A-850002

CHEMBL223869, GTPL6355, SCHEMBL6102967, BDBM50177062
A Selective and Potent Antagonist of mGluR1 Receptors
    Cat #: A-390
    Alternative Name CHEMBL223869, GTPL6355, SCHEMBL6102967, BDBM50177062
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 336.41
    Purity: >99%
    Effective concentration 1 nM – 1 µM.
    Structure
    • A-850002
    Chemical name 9-(dimethylamino)-3-(4-methylphenyl)pyrido[2,3]thieno[2,4-d]pyrimidin-4-one.
    Molecular formula C18H16N4OS.
    PubChem CID 11515548
    Activity A-850002 inhibits mGluR1 in rat primary cerebellar granule neurons with an IC50 of 27 nM1 and human mGluR1 expressed in 1321N1 cells with an IC50 of 43 nM2.
    References-Activity
    1. Zhu, C.Z. et al. (2008) Eur. J. Pharmacol. 580, 314.
    2. Zheng, G.Z. et al. (2005) J. Med. Chem. 48, 7374.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility Up to 25 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions -20°C.
    Our bioassay
    • A-850002
      Alomone Labs A-850002 inhibits mGluR1 mediated Ca2+ mobilization in U2OS cells.
      Dose-response of normalized inhibition of human mGluR1 mediated, L-glutamate evoked Ca2+ mobilization by A-850002 (#A-390). IC50 was determined at 253 nM. hmGluR1-expressing cells were loaded with calcium-sensitive dye, incubated with a range of concentrations of A-850002, and stimulated by 15 µM L-glutamate (EC80). Changes in intracellular Ca2+ following stimulation were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™.
    References - Scientific background
    1. Zhu, C.Z. et al. (2008) Eur. J. Pharmacol. 580, 314.
    2. Zheng, G.Z. et al. (2005) J. Med. Chem. 48, 7374.
    3. Eom, H.S. et al. (2016) PLoS One 11, e0147538.
    Scientific background

    A-850002 is a synthetic, selective and potent antagonist of mGluR1 receptors. It inhibits mGluR1 receptors in rat primary cerebellar granule neurons with an IC50 value of 27 nM in calcium mobilization assays and human mGluR1 receptors expressed in 1321N1 type cells with an IC50 of 43 nM1,2.

    Metabotropic glutamate receptors (mGluRs) are G-protein coupled receptors that play an important role in synaptic plasticity and other neuro-physiological and pathological processes including a major role in central sensitization and neuropathic pain. Type 1 mGluRs are mainly found on post-synaptic neurons and are known to affect the fate of neuronal progenitor cells, neural stem cells and the formation of the hippocampus3.

    Target mGluR1 receptor
    Last update: 24/01/2020

    A-850002 (#A-390) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use

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    Scientific Background

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    Citations
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