Elastase Inhibitor

CHF-6333 xinafoate is a neutrophil elastase (NE) inhibitor (IC₅₀ = 0.21 nM; K_D = 0.16 nM). CHF6333 xinafoate retains its activity in both human (IC₅₀ = 0.22 nM) and rat (IC₅₀ = 3.63 nM) proteases. CHF6333 xinafoate exhibits inhibitory activity against Proteinase 3 (IC₅₀ = 22 nM). CHF-6333 xinafoate can be used for the study of bronchiectasis (BE).

XDS-23 is a selective biofilm inhibitor with an IC₅₀ of 1.26 µM against Pseudomonas aeruginosa. XDS-23 exerts a dual inhibitory effect on the LasI/LasR System (las) and Pseudomonas Quinolone Signal System (pqs). XDS-23 suppress the production of key virulence factors including elastase, pyocyanin, and extracellular polysaccharides. XDS-23 exhibits synergistic antibacterial activity and can enhance the efficacy of multiple antibiotics in both in vitro and in vivo models, while maintaining a favorable safety profile. XDS-23 can be employed for research in combating biofilm-mediated drug-resistant P. aeruginosa infections.

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.

Endosidin1 (Prieurianin) is a Prieurianin with cleaved A and B rings. Endosidin1 is isolated from the roots of Aphanamixis polystachya. Endosidin1 inhibits superoxide anion production and Elastase release in neutrophils, with an IC₅₀ >10 μg/mL. Endosidin1 exhibits mild cytotoxic activity against laryngeal cancer cells in vitro. Endosidin1 shows anti-inflammatory activity. Endosidin1 can be used in studies related to laryngeal cancer.\n

MeO-Suc-Ala-Ala-Pro-Ala-CMK (MSACK) is an inhibitor of human neutrophil elastase (HNE), with an IC₅₀ of 20.3 μM. MeO-Suc-Ala-Ala-Pro-Ala-CMK can inhibit the hydrolysis of substrates such as elastin in lung tissue by HNE. MeO-Suc-Ala-Ala-Pro-Ala-CMK can be used in the research of related diseases such as chronic obstructive pulmonary disease (COPD).

ICI-200880 is a potent, selective and reversible human neutrophil elastase (HNE) inhibitor. ICI-200880 is promising for research of inflammatory lung diseases related to neutrophil elastase, such as chronic obstructive pulmonary disease (COPD) and cystic fibrosis (CF).

Eglin c (60-63) is a selective Elastase inhibitor, with a K_i value of 2.3e-3 M against human leukocyte hElastase and a K_i value of 4.8e-3 M against porcine pancreatic Elastase. Eglin c (60-63) can be used in research related to rheumatoid arthritis.

Pyracrenic acid is an elastase inhibitor (IC₅₀ = 2.42 µM), can be obtained from the bark of Pyracantha crenulata. Pyracrenic acid has DPPH free radical scavenging activity and anti-inflammatory activity.

Tyrosinase/elastase-IN-1 a triterpenoid from Rubus fraxinifolius leaves, has tyrosinase and elastase inhibitory activities.

Phochinenin K is a 9,10-dihydrophenanthrene derivative present in the rhizomes of Bletilla formosana. Phochinenin K exhibits anti-inflammatory activity and can be used in the study of inflammatory diseases.

MeOSuc-AAPA-CMK is a potent inhibitor of human neutrophil elastase.

Neutrophil elastase inhibitor 4 is a human neutrophil elastase (HNE) inhibitor with an IC₅₀ of 21.78 nM and a K_i of 8.04 nM. Neutrophil elastase inhibitor 4 induces G₂/M cell cycle arrest and apoptosis. Neutrophil elastase inhibitor 4 is applicable to research related to breast cancer, multiple myeloma and non-small cell lung cancer.

KRP-109 is a neutrophil elastase (NE) inhibitor with activity in reducing lung inflammation. KRP-109 improves survival in mouse models and reduces the number of neutrophils and inflammation in the alveolar walls. KRP-109 significantly reduced cell and neutrophil counts in bronchoalveolar lavage fluid, as well as cytokine levels such as interleukin 1β and macrophage inflammatory protein 2. KRP-109 can be used in the research of severe pneumonia.

(S)-MDL-101146 is the S-isomer of MDL-101146. MDL-101146 is an orally active, competitive and reversible inhibitor against human neutrophil elastase (HNE) with a K_i value of 25 nM. MDL-101146 inhibits HNE-induced hemorrhage in hamsters. MDL-101146 is promising for research of emphysema, rheumatoid arthritis, chronic bronchitis, cystic fibrosis, adult respiratory distress syndrome and glomerulonephritis.

CE-1037 (MDL 201,404YA) is a selective inhibitor of human neutrophil elastase (HNE) (K_i: 0.45 nM). CE-1037 prevents the pulmonary hemorrhage induced by intratracheal instillation of HNE. CE-1037 can be used for research of pulmonary diseases, such as COPD.

DPP-1-IN-1 (Compound 14) is an orally active inhibitor of Cathepsin C (also known as Dipeptidyl peptidase I) with an IC₅₀ of 5.31 nM. DPP-1-IN-1 can inhibit the activity of Cathepsin C downstream Neutrophil elastase in neutrophils. DPP-1-IN-1 can be used in the research of inflammatory diseases.

Roseltide rT1 is a neutrophil elastase inhibitor (IC₅₀=0.47 μM) rich in cysteine and one of the Roseltide (rT1-rT8) family members. Roseltide rT1 improves cAMP accumulation stimulated by neutrophil elastase in vitro, showing potential for inhibiting related diseases.

Chrysophanol 8-O-glucoside (Standard) is the analytical standard of Chrysophanol 8-O-glucoside. This product is intended for research and analytical applications. Chrysophanol 8-O-glucoside, from the roots of Rumex acetosa, shows moderate elastase inhibition activity.

Elasnin is a selective granulocyte elastase inhibitor. Elasnin is almost ineffective for pancreatic elastase, trypsin, chymotrypsin, thermolysin and papain.

Neutrophil elastase-IN-7 is a human neutrophil elastase inhibitor with an IC₅₀ of 0.54 μM. Neutrophil elastase-IN-7 also exhibits significant inhibitory activity against multiple coagulation proteins, with IC₅₀ values of 8.2, 12.7, 1.2 and 5.7 μM against thrombin, FXa, FXIa and FXIIIa, respectively. Neutrophil elastase-IN-7 can be used in the research of cardiopulmonary diseases and inflammatory diseases.