CAS NO: | 1448314-31-5 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 261.3 |
Cas No. | 1448314-31-5 |
Formula | C16H11N3O |
Solubility | ≤0.5mg/ml in ethanol;10mg/ml in DMSO;30mg/ml in dimethyl formamide |
Chemical Name | 1-(3-methylbenzoyl)-1H-indazole-3-carbonitrile |
Canonical SMILES | O=C(C1=CC=CC(C)=C1)N2C3=CC=CC=C3C(C#N)=N2 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
IC50: 7 nM
Neutrophil Elastase Inhibitor is a neutrophil elastase inhibitor.
Human neutrophil elastase (HNE) is a member of the chymotrypsin superfamily of serine proteases that is involved in the response to inflammatory stimuli. HNE is reported to be stored in azurophilic granules of neutrophils and is greatly aggressive and cytotoxic, as its substrates include various components of the extracellular matrix.
In vitro: Previous study found that Neutrophil Elastase Inhibitor was able to inhibit thrombin and urokinase at micromolar concentrations. In addition, Neutrophil Elastase Inhibitor appeared to be a specific HNE inhibitors in a competitive manner. Moreoer, the hydrolysis of the acyl-enzyme complex for Neutrophil Elastase Inhibitor was found to be much slower than spontaneous hydrolysis of Neutrophil Elastase Inhibitor, and HNE was observed to be still inhibited to 80% of control level at 7 h after treatment [1].
In vivo: So far, there is no animal in vivo data reported.
Clinical trial: Up to now, Neutrophil Elastase Inhibitor is still in the preclinical development stage.
References:
[1] L. Crocetti, I. A. Schepetkin, A. Cilibrizzi, et al. Optimization of N-benzoylindazole derivatives as inhibitors of human neutrophil elastase. Journal of Medicinal Chemistry 56(15), 6259-6272 (2013).