Lonodelestat(Synonyms: POL6014)

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Lonodelestat;(Synonyms: POL6014)

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。

Lonodelestatamp;;(Synonyms: POL6014)

Lonodelestat Chemical Structure

CAS No. : 906547-89-5

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生物活性

Lonodelestat (POL6014) is a potent, orally active and selective peptide inhibitor of human neutrophil elastase (hNE)[1][2].

体内研究
(In Vivo)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Ten-week-old male C57BL/6j mice[1].
Dosage: 0.05, 0.2, 0.5 and 5 mg/kg.
Administration: Administered intranasally (i.n.) 15 minutes before HNE (30 UI, i.n.).
Result: Reduced the inflammatory processes of ALI in HNE treated mice.

分子量

1478.73

Formula

C71H111N15O19
CAS 号

906547-89-5
Sequence Shortening

cyclo[ASIPPQKYPPNle(bu)ET]
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Lagente V, et al. A novel Protein Epitope Mimetic (PEM) neutrophil elastase (NE) inhibitor, POL6014, inhibits human NE-induced acute lung injury in mice. ATS, San Diego, May 15-20, 2009.

    [2]. Odile Sellier-Kessler, et al. Inhibition of lung inflammation by a protein epitope mimetic (PEM) neutrophil elastase inhibitor, POL6014, in a sub-chronic tobacco smoke (TS) model in mice. European Respiratory Journal 2013 42: 1762.