AE-3763
AE-3763是基于多肽的人中性粒细胞弹性蛋白酶(humanneutrophilelastase)抑制剂，IC50值为29nM。
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包装价格促销价数量
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250mg￥0.000.00- +
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500mg￥0.000.00- +
- 货号: ajcx12730
- CAS: 291778-77-3
- 别名:
- 分子式: C23H34F3N5O7
- 分子量: 549.54
- 纯度: ＞98%
- 溶解度: Soluble in DMSO
- 储存: Store at -20°C
- 库存: 现货
Background
AE-3763 is a peptide-based human neutrophil elastase inhibitor with an IC50 of 29 nM.
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].
[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.
Protocol
Animal experiment: | 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]. |
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. | |
