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    A-804598 (A804598)
    A-804598 (A804598)

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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 #: V0084
    CAS #: 1125758-85-1 Purity ≥98%

    Description: A-804598 (A 804598) is a structurally novel, CNS penetrant, potent, competitive, and selective antagonist of the purinergic P2X7 receptors (IC50 = 10 nM, 9 nM and 11 nM for rat, mouse and human P2X7 receptors respectively) with potential anti-inflammatory activity. Purinergic P2X7 receptors (P2X7Rs) play an important role in the generation of inflammatory responses during a number of CNS pathologies. A804598 treatment reversed the changes in microglia and astrocytes, reduced/abolished increases in mRNA levels of number of inflammatory markers, including IL-1β, iNOS, CXCR2, and components of inflammatory signaling pathways, such as TLR2, CASP1, NF-kB1 and CREB1, as well in the protein levels of pro-IL-1β and Nf-kB1. 

    References: Journal of Neuroimmune Pharmacology, 2019,14, 263–277 2009 Jan;56(1):223-9. 

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    Molecular Weight (MW) 315.38
    Formula C19H17N5
    CAS No. 1125758-85-1 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: > 10mg/mL
    Water: N/A
    Ethanol: N/A
    Chemical NameN-Cyano-N′′-[(1S)-1-phenylethyl]-N′-5-quinolinyl-guanidine
    SynonymsA-804598; A 804598; A804598
    SMILES CodeC[[email protected]](/N=C(NC1=C2C=CC=NC2=CC=C1)/NC#N)C3=CC=CC=C3


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    In Vitro

    In vitro activity: A-804598 is a structurally novel, competitive, and selective antagonist that has equivalent high affinity at rat (IC50 = 10 nM), mouse (IC50 = 9 nM) and human (IC50 = 11 nM) P2X7 receptors. A-804598 also potently blocks agonist stimulated release of IL-1β(IC50 of 8.5 nM) and Yo-Pro uptake (IC50 of 8.1 nM) from differentiated THP-1 cells that natively express human P2X7 receptors. Although A-840598 potently blocks P2X7 receptor activation, at concentrations up to 100 μM, it does not significantly reduce agonist-evoked changes in intracellular calcium concentrations mediated by a variety of other P2X and P2Y receptors. A-840598 shows weak or no activity for interating with a large array of G-protein-coupled receptors, enzymes, transporters, and ion channels (CEREP, Poitiers, France)(IC50 > 5-10 μM).


    Kinase Assay: A-804598 is a CNS penetrant, competitive and selective P2X7 receptor antagonist with IC50s of 9 nM, 10 nM and 11 nM for mouse, rat and human P2X7 receptors, respectively.


    Cell Assay: SOD1-G93A microglia are treated with 300 μM BzATP or 3 mM ATP for 15 min or 1 h with or without 10 μM A-804598 and subjected to western blotting and immunoreactions with anti-p-mTOR and anti-mTOR or anti-GAPDH. 

    In VivoInhibition of P2X7 by A-804598 in SOD1-G93A mice suppresses SQSTM1/p62 up-regulation in lumbar spinal cord.
    Animal model SOD1-G93A mice
    Formulation & Dosage 30 mg/kg; i.p.
    References  2009 Jan;56(1):223-9;  2017 Aug 21;11:249. 


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

    A-804598

    P2X7 activation modulates microtubule-associated protein 1 light chain 3 (LC3)-II in superoxide dismutase 1 (SOD1)-G93A microglia.  2017 Aug 21;11:249.

     

    A-804598

    P2X7 induces autophagic flux in SOD1-G93A microglia.  2017 Aug 21;11:249.

     

    A-804598

    In vivo chronic treatment with P2X7 antagonist A-804598 decreases SQSTM1/p62 expression in lumbar spinal cord of SOD1-G93A mice.  2017 Aug 21;11:249.


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