ONO 6818

Pricing Availability Delivery Time Qty
Cat.No. 5651 - ONO 6818 | C23H28N6O4 | CAS No. 208848-19-5
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)
Datasheet
Citations
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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

Safety Datasheet

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


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Keywords: ONO6818 High affinity selective human neutraphil elastases 1 HNE1 inhibitors inhibits COPD chronic obstructive pulmonary disease colitis orally active Elastase

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