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    VX-702
    VX-702

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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 #: V0480
    CAS #: 745833-23-2 Purity ≥98%

    Description: VX-702 is a novel, highly potent, orally bioavailable and selective inhibitor of p38α MAPK with potential anti-inflammatory activity. It inhibits p38α MAPK with 14-fold higher potency than p38β. It is one of the 2nd-generation and orally bioactive p38 MAP kinase inhibitors that are potentially useful for the treatment of inflammation, rheumatoid arthritis and cardiovascular diseases. VX-702 prevents activation of p38MAPK and decrements in many platelet storage parameters after exposure to 16 °C without agitation for 24 h. 

    References: Thromb Haemost. 2004 Dec;92(6):1387-93; Circulation. 2003;108:e9045-e9046.

    Related CAS: 479543-46-9

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    Molecular Weight (MW)404.3
    FormulaC19H12F4N4O2
    CAS No.745833-23-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 81 mg/mL (200.3 mM)
    Water: <1 mg/mL
    Ethanol:<1 mg/mL
    Solubility (In vivo)30% PEG400+0.5% Tween80+5% propylene glycol: 30mg/mL
    SynonymsVX-702; VX 702; VX702 


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    In Vitro

    In vitro activity: Pre-incubation of platelets with VX-702 (1 μM) completely or partially inhibits p38 activation (IC50 4 to 20 nM) induced by platelet agonists including thrombin, SFLLRN, AYPGKF, U46619 and collagen. VX-702 shows no effect on platelet aggregation induced by any of the p38 MAPK agonists in the presence or absence of anti-platelet therapies. VX-702 inhibits the production of IL-6, IL-1β and TNFα (IC50 = 59, 122 and 99 ng/mL, respectively) in a dose-dependent manner.


    Kinase Assay: Pre-incubation of platelets with VX-702 (1 μM) completely or partially inhibits p38 activation (IC50 4 to 20 nM) induced by platelet agonists including thrombin, SFLLRN, AYPGKF, U46619 and collagen. VX-702 shows no effect on platelet aggregation induced by any of the p38 MAPK agonists in the presence or absence of anti-platelet therapies. VX-702 inhibits the production of IL-6, IL-1β and TNFα (IC50 = 59, 122 and 99 ng/mL, respectively) in a dose-dependent manner.


    Cell Assay: In the isolated perfused rat kidney (IPRK) model, administration of VX-702 at a range of doses between 100 and 600 ng/mL showed linear excretion and the clearance data were consistent with net reabsorption by the kidney. Further, VX-702 was showed not a substrate for renal organic anion and organic cation transport systems.

    In VivoThe half-life of VX-702 is 16 to 20 hours, with a median clearance of 3.75 L/h and a volume of distribution of 73 L/kg. Both AUC and Cmax values are dose proportional for VX-702, which is predominantly cleared renally.  VX-702 (at a dose of 0.1 mg/kg twice daily) has an equivalent effect as that of methotrexate (0.1 mg/kg). In addition, VX-702 (5 mg/kg twice daily) also has an equivalent effect as prednisolone (10 mg/kg once daily), as measured by percentage inhibition of wrist joint erosion and inflammation score. VX-702 selectively inhibits activation of p38 MAPK after ischemia with no effects on ERKs and JNKs. The MI/AAR ratio is significantly reduced in the 50 mg/kg group compared with the 5 mg/kg and vehicle groups.
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    References

    Thromb Haemost. 2004 Dec;92(6):1387-93; Circulation. 2003;108:e9045-e9046.


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

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