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    MRS 2578
    MRS 2578

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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 #: V1302
    CAS #: 711019-86-2Purity ≥98%

    Description: MRS2578 (MRS-2578; MRS 2578) is a potent and selective P2Y6 receptor antagonist with potentially usefulness in controlling persistent storage symptoms in obstructed patients. It inhibits P2Y6 receptor with an IC50 of 37 nM and exhibits little activity against closely related P2Y1, P2Y2, P2Y4, and P2Y11 receptors. Activation of P2Y6 receptor amplifies mucosal adenosine triphosphate release underlying bladder overactivity in patients with benign prostatic hyperplasia. Therefore, selective P2Y6 receptor blockade as a novel therapeutic strategy is potentially useful to control persistent storage symptoms in obstructed patients. 

    References: Blood. 2011 Feb 24;117(8):2548-55; Biochem Pharmacol. 2004 May 1;67(9):1763-70.

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    Molecular Weight (MW)472.67
    FormulaC20H20N6S4 
    CAS No.711019-86-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 42 mg/mL (88.8 mM)
    Water:<1 mg/mL
    Ethanol:<1 mg/mL
    Solubility (In vivo)30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL  
    SynonymsMRS-2578; MRS2578; MRS 2578.


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    In Vitro

    In vitro activity: MRS2578 selectively blocks P2Y6 receptor activity versus activity at P2Y1, P2Y2, P2Y4 or P2Y11 receptors. MRS2578 (1 μM) completely blocks the protection by UDP undergoing TNFalpha-induced apoptosis in 1321N1 astrocytoma cells. MRS 2578 inhibits basal NF-κB activity in time and dose dependent manner in HMEC-1 cells transfected with 0.25 μg NF-κB promoter reporter. MRS 2578 (10 μM) completely abolishes TNF-α induced NF-κB reporter activity in HMEC-1 cells. MRS 2578 (10 μM) significant reduces TNF-α–induced proinflammatory gene expression in HMEC-1 cells. MRS 2578 potentiates ATPγS and UDP response at concentrations below 316 nM whereas above this concentration, MRS 2578 inhibits ATPS- and UDP-induced IP accumulation in neonatal rat cardiac myofibroblasts. MRS2578-treated mice shows reduced bronchial hyperresponsiveness toward methacholine in OVA-sensitized mice. MRS2578 completely blocks UDP-induced the release of IL-6, KC, and IL-8 in lung epithelial cells.


    Cell Assay: MRS2578 (1 μM) completely blocks the protection by UDP undergoing TNFα-induced apoptosis in 1321N1 astrocytoma cells. MRS 2578 (10 μM) completely abolishes TNF-α induced NF-κB reporter activity in HMEC-1 cells. MRS 2578 (10 μM) significant reduces TNF-α–induced proinflammatory gene expression in HMEC-1 cells

    In VivoMRS 2578 (10 μM) attenuates Keratinocyte-derived chemokine serum protein levels in LPS-induced vascular inflammation in C57BL/6 mice. MRS2578 (10 μM, intratracheally) reduces BALF eosinophilia and the levels of IL-5 and IL-13 in the BALF in OVA-sensitized mice and leads to a markedly attenuated change in methacholine responsiveness after OVA challenge. MRS2578 (10 μM, intratracheally) inhibits house dust mite–induced allergic airway inflammation in OVA-sensitized mice. MRS2578 (10 μM, intratracheally) reduces of IL-6 and KC levels in BALF in OVA-sensitized mice.
    Animal modelMurine endotoxinemia model 
    Formulation & DosageDissolved in saline; 10 μM (100 μL); i.v. 
    References

    Blood. 2011 Feb 24;117(8):2548-55; Biochem Pharmacol. 2004 May 1;67(9):1763-70.


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

    MRS 2578

    Inositol phosphate production in human P2Y6-transfected 1321N1 human astrocytes. Biochem Pharmacol. 2004 May 1;67(9):1763-70.



    MRS 2578

    Concentration dependence of inhibition by compounds 5 and 11 of inositol phosphate production induced by UDP (300 nM) in human P2Y6-receptor transfected 1321N1 human astrocytes.

    MRS 2578

    (A) Inositol phosphate production in human P2Y6-transfected 1321N1 human astrocytes. (B) Concentration dependence of inhibition by compound MRS2575 (7) of inositol phosphate production induced by UDP (300 nM) in human P2Y6-receptor transfected 1321N1 human astrocytes. Biochem Pharmacol. 2004 May 1;67(9):1763-70.
     

    MRS 2578

    Effects of P2Y6 receptor antagonists on cell death induced by the treatment of hP2Y6 receptor-expressing 1321N1 astrocytoma cells with TNFα. Biochem Pharmacol. 2004 May 1;67(9):1763-70.

    MRS 2578

    Effect of P2Y6 receptor antagonist MRS 2578 on endothelial NF-κB activity. Blood. 2011 Feb 24;117(8):2548-55.

    MRS 2578

    Effect of P2Y6 receptor antagonist MRS 2578 on TNF-α–induced gene expression in vascular endothelia. Blood. 2011 Feb 24;117(8):2548-55.
     

    MRS 2578

    P2Y6 receptor expression after intravenous LPS treatment and attenuated inflammatory responses in P2Y6−/− mice after intravenous LPS exposure. Blood. 2011 Feb 24;117(8):2548-55. 


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