An inhibitor of neutrophil elastase (IC50 = 12 nM); greater than 600-fold selective for neutrophil elastase over several other serine proteases; inhibits neutrophil elastase activity in zymosan-stimulated isolated whole blood and in cell-associated assays (IC50s = 46 and 48 nM

AZD 9668 – 5 mg

Brand:
Cayman
CAS:
848141-11-7
Storage:
-20
UN-No:
De Minimis - 3077 / 9

AZD 9668 is an orally bioavailable inhibitor of neutrophil elastase (IC50 = 12 nM for the human enzyme).{42559} It is greater than 600-fold selective for neutrophil elastase over other serine proteases, including human proteinase-3 and cathepsin G, bovine trypsin and chymotrypsin, and porcine pancreatic elastase. AZD 9668 inhibits neutrophil elastase activity in zymosan-stimulated isolated whole blood and in cell-associated assays (IC50s = 46 and 48 nM, respectively). It decreases the number of neutrophils in bronchoalveolar lavage fluid (BALF) in a mouse model of smoke-induced airway inflammation when administered at a dose of 6 mg/kg. AZD 9668 also prevents airspace enlargement and small airway remodeling in a guinea pig model of chronic smoke-induced inflammation and emphysema.  

 

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SKU: 26083 - 5 mg Category:

Description

An inhibitor of neutrophil elastase (IC50 = 12 nM); greater than 600-fold selective for neutrophil elastase over several other serine proteases; inhibits neutrophil elastase activity in zymosan-stimulated isolated whole blood and in cell-associated assays (IC50s = 46 and 48 nM, respectively); decreases the number of neutrophils in BALF in a mouse model of smoke-induced airway inflammation at 6 mg/kg

Formal name: 1,2-dihydro-6-methyl-5-(1-methyl-1H-pyrazol-5-yl)-N-[[5-(methylsulfonyl)-2-pyridinyl]methyl]-2-oxo-1-[3-(trifluoromethyl)phenyl]-3-pyridinecarboxamide

Synonyms: 

Molecular weight: 545.5

CAS: 848141-11-7

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Immunology & Inflammation|Pulmonary Diseases|COPD/Emphysema

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