Elastase Inhibitor

Aristololactam IIIa exhibits significant inhibitory effects on superoxide anion generation and elastase release with IC₅₀ values of 0.12 and 0.20 μg/mL, respectively.

MDL 101146 is an orally active neutrophil elastase inhibitor. MDL 101146 inhibits neutrophil elastase for human with a K_i value of 25 nM. MDL 101146 can be used for the research of arthritis.

ICI 186756 is a compound that inhibits the activity of human neutrophil elastase, has a competitive inhibitory effect on the enzyme, can inhibit enzyme-induced lung changes, and can also modulate hamster lung lesions.

BI-9740 is an orally active and selective cathepsin C (CatC) inhibitor, with an IC₅₀ of 0.6 nM in mice and 2.6 nM in rats. BI-9740 can inhibit the production of active neutrophil elastase. Additionally, BI-9740 is capable of reducing the activities of neutrophil elastase and cathepsin G in the bone marrow of rats, alleviating pathological damage to grafts after heart transplantation, shortening the reperfusion time, and improving left ventricular function. BI-9740 can be used in research related to organ transplantation.

Elastase-IN-1 (Compound Q11) is an elastase inhibitor with an IC₅₀ of 0.897 µM. Elastase-IN-1 is non-toxic.

SP-Chymostatin B (α-MAPI) is a strong inhibitor of many proteases, including chymotrypsin, papain, chymotrypsin-like serine proteinases, chymases, and lysosomal cysteine proteinases such as cathepsins A,B,C, H, and L. SP-Chymostatin B weakly inhibits human leucocyte elastase.

Neutrophil elastase inhibitor 6 is a dual inhibitor of human neutrophil elastase (HNE) and proteinase 3 (PR3), with high selectivity for cathepsin G. Neutrophil elastase inhibitor 6 can be used in the research of chronic neutrophilic inflammatory diseases.

JCP174 is an inhibitor of palmitoyl protein thioesterase-1 (TgPPT1), a depalmitoylase in the parasite T. gondii. JCP174 is also an inhibitor of porcine pancreatic elastase and human leukocyte elastase.

(R)-MDL-101146 is the R-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.

Cyclotheonellazole A is a natural macrocyclic peptide and a potent elastase inhibitor (IC₅₀=0.034 nM). Cyclotheonellazole A inhibits chymotrypsin with an IC₅₀ value of 0.62 nM.

AZD-9819 is a neutrophil elastase (HNE) inhibitor. AZD-9819 can be used to study chronic obstructive pulmonary disease.

(1'S,2'S)-1'-O-Methylvaginol, a coumarin found in the fruits of Cnidium monnieri, is an elastase inhibitor. (1'S,2'S)-1'-O-Methylvaginol exhibits 11.99% inhibition of superoxide anion generation and 6.42% inhibition of elastase release by human neutrophils at 10 µg/mL. (1'S,2'S)-1'-O-Methylvaginol can be used for research on inflammatory diseases.

Scyptolin B, a cyclic depsipeptides, is a secondary metabolite. Scyptolin B can be isolated from axenic cultures of Scytonema hofmanni PCC 7110. Scyptolin B selective inhibits porcine pancreatic Elastase with an IC₅₀ of 3.1 μg/mL.

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

L 659286 is an inhibitor of human polymorphonuclear leukocyte elastase (PMN elastase) (Ki=0.4 μM). Intratracheal injection of L 659286 can induce lung injury in hamsters.

Secologanoside (Standard) is the analytical standard of Secologanoside. This product is intended for research and analytical applications. Secologanoside is a triterpenoid isolated from Poraqueiba sericea, weakly inhibits elastase with an IC₅₀ of 164 μg/mL. Secologanoside is moderate cytotoxic to fibroblasts.

Alvelestat (Standard) (AZD9668 (Standard)) is the analytical standard of Alvelestat (HY-15651). This product is intended for research and analytical applications. 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.

Rhusflavanone is a biflavonoid found in the stamens of Mesua ferrea. Rhusflavanone IC₅₀ values against elastase and tyrosinase are 10.6 and 14.3 μg/mL, respectively. Rhusflavanone inhibits the replication of influenza B virus, SARS-CoV-2, Measles virus and HSV-2, and suppresses the secretion of Salmonella T3SS effector proteins. Rhusflavanone inhibits the production of pro-inflammatory mediators and exerts cytotoxic effects on cancer cells. Rhusflavanone can be used in research related to colon cancer, breast cancer, cervical cancer, COVID-19, influenza B, measles, HSV-2 infection and Salmonella infection.

Alvelestat-¹³C,d₃ (AZD9668-¹³C,d₃) is the deuterated, ¹³C-labeled Alvelestat (HY-15651). 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.

BAY-8040 is a pyrimidopyridazine derivative which has inhibitory activity against human neutrophil elastase (HNE). BAY-8040 decreases cardiac remodeling and ameliorates cardiac function in a Monocrotaline (HY-N0750)-induced rat model for pulmonary arterial hypertension. BAY-8040 is promising for research of inflammatory pathologies and cardiopulmonary pathologies.