906547-89-5

906547-89-5 structure

Name: Lonodelestat
Chemical Name: 3-[(6S,9S,12S,15S,18S,21S,23aS,28aR,34S,37S,40S,42aS,47aS)-37-(4-Aminobutyl)-40-(3-amino-3-oxopropyl)-6-[(2S)-2-butanyl]-34-(4-hydroxybenzyl)-15-[(1R)-1-hydroxyethyl]-9-(hydroxymethyl)-12-methyl-21-octyl-5,8,11,14,17,20,23,28,33,36,39,42,47-tridecaoxotetratetracontahydro-1H,5H,28H-tetrapyrrolo[1,2-a:1',2'-d:1'',2''-p:1''',2'''-s][1,4,7,10,13,16,19,22,25,28,31,34,37]tridecaazacyclononatriacontin-18-yl]propanoic acid
CAS Number: 906547-89-5
Molecular Formula: C₇₁H₁₁₁N₁₅O₁₉
Molecular Weight: 1478.73
Catalog: Signaling Pathways Metabolic Enzyme/Protease Elastase
Create Date: 2021-12-20 13:57:34
Modify Date: 2024-04-07 17:33:38
Lonodelestat (POL6014) is a potent, orally active and selective peptide inhibitor of human neutrophil elastase (hNE)[1][2].

Name	3-[(6S,9S,12S,15S,18S,21S,23aS,28aR,34S,37S,40S,42aS,47aS)-37-(4-Aminobutyl)-40-(3-amino-3-oxopropyl)-6-[(2S)-2-butanyl]-34-(4-hydroxybenzyl)-15-[(1R)-1-hydroxyethyl]-9-(hydroxymethyl)-12-methyl-21-octyl-5,8,11,14,17,20,23,28,33,36,39,42,47-tridecaoxotetratetracontahydro-1H,5H,28H-tetrapyrrolo[1,2-a:1',2'-d:1'',2''-p:1''',2'''-s][1,4,7,10,13,16,19,22,25,28,31,34,37]tridecaazacyclononatriacontin-18-yl]propanoic acid
Synonyms	1H,5H,28H-Tetrapyrrolo[1,2-a:1',2'-d:1'',2''-p:1''',2'''-s][1,4,7,10,13,16,19,22,25,28,31,34,37]tridecaazacyclononatriacontine-18-propanoic acid, 37-(4-aminobutyl)-40-(3-amino-3-oxopropyl)tetratetracontahydro-15-[(1R)-1-hydroxyethyl]-9-(hydroxymethyl)-34-[(4-hydroxyphenyl)methyl]-12-methyl-6-[(1S)-1-methylpropyl]-21-octyl-5,8,11,14,17,20,23,28,33,36,39,42,47-tridecaoxo-, (6S,9S,12S,15S,18S,21S,23aS,28aR,34S,37S,40S,42aS,47aS)- 3-[(6S,9S,12S,15S,18S,21S,23aS,28aR,34S,37S,40S,42aS,47aS)-37-(4-Aminobutyl)-40-(3-amino-3-oxopropyl)-6-[(2S)-2-butanyl]-34-(4-hydroxybenzyl)-15-[(1R)-1-hydroxyethyl]-9-(hydroxymethyl)-12-methyl-21-octyl-5,8,11,14,17,20,23,28,33,36,39,42,47-tridecaoxotetratetracontahydro-1H,5H,28H-tetrapyrrolo[1,2-a:1',2'-d:1'',2''-p:1''',2'''-s][1,4,7,10,13,16,19,22,25,28,31,34,37]tridecaazacyclononatriacontin-18-yl]propanoic acid

Description	Lonodelestat (POL6014) is a potent, orally active and selective peptide inhibitor of human neutrophil elastase (hNE)[1][2].
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Elastase Research Areas >> Inflammation/Immunology
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]. 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.
References	[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.