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A-794278

An Antagonist of mGluR1 and mGluR5

Cat #: A-435
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 342.46
    Purity: >98%
    Effective concentration 1-100 nM.
    Structure
    Chemical name 3-cycloheptyl-9-(dimethylamino)pyrido[1,2]thieno[3,4-d]pyrimidin-4-one.
    Molecular formula C18H22N4OS.
    CAS No.: 869802-57-3
    PubChem CID 11537456
    Activity A-794278 is a potent and selective noncompetitive mGluR1 antagonist, acting on mGluR1 and mGluR5 with IC50 values of 4.1 nM and 147 nM, respectively1. In vivo it shows analgesic properties, significantly attenuating spontaneous post-operative pain behavior in rats (ED50 = 50 μmol/kg)2.
    References-Activity
    1. Zheng, G.Z. et al. (2005) J. Med. Chem. 48, 7374.
    2. Zhu, C.Z. et al. (2008) Eur. J. Pharmacol. 580, 314.
    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. Protect from light and moisture.
    Solubility Soluble in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions -20°C.
    Our bioassay
    • Alomone Labs A-794278 inhibits mGluR1-mediated Ca2+ mobilization in U2OS cells.
      Alomone Labs A-794278 inhibits mGluR1-mediated Ca2+ mobilization in U2OS cells.
      Dose-response of A-794278 (#A-435) normalized inhibition of human mGluR1-mediated, L-glutamate-evoked Ca2+ mobilization. Cells were loaded with calcium-sensitive dye, incubated with a range of A-794278 concentrations, and stimulated with 5 µM L-glutamate (EC80). Changes in intracellular Ca2+ following stimulation were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™. IC50 was determined at 4.16 nM.
    References - Scientific background
    1. Zheng, G.Z. et al. (2005) J. Med. Chem. 48, 7374.
    2. Zhu, C.Z. et al. (2008) Eur. J. Pharmacol. 580, 314.
    Scientific background

    A-794278 is a potent, non-competitive antagonist of mGluR1. It is a triazafluorenone derivative that also antagonizes mGluR5 receptors. It demonstrates IC50 values of 4.1 nM and 147 nM for mGluR1 and mGluR5, respectively1. A-794278 binds to a putative allosteric recognition site located within the seven-transmembrane domain of the receptor1,2.

    Glutamate is the most abundant excitatory neurotransmitter in the central nervous system. It modulates the activity of many types of synapses by activating in part metabotropic glutamate receptors (mGluRs). mGluRs consist of three groups: I, II, and III with a total of eight subtypes, mGluR1 to mGluR8. mGluR1 plays an important role in the central sensitization of pain and in a variety of functions with potential implications in neurological and psychiatric disorders1,2.

    Target mGluR1, mGluR5
    Lyophilized Powder
    Last update: 08/06/2021

    A-794278 (#A-435) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use
    Shipping and Ordering information

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