Catalog Number: 5651
Chemical Name: 5-Amino-N-[1-[[5-(1,1-dimethylethyl)-1,3,4-oxadiazol-2-yl]carbonyl]-2-methylpropyl]-6-oxo-2-phenyl-1(6H)-pyrimidineacetamide
Biological Activity
High affinity and selective human neutrophil elastase 1 (HNE1) inhibitor (Ki = 12 nM). Exhibits >100-fold less activity at other related proteases including trypsin, pancreatic elastase, collagenase and murine macrophage elastase. Inhibits HNE-induced lung hemorrhaging and suppresses leukocyte levels in an in vivo model of COPD. Orally active.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
  • Storage:
    Store at -20°C
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. AZD9668: pharmacological characterization of a novel oral inhibitor of neutrophil elastase.
    Stevens et al.
    J.Pharmacol.Exp.Ther., 2011;339:313
  2. Effects of the neutrophil elastase inhibitor (ONO-6818) on acetic acid induced colitis in Syrian hamsters.
    Hirota et al.
    J.Vet.Med.Sci., 2004;66:1223
  3. Serine proteases increase oxidative stress in lung cells.
    Aoshiba et al.
    Am.J.Physiol.Lung Cell Mol.Physiol., 2001;281:556
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