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| | AZD 9668 Basic information |
| Product Name: | AZD 9668 | | Synonyms: | Alvelestat;AZD 9668;AZD9668;AZD-9668;Avelestat (AZD9668);6-Methyl-5-(1-methyl-1H-pyrazol-5-yl)-N-[[5-(methylsulfonyl)pyridin-2-yl]methyl]-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2-dihydropyridine-3-carboxamide;Avelestat;Alvelestat (AZD9668) | | CAS: | 848141-11-7 | | MF: | C25H22F3N5O4S | | MW: | 545.53 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 848141-11-7.mol |  |
| | AZD 9668 Chemical Properties |
| Melting point | 207-209°C | | Boiling point | 780.4±60.0 °C(Predicted) | | density | 1.42±0.1 g/cm3(Predicted) | | storage temp. | -20°C Freezer | | solubility | DMSO (Slightly), Methanol (Slightly) | | pka | 11.00±0.20(Predicted) | | form | Solid | | color | White |
| | AZD 9668 Usage And Synthesis |
| Description | 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. | | Uses | Avelstat inhibits plasma neutrophil elastase (NE) activity in zymosan-stimulated whole blood, and also inhibits NE activity on the surface of stimulated polymorphonuclear cells and in the supernatant of primed, stimulated cells. | | target | NE | | references | [1] stevens t, ekholm k, gränse m, et al. azd9668: pharmacological characterization of a novel oral inhibitor of neutrophil elastase. journal of pharmacology and experimental therapeutics, 2011, 339(1): 313-320. |
| | AZD 9668 Preparation Products And Raw materials |
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