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Submit ReviewONO 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.
ONO 6818 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 452.51 |
公式 | C23H28N6O4 |
储存 | Store at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 45.25 | 100 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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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