AE-3763 is a peptide-based human neutrophil elastase inhibitor with an IC 50 of 29 nM.
性状
Solid
IC50 & Target[1][2]
IC50: 29 nM (Human neutrophil elastase)
体外研究(In Vitro)
AE-3763 exhibits potent in vitro inhibitory activity against human neutrophil elastase as well as extremely high solubility and stability in water. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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 (ED 50 : 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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 16.67 mg/mL (30.33 mM; Need ultrasonic)配制储备液