AZD 9668
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
- 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.
in vivo
Alvelestat (1-10 mg/kg; oral administration; twice daily; for 4 days; Female BALB/cJBomTac mice) treatment reduces the inflammatory response to cigarette smoke as indicated by a reduction in BAL neutrophils and interleukin-1β[1].
| Animal Model: | Female BALB/cJBomTac mice exposed to smoke cigarette smoke[1] |
| Dosage: | 1 mg/kg , 3 mg/kg , 6 mg/kg , 10 mg/kg |
| Administration: | Oral administration; twice daily; for 4 days |
| Result: | Reduced the inflammatory response to cigarette smoke as indicated by a reduction in BAL neutrophils and interleukin-1β. |
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.
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