[CAS NO. 848141-11-7]  Alvelestat (AZD9668)

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PRODUCTS SPECIFICATIONS [848141-11-7]

Store
Catalog
SLK-S7218
Brand
Selleck
CAS
848141-11-7

DESCRIPTION [848141-11-7]

Overview

MDLMFCD26960961
Molecular Weight545.53
Molecular FormulaC25H22F3N5O4S
SMILESO=C(C1=CC(C2=CC=NN2C)=C(C)N(C3=CC=CC(C(F)(F)F)=C3)C1=O)NCC4=NC=C(S(=O)(C)=O)C=C4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM1.8331 mL9.1654 mL18.3308 mL
5 mM0.3666 mL1.8331 mL3.6662 mL
10 mM0.1833 mL0.9165 mL1.8331 mL
50 mM0.0367 mL0.1833 mL0.3666 mL

Description

Alvelestat (AZD9668, Avelestat) is an oral, highly selective inhibitor of with and 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.

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.