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.

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