Alvelestat (AZD9668)

Catalog No.S7218 Synonyms: Avelestat

For research use only.

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.

Alvelestat (AZD9668) Chemical Structure

CAS No. 848141-11-7

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

Purity & Quality Control

Choose Selective Serine Protease Inhibitors

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 Research:

[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.

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(183.3 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 545.53
Formula

C25H22F3N5O4S

CAS No. 848141-11-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C=C(C(=O)N1C2=CC=CC(=C2)C(F)(F)F)C(=O)NCC3=NC=C(C=C3)S(=O)(=O)C)C4=CC=NN4C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

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%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02669251 Recruiting Drug: MPH966 Chronic Graft vs Host Disease|Chronic Graft-Versus-Host-Disease|Bronchiolitis Obliterans Syndrome National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) April 28 2016 Phase 1|Phase 2
NCT01214122 Withdrawn Drug: AZD9668|Drug: Warfarin Pharmacokinetics|Pharmacodynamics AstraZeneca November 2010 Phase 1
NCT01161355 Completed Drug: AZD9668 Healthy AstraZeneca June 2010 Phase 1
NCT01147549 Completed Drug: [C14]AZD9668 Healthy AstraZeneca June 2010 Phase 1
NCT01035411 Completed Drug: AZD9668 Chronic Obstructive Pulmonary Disease AstraZeneca November 2009 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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