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    VU 0357121
    VU 0357121

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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 #: V1090
    CAS #: 433967-28-3Purity ≥98%

    Description: VU0357121 (VU-0357121, VU 0357121) is a positive allosteric modulator (PAM) of mGlu5 (metabotropic glutamate receptor 4) with antiparkinsonian-like effects. In inhibits mGlu5 with an EC50 of 33 nM, and exhibits little activity against other mGlu receptor subtypes. 

    References: ACS Chem Neurosci. 2010 Oct 20;1(10):702-716; Mol Pharmacol. 2012 Nov;82(5):860-75.

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    Molecular Weight (MW)305.32
    FormulaC17H17F2NO2
    CAS No.433967-28-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 61 mg/mL (199.8 mM)
    Water: <1 mg/mL
    Ethanol: 21 mg/mL (68.8 mM)
    SMILES CodeO=C(NC1=CC=C(F)C=C1F)C2=CC=C(OCCCC)C=C2
    SynonymsVU-0357121, VU0357121, VU 0357121


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    In Vitro

    In vitro activity: VU0357121 do not bind at the MPEP allosteric site of mGlu5, thus do not possess mGlu5 NAM activity. The A809V/rmGlu5 mutation inhibited the ability of VU0357121 to shift the glutamate concentration−response curve, whereas the response to VU0357121 is not altered by the F585I/rmGlu5 mutation. VU0357121 show weaker cooperativity in the Ca2+ mobilization assay in the low-expressing HEK293A-mGlu5 cell line. 


    Kinase Assay: VU0357121 is a novel positive and highly selective allosteric modulator (PAM) of mGlu5R with EC50 of 33 nM.


    Cell Assay: VU0357121 is a novel and highly selective positive allosteric modulator (PAM) of mGlu5 (metabotropic glutamate receptor 4) with EC50 of 33 nM; it is inactive or very weakly antagonizing at other mGlu receptor subtypes. ositive allosteric modulators (PAMs) of metabotropic glutamate receptor 4 (mGlu₄), including N-phenyl-7-(hydroxyimino) cyclopropa[b]chromen-1a-carboxamide, can produce antiparkinsonian-like effects in preclinical models of PD. Mutagenesis studies indicate that VU0357121 and related analogues bind to a yet uncharacterized allosteric site on mGlu(5), distinct from CPPHA, yet share a functional interaction with the MPEP site. 

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    ReferencesACS Chem Neurosci. 2010 Oct 20;1(10):702-716; Mol Pharmacol. 2012 Nov;82(5):860-75.


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

    VU 0357121

    Test compounds are able to potentiate the calcium flux response of mGlu5 to a suboptimal (EC20) concentration of glutamate. ACS Chem Neurosci. 2010 Oct 20;1(10):702-716.
     
     

    VU 0357121

    Benzamide PAMs induce a leftward shift in the glutamate response curve at mGlu5. ACS Chem Neurosci. 2010 Oct 20;1(10):702-716.
     

    VU 0357121

    Benzamide compounds are able to potentiate the calcium mobilization response of mGlu5 to glutamate. ACS Chem Neurosci. 2010 Oct 20;1(10):702-716.


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