VU 0364770

CAS No. 61350-00-3

VU 0364770( VU0364770, VU 0364770, VU 0364770 )

Catalog No. M18900 CAS No. 61350-00-3

VU 0364770(EC50=1.1 μM), a positive allosteric modulator(PAM) of mGlu4, shows insignificant activity at 68 other receptors, including other mGlu subtypes.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    VU 0364770
  • Note
    Research use only, not for human use.
  • Brief Description
    VU 0364770(EC50=1.1 μM), a positive allosteric modulator(PAM) of mGlu4, shows insignificant activity at 68 other receptors, including other mGlu subtypes.
  • Description
    VU0364770 is a Positive allosteric modulator at mGlu4 receptors (EC50 = 290 nM in mGlu4-expressing HEK 293 cells). VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson's disease.
  • In Vitro
    VU0364770 is a selective positive allosteric modulator of mGlu4 in recombinant systems. VU0364770 is a potent PAM of multiple signaling pathways that enhances the response of the rat and human mGlu4 receptors to the endogenous agonist glutamate. VU0364770 produces a concentration-dependent potentiation of the response to an EC20 concentration of glutamate with EC50 of 1.1±0.2 μM and increases the maximal response to glutamate from 100 to 227±17%. Because of concerns that this chemical scaffold might possess activity at MAO, full IC50 determinations is performed for VU0364770 at the MAO-A and MAO-B isoforms; these studies result in Kis of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively. When tested at a 10 μM concentration at each mGlu receptor, VU0364770 exhibits weak PAM activity (4.3-fold left shift of the glutamate CRC) at mGlu6 and antagonist activity (3.3-fold right shift of the glutamate CRC) at mGlu5 (compare to the 16.5-fold left shift of the glutamate concentration-response for mGlu4 at 10 μM). When further evaluated in a full concentration-response curve format, VU0364770 exhibits antagonist activity at mGlu5 with a potency of 17.9±5.5 μM and PAM activity at mGlu6 with a potency of 6.8±1.7 μM (compare with the potency of VU0364770 on the rat mGlu4 receptor of 290±80 nM).
  • In Vivo
    VU0364770 exhibits suitable pharmacokinetic properties for systemic dosing in animal models. After intravenous administration, VU0364770 is rapidly clears from the systemic circulation (165 ml/min/kg) and exhibits a volume of distribution of 2.92 L/kg. VU0364770 is a highly protein-bound ligand displaying free fractions of 2.7 and 1.8% in human and rat plasma, respectively. VU0364770 also shows an improved pharmacokinetic profile relative to previously reported mGlu4 PAMs with enhanced central penetration and a total brain-to-plasma ratio of more than 1 after systemic administration of a 10 mg/kg dose. VU0364770 produces a dose-dependent reversal of haloperidol-induced catalepsy. VU0364770 dose-dependently reverses haloperidol (0.75 mg/kg)-induced catalepsy in rats, significant at doses of 10 to 56.6 mg/kg, after subcutaneous dosing (F6,69=8.04; p<0.001).
  • Synonyms
    VU0364770, VU 0364770, VU 0364770
  • Pathway
    Endocrinology/Hormones
  • Target
    Reductase
  • Recptor
    mGluR4
  • Research Area
    Neurological Disease
  • Indication
    ——

Chemical Information

  • CAS Number
    61350-00-3
  • Formula Weight
    232.67
  • Molecular Formula
    C12H9ClN2O
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : ≥ 100 mg/mL; 429.79 mM
  • SMILES
    c1ccnc(c1)C(=O)Nc1cc(ccc1)Cl
  • Chemical Name
    N-(3-Chlorophenyl)-2-pyridinecarboxamide

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Jones CK, et al. J Pharmacol Exp Ther, 2012, 340(2), 404-421.
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