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906547-89-5
2024/12/16 14:04:23
Lonodelestat (POL6014) 是有效的、具有口服活性的、选择性的人中性粒细胞弹性蛋白酶(hNE)的肽类抑制剂。序列中含有13个氨基酸,其中包含一个非天然氨基酸。多肽具备较强的疏水性,带有立体环状结构。Lonodelestat (POL6014) 具有囊性纤维化 (CF) 研究的潜力 。
Lonodelestat (POL6014) significantly and efficiently reduced the inflammatory processes of ALI in HNE treated mice[1].
Lonodelestat (POL6014, 0.1, 0.5, 2 and 10 mg/kg, intranasally administered) dose-dependently and significantly reduces the number of macrophages, epithelial cells, neutrophils and lymphocytes recovered in BAL. The maximum inhibition was reached at 2 mg/kg in reducing neutrophils by 65% (p<0.001), epithelial cells by 68% (p<0.001), macrophages by 33% (p<0.001) and lymphocytes by 77% (p<0.001)[1].
分子量:1478.73
分子式:C71H111N15O19
CAS 号:906547-89-5
序列:cyclo[ASIPPQKYPPNle(bu)ET]
外观与性状:粉末状固体
消光系数: -
来源: 人工化学合成,仅限科学研究使用,不得用于人体。
储存条件:负80℃至负20℃
参考文献:
Single dose escalation studies with inhaled POL6014, a potent novel selective reversible inhibitor of human neutrophil elastase, in healthy volunteers and subjects with cystic fibrosis【DOI: 10.1016/j.jcf.2019.08.020】
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