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    Alvelestat (AZD-9668; MPH-966)
    Alvelestat (AZD-9668; MPH-966)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0713
    CAS #: 848141-11-7 Purity ≥98%

    Description: Alvelestat (formerly also known as MPH966; AZD9668) is a novel, potent, orally bioavailable, and highly selective inhibitor of neutrophil elastase (NE) with potential anti-inflammatory activity. It inhibits neutrophil elastase with an IC50 and Ki of 12 nM and 9.4 nM, it is at least 600-fold more selective over other serine proteases. 

    References: J Pharmacol Exp Ther. 2011 Oct;339(1):313-20.

    Related CAS: 1240425-05-1 (Alvelestat tosylate salt)

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    Molecular Weight (MW)545.53
    FormulaC25H22F3N5O4S
    CAS No.848141-11-7 (Alvelestat); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (183.3 mM)
    Water:<1 mg/mL
    Ethanol:<1 mg/mL
    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
    SynonymsAlvelestat; AZD 9668; MPH966; MPH 966; AZD9668; AZD-9668; MPH-966 

    Chemical Name: 6-methyl-5-(1-methyl-1H-pyrazol-5-yl)-N-((5-(methylsulfonyl)pyridin-2-yl)methyl)-2-oxo-1-(3-(trifluoromethyl)phenyl)-1,2-dihydropyridine-3-carboxamide

    InChi Key: QNQZWEGMKJBHEM-UHFFFAOYSA-N

    InChi Code: InChI=1S/C25H22F3N5O4S/c1-15-20(22-9-10-31-32(22)2)12-21(23(34)30-13-17-7-8-19(14-29-17)38(3,36)37)24(35)33(15)18-6-4-5-16(11-18)25(26,27)28/h4-12,14H,13H2,1-3H3,(H,30,34)


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    In Vitro

    In vitro activity: Alvelestat, also known as AZD9668, is an orally bioavailable, novel and highly selective inhibitor of neutrophil elastase (NE) with IC50 and Ki of 12 nM and 9.4 nM, it is at least 600-fold more selective over other serine proteases. Neutrophil elastase (NE) is 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.


    Kinase Assay: AZD9668 had a high binding affinity for human NE (KD = 9.5 nM) and potently inhibited NE activity. The calculated pIC50 (IC50) and Ki values for AZD9668 for human NE were 7.9 (12 nM) and 4.9 nM, respectively. In contrast to earlier NE inhibitors, the interaction between AZD9668 and NE was rapidly reversible. AZD9668 was also highly selective for NE over other neutrophil-derived serine proteases. 


    Cell Assay: In cell-based assays, AZD9668 inhibited plasma NE activity in zymosan-stimulated whole blood. In isolated human polymorphonuclear cells, AZD9668 inhibited NE activity on the surface of stimulated cells and in the supernatant of primed, stimulated cells.AZD9668 showed good crossover potency to NE from other species.

    In VivoIn 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.
    Animal modelHuman NE-induced acute lung injury in mice or rats, guinea pig chronic smoke model.
    Formulation & DosageFormulated in 0.5% hydroxypropyl methylcellulose in citrate buffer, 20% glucose and 0.1% polysorbate in water or corn oil; ~10 mg/kg (mice); ~20 mg/kg (rats); ~100 mg/kg (pigs); oral gavage
    ReferencesJ Pharmacol Exp Ther. 2011 Oct;339(1):313-20.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     

    Alvelestat (AZD9668)

    Effects of AZD9668 on human NE-induced acute lung injury in mice. J Pharmacol Exp Ther. 2011 Oct;339(1):313-20. 
     

    Alvelestat (AZD9668)

    Effects of AZD9668 on human NE-induced acute lung injury in rats. J Pharmacol Exp Ther. 2011 Oct;339(1):313-20. 
     

    Alvelestat (AZD9668)

    Effects of AZD9668 on tobacco smoke-induced airway inflammation in mice. J Pharmacol Exp Ther. 2011 Oct;339(1):313-20. 


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