Alvelestat (AZD9668)

Catalog No.S7218 Batch:S721802

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Technical Data

Formula

C25H22F3N5O4S
Molecular Weight 545.53 CAS No. 848141-11-7
Solubility (25°C)* In vitro DMSO 57 mg/mL (104.48 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Alvelestat (AZD9668, Avelestat) is an oral, highly selective inhibitor of neutrophil elastase (NE) with IC50 and Ki of 12 nM and 9.4 nM, at least 600-fold more selective over other serine proteases. Phase 2.
Targets
neutrophil elastase [1]
(Cell-free assay)		 neutrophil elastase [1]
(Cell-free assay)
9.4 nM(Ki) 12 nM
In vitro AZD9668 inhibits plasma 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. [1]
In vivo In mice and rats, AZD9668 (p.o.) prevents human NE-induced lung injury. In a mouse model of smoke-induced airway inflammation, AZD9668 significantly reduces the number of BAL neutrophils and BAL IL-1β. In a guinea pig chronic smoke model, AZD9668 prevents airspace enlargement and small airway wall remodeling in guinea pigs in response to chronic tobacco smoke exposure. [1]

Protocol (from reference)

Animal Study:

[1]
  • Animal Models

    Human NE-induced acute lung injury in mice or rats, guinea pig chronic smoke model.

  • Dosages

    ~10 mg/kg (mice); ~20 mg/kg (rats); ~100 mg/kg (pigs)

  • Administration

    p.o.

Selleck's Alvelestat (AZD9668) has been cited by 4 publications

Inhibition of elastase enhances the adjuvanticity of alum and promotes anti-SARS-CoV-2 systemic and mucosal immunity [ Proc Natl Acad Sci U S A, 2021, 118(34)e2102435118] PubMed: 34353890
A Novel Supplementation Approach to Enhance Host Response to Sublingual Vaccination [ Sci Rep, 2019, 9(1):715] PubMed: 30679470
NETs promote ALI/ARDS inflammation by regulating alveolar macrophage polarization. [ Exp Cell Res, 2019, 382(2):111486] PubMed: 31255598
Inhibitors of elastase stimulate murine B lymphocyte differentiation into IgG‐and IgA‐producing cells [Attia Z Eur J Immunol, 2018, 48(8):1295-1301] PubMed: 29710424

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.