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 bioavailable, affinity and selective inhibitor of neutrophil elastase (NE) with a pIC₅₀ value of 7.9 nM, a K_i value of 9.4 nM and a K_d value of 9.5 nM.

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.

CHF-6333 chloride is a neutrophil elastase (NE) inhibitor (IC₅₀ = 0.21 nM; K_D = 0.16 nM). CHF-6333 chloride retains its activity in both human (IC₅₀ = 0.22 nM) and rat (IC₅₀ = 3.63 nM) proteases. CHF-6333 chloride exhibits inhibitory activity against Proteinase 3 (IC₅₀ = 22 nM). CHF-6333 chloride can be used for the study of bronchiectasis (BE).

Antibiofilm agent-22 is an FpvA receptor-targeting antibacterial agent. Antibiofilm agent-22 chelates iron, disrupts las, pqs, and rhl pathways, reduces elastase, pyocyanin, and rhamnolipid production, and induces bacterial iron starvation. Antibiofilm agent-22 can be used for the research of Pseudomonas aeruginosa infection.

PV-DPD-19 is an autoinducer-2 (AI-2) quorum sensing inhibitor. PV-DPD-19 reduces AI-2 production and inhibits the expression of multiple MSCRAMMs. In co-culture systems with Staphylococcus aureus, PV-DPD-19 decreases the production of pyocyanin and Elastase in Pseudomonas aeruginosa. PV-DPD-19 impairs the adhesion ability of Staphylococcus aureus to lung epithelial cells. PV-DPD-19 inhibits biofilm formation of Pseudomonas aeruginosa (MBIC₅₀ = 27 μg/mL) and Staphylococcus aureus (MBIC₅₀ = 35 μg/mL). PV-DPD-19 shows no cytotoxicity in both in vitro lung epithelial cell models and in vivo Galleria mellonella larva models.

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).

Elastase-IN-3 (Compound 2i) is an Elastase inhibitor of Pseudomonas aeruginosa. Elastase-IN-3 inhibits the quorum sensing system of Pseudomonas aeruginosa by targeting the LasR protein (K_D value of 7.04 M), thereby preventing food spoilage caused by Pseudomonas aeruginosa.

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.