Alvelestat

SKU: orb1304533

Description

Alvelestat (AZD9668) is an oral, selective, and reversible inhibitor of human neutrophil elastase (NE). It has demonstrated anti-inflammatory activity in research models of pulmonary diseases such as COPD and bronchiectasis, as investigated in both in vitro and in vivo studies.

Research Area

Protein Biochemistry

Key Properties

• CAS Number: 848141-11-7
• MW: 545.53
• Purity: 98.00% (May vary between batches)
• Formula: C₂₅H₂₂F₃N₅O₄S
• SMILES: Cc1c(cc(C(=O)NCc2ccc(cn2)S(C)(=O)=O)c(=O)n1-c1cccc(c1)C(F)(F)F)-c1ccnn1C
• Target: Serine Protease
• Solubility: DMSO:40 mg/mL (73.32 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.67 mM)

Bioactivity

• Target IC50:
  Neutrophil elastase:12 nM|Neutrophil elastase:9.4 nM(Ki)
• In Vivo:
  In whole blood stimulated by yeast polysaccharide, AZD9668 effectively inhibits NE (NE) activity in the supernatant of antigen-challenged cells and on the surface of stimulated polymorphonuclear cells.
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• In Vitro:
  In a mouse model of (smoke)-induced airway inflammation, AZD9668 significantly reduced the number of (neutrophils) in the bronchoalveolar lavage (BAL) and the level of BAL IL-1β. Oral administration of AZD9668 in both mice and rats was able to inhibit (NE)-induced lung injury.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

neutrophil elastase, inhibit, Elastase, Inhibitor, AZD 9668, AZD9668, AZD-9668, Avelestat, Alvelestat, SerineProtease, Serine Protease

Compound Identifiers

PubChem CID

46861623