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    VU 0364439
    VU 0364439

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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 #: V1085
    CAS #: 1246086-78-1Purity ≥98%

    Description: VU 0364439 (VU0364439; VU-0364439) is a mGlu4 (metabotropic glutamate receptor 4) positive allosteric modulator (PAM) with important biological activity. It inhibits mGlu4 with an EC50 value of 19.8 nM. Due to the fact that VU 0364439 possessed less favorable pharmacokinetic properties, thus it can not be used as an in vivo tool, but VU 0364439 might inform the mGlu4 community with more in vitro tool compounds. The activation of the mGlu4 receptor, either with an orthosteric agonist or a positive allosteric modulator (PAM), provides impactful interventions in diseases such as Parkinson's disease, anxiety, and pain. mGlu4 PAMs may have several advantages over mGlu4 agonists for a number of reasons. 

    References: Bioorg Med Chem Lett. 2010 Sep 1;20(17):5175-8;  2011 Jul 28;54(14):5070-81.

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    Molecular Weight (MW)422.29
    FormulaC18H13Cl2N3O3S
    CAS No.1246086-78-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 85 mg/mL (201.3 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    SMILES CodeO=C(C1=NC=CC=C1)NC2=CC=C(S(=O)(NC3=CC=CC=C3Cl)=O)C(Cl)=C2
    SynonymsVU0364439, VU-0364439, VU 0364439


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    In Vitro

    In vitro activity: VU 0364439 is a mGlu4 (metabotropic glutamate receptor 4) positive allosteric modulator (PAM) with EC50 value of 19.8 nM. VU 0364439 possessed less favorable pharmacokinetic properties. The properties of VU 0364439 prevents VU 0364439 itself from being used as an in vivo tool, but VU 0364439 might inform the mGlu4 community with more in vitro tool compounds. The activation of the mGlu4 receptor, either with an orthosteric agonist or a positive allosteric modulator (PAM), provides impactful interventions in diseases such as Parkinson's disease, anxiety, and pain. mGlu4 PAMs may have several advantages over mGlu4 agonists for a number of reasons. 


    Kinase Assay: VU 0364439 is a mGlu4 (metabotropic glutamate receptor 4) positive allosteric modulator (PAM) with EC50 value of 19.8 nM.


    Cell Assay:  VU 0364439 exhibited excellent in vitro maximal response and potency relative to another PAM, (−)-PHCCC (a partially selective mGlu4 potentiator, its chemical structure could be found in reference 4). Starting at 30µM, using a 1:3 serial dilutions, VU 0364439 was tested in triplicate. The entire test was performed on one day. Finally, the % (−)-PHCCC value of VU 0364439 was 102.3. The value of % (−)-PHCCC was computed through dividing the maximal response elicited by VU 0364439 by the response of the control PAM, (−)-PHCCC, on the same day. It was also found that the EC50 value of VU 0364439 was 19.8 nM at human mGlu4 

    In VivoVU 0364439 possess less than ideal PK properties preventing their use as in vivo tools. It shows better stability in HLM (63% remaining) than RLM (2% remaining).  
    Animal modelN/A
    Formulation & DosageN/A
    ReferencesBioorg Med Chem Lett. 2010 Sep 1;20(17):5175-8;  2011 Jul 28;54(14):5070-81.


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

    VU 0364439

    Concentration-dependent potentiation of glutamate in mGlu4/Gqi5 CHO cells by 5. In the absence of an EC20 concentration of glutamate, 5, does not elicit receptor activation.  2010 Sep 1;20(17):5175-8. 
     

    VU 0364439

    HTS Hit (VU0130734, 4) to lead (VU0361591, 5).  2010 Sep 1;20(17):5175-8.



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