AZD 9668

AZD 9668 is an orally bioavailable inhibitor of neutrophil elastase (IC50 = 12 nM for the human enzyme). 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.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. CAS Number: 848141-11-7. Molecular Formula: C25H22F3N5O4S. Formula Weight: 545.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMSO: 5 mg/ml, DMSO:PBS (pH 7.2)(1:5): 0.16 mg/ml. lambdamax: 341 nm. SMILES: CS(C1=CC=C(CNC(C2=CC(C3=CC=NN3C)=C(C)N(C4=CC=CC(C(F)(F)F)=C4)C2=O)=O)N=C1)(=O)=O. InChi Code: InChI=1S/C25H22F3N5O4S/c1-15-20(22-9-10-31-32(22)2)12-21(23(34)30-13-17-7-8-19(14-29-17)38(3,36)37)24(35)33(15)18-6-4-5-16(11-18)25(26,27)28/h4-12,14H,13H2,1-3H3,(H,30,34). InChi Key: QNQZWEGMKJBHEM-UHFFFAOYSA-N.