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 | 452.51 |
| Formula | C23H28N6O4 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 208848-19-5 |
| PubChem ID | 216294 |
| InChI Key | YSIHYROEMJSOAS-UHFFFAOYSA-N |
| Smiles | O=C(NC(C(C)C)C(C1=NN=C(C(C)(C)C)O1)=O)CN(C(C2=CC=CC=C2)=NC=C3N)C3=O |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 45.25 | 100 |
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 solvent 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 |
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References
References are publications that support the products' biological activity.
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
Keywords: ONO 6818, supplier, ONO6818, High, affinity, selective, human, neutraphil, elastases, 1, HNE1, inhibitors, inhibits, COPD, chronic, obstructive, pulmonary, disease, colitis, orally, active, Elastase, Elastase, Tocris Bioscience
