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Submit ReviewONO 6818
Description: High affinity and selective human neutrophil elastase 1 (HNE1) inhibitor; orally active
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
Purity: ≥98% (HPLC)
Biological Activity for ONO 6818
ONO 6818 is a 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.
Compound Libraries for ONO 6818
ONO 6818 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for ONO 6818
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for ONO 6818
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 45.25 | 100 |
Preparing Stock Solutions for ONO 6818
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 |
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Product Datasheets for ONO 6818
References for ONO 6818
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
If you know of a relevant reference for ONO 6818, please let us know.
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Citations for ONO 6818
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