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291778-77-3

中文名称 291778-77-3
英文名称 AE-3763
CAS 291778-77-3
分子式 C23H34F3N5O7
分子量 549.54
MOL 文件 291778-77-3.mol
更新日期 2023/03/20 15:41:17
291778-77-3 结构式 291778-77-3 结构式

基本信息

中文别名
化合物 T10254
英文别名
AE-3763
1-Imidazolidineacetic acid, 3-[2-[[(1S)-2-methyl-1-[[(2S)-2-[[[(1S)-3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]carbonyl]-1-pyrrolidinyl]carbonyl]propyl]amino]-2-oxoethyl]-2-oxo-

物理化学性质

储存条件-20°C储存
溶解度溶于二甲基亚砜
形态Solid
颜色White to off-white

常见问题列表

生物活性
AE-3763 是基于多肽的人中性粒细胞弹性蛋白酶 (human neutrophil elastase) 抑制剂,IC50 值为29 nM。
靶点

IC50: 29 nM (Human neutrophil elastase)

体外研究

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

体内研究

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.

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