My cart
In the shopping cart is not goods, to choose and buy!
  • Product Name
  • Size
  • Quantity
  • Amount
    Selected items : 0 pieces Total : CHECK OUT()
    VU 0364770
    VU 0364770

    Price:
    Market Price:

    This product is for research use only, not for human use. We do not sell to patients.
    Number: - + Pieces(InventoryPieces)
    InvivoChem Cat #: V1091
    CAS #: 61350-00-3Purity ≥98%

    Description: VU 0364770 (VU-0364770, VU0364770) is a potent positive allosteric modulator (PAM) of mGlu4 (metabotropic glutamate receptor 4) with anti-parkinsonian-like activity. It inhibits mGlu with an EC50 of 1.1 μM for human mGlu4. It exhibits little activity at 68 other receptors such as other mGlu subtypes. Positive allosteric modulators (PAMs) of metabotropic glutamate receptor 4 (mGlu₄), including N-phenyl-7-(hydroxyimino) cyclopropa[b]chromen-1a-carboxamide, can produce anti-parkinsonian-like effects in preclinical models of PD. VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson's disease.  

    References: J Pharmacol Exp Ther. 2012 Feb;340(2):404-21.

    Customer Validation
    Official Supplier of
    • VE
    • OF
    • YALE
    • hhmi
    • 香港大学
    Related Products
    Publications Citing InvivoChem Products
    • Physicochemical and Storage Information
    • Protocol
    • Quality Control Documentation
    • Related Biological Data
    • Customer Review
    Molecular Weight (MW)232.67
    FormulaC12H9ClN2O
    CAS No.61350-00-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 47 mg/mL (202.0 mM)
    Water: <1 mg/mL
    Ethanol: 47 mg/mL (202.0 mM)
    SMILES CodeO=C(C1=NC=CC=C1)NC2=CC=CC(Cl)=C2
    SynonymsVU0364770, VU 0364770, VU 0364770


    • Molarity Calculator
    • Dilution Calculator
    • The molarity calculator equation

      Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

      • Mass
      • Concentration
      • Volume
      • Molecular Weight *
      • =
      • ×
      • ×
    • The dilution calculator equation

      Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

      This equation is commonly abbreviated as: C1V1 = C2V2

      • Concentration (start)
      • ×
      • Volume (start)
      • =
      • Concentration (final)
      • ×
      • Volume (final)
      • ×
      • =
      • ×
      • C1
      •  
      • V1
      •  
      • C2
      •  
      • V2
    In Vitro

    In vitro activity: VU 0364770 is a positive allosteric modulator (PAM) of mGlu4 (metabotropic glutamate receptor 4) with EC50 of 1.1 μM for human mGlu4, it exhibits insignificant activity at 68 other receptors, including other mGlu subtypes. Positive 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. VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson's disease. VU0364770 exhibits a potency of 290 ± 80 nM at rat mGlu4 and induces an 18.1 ± 1.7-fold left shift of the glutamate concentration-response curve. 


    Kinase Assay: the effects of VU0364770 on rat mGlu1 and mGlu5 are assessed by using calcium mobilization and measuring the glutamate concentration-response relationship in the presence and absence of 10 μM VU0364770. Using a double-addition protocol, VU0364770 is added to the cells, followed 2.5 min later by a full concentration-response of glutamate. Shifts of the concentration-response relationship are used to assess potential potentiator (left shift of more than 2-fold) or antagonist (right shift of more than 2-fold or depression of the maximum response by at least 75%) activity of VU0364770. Compounds are further assessed for mGlu5 antagonist activity by performing a full concentration-response curve, starting at 30 μM and serially diluted it by using 1:3 dilutions, in the presence of an EC80 concentration of glutamate. VU0364770 is a potent and effective positive allosteric modulator of mGlu4. VU0346770 exhibits a potency of 1.1 ± 0.2 μM at human mGlu4 in the presence of an EC20 concentration of glutamate and shifts the glutamate concentration-response curve 31.4 ± 4.0-fold to the left. VU0364770 exhibits a potency of 290 ± 80 nM at rat mGlu4 and induces an 18.1 ± 1.7-fold left shift of the glutamate concentration-response curve.

    In VivoVU0364770 shows efficacy alone or when administered in combination with l-DOPA or an adenosine 2A (A2A) receptor antagonist preladenant currently in clinical development. When administered alone, VU0364770 exhibits efficacy in reversing haloperidol-induced catalepsy, forelimb asymmetry-induced by unilateral 6-hydroxydopamine (6-OHDA) lesions of the median forebrain bundle, and attentional deficits induced by bilateral 6-OHDA nigrostriatal lesions in rats. In addition, VU0364770 enhances the efficacy of preladenant to reverse haloperidol-induced catalepsy when given in combination. The effects of VU0364770 to reverse forelimb asymmetry are also potentiated when the compound is coadministered with an inactive dose of l-DOPA, suggesting that mGlu4 positive allosteric modulator may provide l-DOPA-sparing activity. 
    Animal modelHaloperidol-Induced Catalepsy 
    Formulation & DosageSuspended in an aqueous solution of 10% Tween 80; 1 to 2 ml/kg i.p./s.c. or 10 ml/kg p.o.; s.c. or p.o. administration
    ReferencesJ Pharmacol Exp Ther. 2012 Feb;340(2):404-21.


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

    VU 0364770

    VU0364770 exhibits anticataleptic efficacy up to 2 h after administration.  J Pharmacol Exp Ther.2012 Feb;340(2):404-21.

    VU 0364770

    U0364770 has no effect on spontaneous locomotor activity in the open field (A) or performance on the rotorod test (B). J Pharmacol Exp Ther. 2012 Feb; 340(2): 404–421.  J Pharmacol Exp Ther. 2012 Feb;340(2):404-21.

     


    VU 0364770

    VU0364770 and the A2A antagonist preladenant produce an enhanced anticataleptic effect in rats when administered in combination. J Pharmacol Exp Ther. 2012 Feb;340(2):404-21.

    VU 0364770

    U0364770 has no effect on spontaneous locomotor activity in the open field (A) or performance on the rotorod test (B). J Pharmacol Exp Ther. 2012 Feb;340(2):404-21.

    VU 0364770

    VU0364770 exhibits efficacy in bilateral 6-OHDA-lesioned animals exhibiting attentional and akinetic deficits in the reaction time task. J Pharmacol Exp Ther. 2012 Feb;340(2):404-21.


    评论

      Home Prev Next Last page / pices

      发评论

      ×
      Your information is safe with us. * Required Fields.
      Products are for research use only;  We do not sell to patients
      Tel: 1-708-310-1919
      Fax: 1-708-557-7486
      Subscribe to our E-newsletter
      • Name*
      • *
      • E-mail*
      • *
      • instructions:
      • *
      Copyright 2020 InvivoChem LLC | All Rights Reserved
      prompt
      Do you confirm the receipt?