Home Proteases Serine Protease inhibitor Alvelestat (AZD9668) For research use only.

Alvelestat (AZD9668)

Synonyms: Avelestat

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

Alvelestat (AZD9668) Chemical Structure

CAS No. 848141-11-7

Purity & Quality Control

Alvelestat (AZD9668) Related Products

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
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 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]
Animal Research 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.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01214122 Withdrawn
Pharmacokinetics|Pharmacodynamics
AstraZeneca
 November 2010 Phase 1
NCT01161355 Completed
Healthy
AstraZeneca
 June 2010 Phase 1
NCT01147549 Completed
Healthy
AstraZeneca
 June 2010 Phase 1
NCT01035411 Completed
Chronic Obstructive Pulmonary Disease
AstraZeneca
 November 2009 Phase 1
NCT01034982 Completed
Chronic Obstructive Pulmonary Disease
AstraZeneca
 November 2009 Phase 1

Chemical Information & Solubility

Molecular Weight 545.53 Formula

C25H22F3N5O4S
CAS No. 848141-11-7 SDF Download Alvelestat (AZD9668) SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 57 mg/mL ( (104.48 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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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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