848141-11-7

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 NO: 848141-11-7
• Molecular Formula: C25H22F3N5O4S
• Molecular Weight: 545.5334896
• Product Categories: Inhibitors
• Mol File: 848141-11-7.mol
• Article Data: 2

Chemical Properties

• Boiling Point: 780.4±60.0 °C(Predicted)
• Appearance: /
• Density: 1.42±0.1 g/cm3(Predicted)
• Storage Temp.: -20°C Freezer
• Solubility: DMSO (Slightly), Methanol (Slightly)
• PKA: 11.00±0.20(Predicted)
• CAS DataBase Reference: AZD 9668(CAS DataBase Reference)
• NIST Chemistry Reference: AZD 9668(848141-11-7)
• EPA Substance Registry System: AZD 9668(848141-11-7)

Safety Data

• Hazardous Substances Data: 848141-11-7(Hazardous Substances Data)

Usage

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.

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.

Upstream product

• 848141-14-0 1-(5-(methylsulfonyl)pyridin-2-yl)methanamine hydrochloride 

Relevant articles and documents

NOVEL SALT 628

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 4-methylbenzenesulfonate and a novel crystalline form thereof are disclosed together with processes for preparing such salt and form, pharmaceutical compositions comprising such a salt and form, and the methods of treatment using such a salt and form.