-77-3

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Biological Description

Chemical Properties

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Description	AE-3763 is a peptide-based human neutrophil elastase inhibitor (IC50: 29 nM).
Targets&IC50	Neutrophil elastase (human):29 nM
In vitro	AE-3763 has potent inhibitory activity against human neutrophil elastase as well as extremely high solubility and stability in water.
In vivo	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.
Animal Research	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.

Molecular Weight	549.54
Formula	C23H34F3N5O7
CAS No.	291778-77-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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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Keywords

AE-3763 291778-77-3 Proteases/Proteasome Serine Protease AE 3763 AE3763 inhibitor inhibit

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