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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.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 452.51. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.21 mL||11.05 mL||22.1 mL|
|5 mM||0.44 mL||2.21 mL||4.42 mL|
|10 mM||0.22 mL||1.1 mL||2.21 mL|
|50 mM||0.04 mL||0.22 mL||0.44 mL|
References are publications that support the biological activity of the product.
Hirota et al (2004) Effects of the neutrophil elastase inhibitor (ONO-6818) on acetic acid induced colitis in Syrian hamsters. J.Vet.Med.Sci. 66 1223 PMID: 15528853
Aoshiba et al (2001) Serine proteases increase oxidative stress in lung cells. Am.J.Physiol.Lung Cell Mol.Physiol. 281 556 PMID: 11504681
Stevens et al (2011) AZD9668: pharmacological characterization of a novel oral inhibitor of neutrophil elastase. J.Pharmacol.Exp.Ther. 339 313 PMID: 21791628
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