| Identification | Back Directory | [Name]
AZD 9668 | [CAS]
848141-11-7 | [Synonyms]
AZD9668
CS-1060
AZD 9668
AZD-9668
Avelestat
Alvelestat
Cavosonstat
Avelestat (AZD9668)
Alvelestat (AZD9668)
AZD9668; AZD-9668; AZD 9668
6-methyl-1-(3-methylphenyl)-5-(2-methylpyrazol-3-yl)-n-[(5-methylsulfonylpyridin-2-yl)methyl]-2-oxopyridine-3-carboxamide
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
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
3-Pyridinecarboxamide, 1,2-dihydro-6-methyl-5-(1-methyl-1H-pyrazol-5-yl)-N-[[5-(methylsulfonyl)-2-pyridinyl]methyl]-2-oxo-1-[3-(trifluoromethyl)phenyl]-
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 (AZD9668) | [Molecular Formula]
C25H22F3N5O4S | [MDL Number]
MFCD26960961 | [MOL File]
848141-11-7.mol | [Molecular Weight]
545.53 |
| Chemical Properties | Back Directory | [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) | [form ]
Solid | [pka]
11.00±0.20(Predicted) | [color ]
White |
| Hazard Information | Back Directory | [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.
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| [target]
NE | [storage]
Store at -20°C | [References]
[1] stevens t, ekholm k, gr?nse 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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| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
|
| Website: |
www.spiropharma.com.cn |
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