A negative allosteric modulator and inverse agonist of mGluR5
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MFZ 10-7

Item No. 42024

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-fluoro-5-[2-(6-methyl-2-pyridinyl)ethynyl]-benzonitrile
CAS Number
1224431-15-5
Molecular Formula
C15H9FN2
Formula Weight
236.2
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
N#CC1=CC(F)=CC(C#CC2=CC=CC(C)=N2)=C1
InChi Code
InChI=1S/C15H9FN2/c1-11-3-2-4-15(18-11)6-5-12-7-13(10-17)9-14(16)8-12/h2-4,7-9H,1H3
InChi Key
ZGEXQIMQZVRTDZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $159

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    10 mg

    $264

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    25 mg

    $572

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    Product Description

    MFZ 10-7 is a negative allosteric modulator (NAM) and inverse agonist of metabotropic glutamate receptor 5 (mGluR5).1 It selectively binds to mGluR5 (Ki = 0.67 nM) over a panel of 63 additional receptors and ion channels at 100 nM. MFZ 10-7 reduces D-myo-inositol 1 phosphate (1-IP1; Item No. 1000777) accumulation, a marker of D-myo-inositol-1,4,5-triphosphate (1,4,5-IP3; Item No. 10008205) production, in an ELISA-based immunocompetitive assay using HEK293A cells expressing rat mGluR5 (IC50 = 2.4 nM). In vivo, MFZ 10-7 (0.3 mg/kg) increases the number of transitions between the light and dark area in a light-dark exploration test, indicating anxiolytic-like activity, and increases locomotor activity in the open field test in mice. It inhibits cocaine self-administration in rats when administered at doses of 3 or 10 mg/kg.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Keck, T.M., Zou, M.F., Zhang, P., et al. Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation. ACS Med. Chem. Lett. 3(7), 544-549 (2012).

    2. Keck, T.M., Zou, M.-F., Bi, G.-H., et al. A novel mGluR5 antagonist, MFZ 10-7, inhibits cocaine-taking and cocaine-seeking behavior in rats. Addict. Biol. 19(2), 195-209 (2014).