Elastase Inhibitor

Alvelestat hydrochloride (AZD9668 hydrochloride) is an orally active, selective inhibitor of neutrophil elastase. Alvelestat hydrochloride reduces elastase activity, myeloperoxidase release, neutrophil recruitment and activation, and calcium phosphate precipitation; promotes smooth muscle cell colonization and collagen deposition; and inhibits the formation of neutrophil extracellular traps (NETs) as well as NET-derived neutrophil elastase activity. Alvelestat hydrochloride restores endothelial dysfunction, regulates antioxidant factors, improves the expression of endothelial tight junctions, reduces vascular leakage, and accelerates wound healing. Alvelestat hydrochloride prevents pulmonary hemorrhage, matrix protein degradation, airspace enlargement, and small airway wall remodeling; and alleviates cigarette-induced inflammatory responses. Alvelestat hydrochloride inhibits the growth of abdominal aortic aneurysms exacerbated by Porphyromonas gingivalis. Alvelestat hydrochloride can be used in research related to chronic obstructive pulmonary disease, abdominal aortic aneurysm, radiation-induced skin injury, and bronchiectasis.

LasB-IN-1 (compound 5f) is a potent and orally active inhibitor of LasB (IC₅₀ = 8.7 μM). LasB-IN-1 effectively attenuates elastase production and biofilm formation by P. aeruginosa while alleviating the inflammatory response through downregulating MAPK and NF-κB pathways. LasB-IN-1 is potential to be a novel anti-infective candidate against drug-resistant infections.

BAY-678 (Standard) is the analytical standard of BAY-678 (HY-111457A). This product is intended for research and analytical applications. BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC₅₀ of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).

HLE-IN-1 (Compound 4) is a human leukocyte elastase HLE inhibitor (K_i=1.8 nM). HLE-IN-1 is used in emphysema and inflammamry pulmonary research.

Nostopeptin B is a cyclic dipeptide that can be isolated from N. minutum (NIES-26). The structure of Nostopeptin B contains Ahp (3-amino-6-hydroxy-2-piperidone), which exhibits effective inhibition against elastase and chymotrypsin.

L 708286 (DFKi) is a slow-binding inhibitor of human leukocyte elastase (HLE). L 708286 is a peptide-based phenethylcarbamoyl difluoromethylene compound. L 708286 can be used in the study of respiratory diseases.

LasB-IN-3 is a protease elastase (LasB) inhibitor of Pseudomonas aeruginosa with an IC₅₀ value of 8.5 nM. LasB-IN-3 shows an IC₅₀ of 58.9 nM for the Met128Val mutant. LasB-IN-3 binds to active sites of wild-type and Met128Val mutant LasB, coordinates zinc ions, forms hydrogen bonds and CH-π interactions, and inhibits LasB proteolytic activity. LasB-IN-3 increases survival rate in LasB-induced acute lung injury mice models. LasB-IN-3 can be used for the research of Pseudomonas aeruginosa infection.

Sivelestat (Standard) is the analytical standard of Sivelestat. This product is intended for research and analytical applications. Sivelestat (EI546) is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19.

Sivelestat (sodium tetrahydrate) (Standard) is the analytical standard of Sivelestat (sodium tetrahydrate). This product is intended for research and analytical applications. Sivelestat (EI546) sodium tetrahydrate is a competitive inhibitor of human neutrophil elastase, with an IC₅₀ of 44 nM and a K_i of 200 nM. Sivelestat (EI546) sodium tetrahydrate has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19.

L-684248 is an inhibitor of human leukocyte elastase (HLE). L-684248 exerts its inhibitory effect on HLE by forming a covalent bond with the active site of the enzyme, showing potential value for applications in anti-inflammatory and anti-tumor research.