Background:

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.

参考文献:
[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).