A negative allosteric modulator of mGluR5
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Dipraglurant

Item No. 42535

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-fluoro-2-[4-(2-pyridinyl)-3-butyn-1-yl]-imidazo[1,2-a]pyridine
CAS Number
872363-17-2
Synonyms
  • ADX-48621
Molecular Formula
C16H12FN3
Formula Weight
265.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Soluble: ≥10 mg/ml
SMILES
FC1=CN2C=C(CCC#CC3=NC=CC=C3)N=C2C=C1
InChi Code
InChI=1S/C16H12FN3/c17-13-8-9-16-19-15(12-20(16)11-13)7-2-1-5-14-6-3-4-10-18-14/h3-4,6,8-12H,2,7H2
InChi Key
LZXMUJCJAWVHPZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    1 mg

    $72

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    5 mg

    $323

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    10 mg

    $466

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    25 mg

    $805

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    Product Description

    Dipraglurant is a negative allosteric modulator (NAM) of metabotropic glutamate receptor 5 (mGluR5; Ki = 21 nM).1 It inhibits glutamate-induced calcium mobilization, inositol monophosphate (IP1) accumulation, and ERK1/2 phosphorylation in HEK293A cells expressing rat mGluR5a (pKBs = 5.83, 6.5, and 6.67, respectively). Dipraglurant increases drinking in the Vogel punished drinking task, indicating anxiolytic-like activity, in rats, decreases marble burying in mice, and reduces immobility time in the forced swim test in mice (ED50s = 7.4, 43, and ~30 mg/kg, respectively).2 It reduces chorea and dystonia scores in a macaque model of MPTP-induced Parkinson’s disease L-DOPA-induced dyskinesia (PD-LID) when administered at a dose of 30 mg/kg.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Arsova, A., Møller, T.C., Vedel, L., et al. Detailed in vitro pharmacological characterization of clinically tested negative allosteric modulators of the metabotropic glutamate receptor 5. Mol. Pharmacol. 98(1), 49-60 (2020).

    2. Epping-Jordan, M.P., Girard, F., Bessis, A.S., et al. Effect of the metabotropic glutamate receptor type 5 negative allosteric modulator dipraglurant on motor and non-motor symptoms of Parkinson’s disease. Cells 12(7), 1004 (2023).

    3. Bezard, E., Pioli, E.Y., Li, Q., et al. The mGluR5 negative allosteric modulator dipraglurant reduces dyskinesia in the MPTP macaque model. Mov. Disord. 29(8), 1074-1079 (2014).