Alvelestat

SKU: orb1223038

Description

Avelestat, also known as AZD9668 and MPH-966, is a novel, oral inhibitor of neutrophil elastase (NE), an enzyme implicated in the signs, symptoms, and disease progression in NE-driven respiratory diseases such as bronchiectasis and chronic obstructive pulmonary disease via its role in the inflammatory process, mucus overproduction, and lung tissue damage. In cell-based assays, AZD9668 inhibited plasma NE activity in zymosan-stimulated whole blood. AZD9668 has the potential to reduce lung inflammation and the associated structural and functional changes in human diseases.

Key Properties

• CAS Number: 848141-11-7
• MW: 545.53
• Purity: >98% (HPLC)
• Formula: C₂₅H₂₂F₃N₅O₄S
• SMILES: c1(n(c(=O)c(cc1c1n(ncc1)C)C(=O)NCc1ccc(cn1)S(=O)(=O)C)c1cc(ccc1)C(F)(F)F)C
• Target: Proteasome
• Solubility: DMSO : ≥ 33 mg/mL; 60.49 mM

Bioactivity

• In Vivo:
  Animal model: Female BALB/cJBomTac mice exposed to smoke cigarette smoke. 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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• In Vitro:
  Cell Viability Assay Cell line: Human bronchial epithelial cells (HBE) and human alveolar epithelial cells (A549). Concentration: 20 μg/mL. Incubation time: 16 hours. Result: Decreased cytotoxicity and inflammatory responses.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AZD-9668 | MPH966 | Alvelestat

Quick Database Links

Gene Symbol

Proteasome