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    VU 0361737
    VU 0361737

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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 #: V1092
    CAS #: 1161205-04-4Purity ≥98%

    Description: VU 0361737 (VU0361737; VU-0361737) is a novel, brain-penetrable and selective positive allosteric modulator (PAM) for mGlu4 receptor with important biological activity. It inhibits mGlu4 receptor with an EC50 of 240 nM and 110 nM at human and rat receptors, respectively. It exhibits little activity against mGlu5/8 receptors.

    References: J Med Chem. 2009 Jul 23;52(14):4115-8; J Med Chem. 2011 Feb 24;54(4):1106-10.

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    Molecular Weight (MW)262.69
    FormulaC13H11ClN2O2
    CAS No.1161205-04-4
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 53 mg/mL (201.8 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    SMILES O=C(C1=NC=CC=C1)NC2=CC=C(Cl)C(OC)=C2
    Synonyms VU 0361737, VU-0361737, VU0361737; ML 128; ML-128; ML128


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    In Vitro

    In vitro activity: VU0361737 is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors and displays weak activity at mGlu5 and mGlu8 receptors.


    Kinase Assay: VU 0361737 is a selective positive allosteric modulator (PAM) for mGlu4 receptor with EC50 of 240 nM and 110 nM at human and rat receptors, respectively, displays weak activity at mGlu5 and mGlu8 receptors, is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors.

    In VivoVU0361737 shows high in vivo CL in rat, a short half-life (T1/2 20 min), and demonstrates significant brain exposure (brain-to-plasma ratio of 4.1).
    Animal modelSprague-Dawley rats
    Formulation & DosageDissolved in 10% Tween-80; 10 ml/kg; i.p. administration
    ReferencesJ Med Chem. 2009 Jul 23;52(14):4115-8; J Med Chem. 2011 Feb 24;54(4):1106-10.


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

    VU 0361737

    Potency and efficacy of the novel mGluR4 PAM. J Med Chem. 2009 Jul 23;52(14):4115-8.
     

    VU 0361737

    Initial HTS hits.   2009 Jul 23;52(14):4115-8.

     

    VU 0361737

    Chemical structure of (-)-PHCCC, 1, the mGluR4 ago-potentiator VU0155041, 2, and mGluR4 PAMs VU0001171, 3, VU0080241, 4, and VU0092145, 5.  2009 Jul 23;52(14):4115-8.


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