Elastase Inhibitor

Sivelestat (EI546) is a competitive inhibitor of human neutrophil elastase, with an IC₅₀ of 44 nM and a K_i 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.

Alvelestat (AZD9668) is an orally active, selective inhibitor of neutrophil elastase. Alvelestat 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 restores endothelial dysfunction, regulates antioxidant factors, improves the expression of endothelial tight junctions, reduces vascular leakage, and accelerates wound healing. Alvelestat prevents pulmonary hemorrhage, matrix protein degradation, airspace enlargement, and small airway wall remodeling; and alleviates cigarette-induced inflammatory responses. Alvelestat inhibits the growth of abdominal aortic aneurysms exacerbated by Porphyromonas gingivalis. Alvelestat can be used in research related to chronic obstructive pulmonary disease, abdominal aortic aneurysm, radiation-induced skin injury, and bronchiectasis.

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

GW-311616 is a potent, orally bioavailable, long duration and selective human neutrophil elastase (HNE) inhibitor with IC₅₀ value of 22 nM and K_i value of 0.31 nM.

(6-Rac)-Kirenol is an ent-pimarane-type diterpenoid. (6-Rac)-Kirenol inhibits the production of superoxide anions in activated human neutrophils. (6-Rac)-Kirenol inhibits the release of elastase from activated human neutrophils.

DMP 777 is a potent, selective, and orally active human leukocyte elastase (HLE) inhibitor.

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.

MeOSuc-AAPV-CMK (Elastase Inhibitor III) is an elastase inhibitor that simultaneously inhibits Cathepsin G and Proteinase 3. MeOSuc-AAPV-CMK blocks the shedding of FcgRIIIb on the surface of human neutrophils. MeOSuc-AAPV-CMK reverses the elastase-mediated reduction in proinflammatory cytokine production by immune cells, partially restores IL-1β levels in immune cell co-culture systems, and prevents elastase-mediated adiponectin cleavage.

BAY-85-8501 is a selective, reversible and potent inhibitor of Human Neutrophil Elastase (HNE), with an IC₅₀ of 65 pM.

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).

LasR antagonist-2 is a LasR competitive antagonist and quorum sensing inhibitor, with a K_d value of 7.04 μM against LasR of Pseudomonas aeruginosa. LasR antagonist-2 reduces the production of virulence factors including elastase (elastase), pyocyanin (pyocyanin) and rhamnolipid (rhamnolipid). LasR antagonist-2 inhibits bacterial (bacterial) swarming and swimming motility, and moderately suppresses biofilm formation. LasR antagonist-2 inhibits Pseudomonas aeruginosa infection in the greater wax moth larva model. Elastase-IN-3 can be used in studies related to Pseudomonas aeruginosa infection.

Lonodelestat TFA (POL6014 TFA) is a potent, orally active and selective peptide inhibitor of human neutrophil elastase (hNE). Lonodelestat TFA has the potential for the research of cystic fibrosis (CF).

FK706 is a potent, slow-binding and competitive inhibitor of human neutrophil elastase with an IC₅₀ of 83 nM and a K_i of 4.2 nM. FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase with IC₅₀s of 22 nM and 100 nM, respectively, and has no inhibitory activity against other serine proteinases such as human pancreatic trypsin, human pancreatic α-chymotrypsin and human leukocyte cathepsin G. FK706 has anti-inflammatory effect.

SSR69071 is a potent, orally active and selective inhibitor of neutrophil elastase. SSR69071 reduces myocardial infarct size following ischemia-reperfusion injury. SSR69071 displays a higher affinity for human elastase (K_i=0.0168 nM) than for rat (K_i=3 nM), mouse (K_i=1.8 nM), and rabbit (K_i= 58 nM) elastases.

Neutrophil elastase inhibitor 5 is an inhibitor of human neutrophil elastase (HNE), proteinase 3 (PR3) and sirt2, with IC₅₀ values of 4.91, 20.69 and 2.42 μM, respectively. Neutrophil elastase inhibitor 5 inhibits superoxide anion production and elastase release in human neutrophils. Neutrophil elastase inhibitor 5 can be used for the research of neutrophil inflammatory diseases.

Chrysophanol 8-O-glucoside, from the roots of Rumex acetosa, shows moderate elastase inhibition activity.

ZD-0892 is a selective and potent inhibitor of a neutrophil elastase with K_is of 6.7 and 200 nM for human neutrophil elastase and porcine pancreatic elastase, respectively.

GW-311616 is a potent, orally bioavailable, long duration and selective human neutrophil elastase (HNE) inhibitor with IC₅₀ value of 22 nM and K_i value of 0.31 nM.

Freselestat (ONO-6818) is a potent and orally active neutrophil elastase inhibitor with a K_i of 12.2 nM. Freselestat is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat has a potent anti-inflammatory activity.

AE-3763 is a peptide-based human neutrophil elastase inhibitor with an IC₅₀ of 29 nM.