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A Selective, Non-Competitive Antagonist of mGluR1 Receptors

Cat #: C-370
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 247.25
    Purity: >98%
    Effective concentration 10-200 µM.
    Chemical name Ethyl (7Z)-7-hydroxyimino-1,7a-dihydrocyclopropa[b]chromene-1a-carboxylate.
    Molecular formula C13H13NO4.
    CAS No.: 179067-99-3
    PubChem CID 6324610
    Activity CPCCOEt is a selective, non-competitive antagonist of mGluR1 receptors, inhibiting hmGluR1b with IC50 of 6.5 µM, whilst having no effect at 100 µM on a range of other receptor subtypes1. It was shown to inhibit synaptic activation of mGluR1 in Purkinje cell cerebellar slices with IC50 of 37µM2.
    1. Litschig, S. et al. (1999) Mol. Pharmacol. 55, 453.
    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. 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 CPCCOEt inhibits mGluR1-mediated Ca2+ mobilization in U2OS cells.
      Alomone Labs CPCCOEt inhibits mGluR1-mediated Ca2+ mobilization in U2OS cells.
      Dose-response of CPCCOEt (#C-370) normalized inhibition of human mGluR1-mediated, L-glutamate-evoked Ca2+ mobilization. hmGluR1-expressing cells were loaded with calcium-sensitive dye, incubated with varying CPCCOEt concentrations, and stimulated by 5 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. Litschig, S. et al. (1999) Mol. Pharmacol. 55, 453.
    2. Fukunaga, I. et al. (2007) Br. J. Pharmacol. 151, 870.
    Scientific background

    CPCCOEt is a compound that acts as a selective, non-competitive antagonist of mGluR1. It can inhibit mGluR1 signaling without affecting glutamate binding1. CPCCOEt selectively inhibits mGluR1b-induced increases in intracellular calcium and demonstrates IC50 of 6.5 µM1.

    Glutamate is the most abundant excitatory neurotransmitter in the central nervous system. It modulates the activity of many types of synapses by activating metabotropic glutamate receptors (mGluRs), members of the G-protein coupled receptor (GPCR) superfamily. These receptors are divided into three groups based on sequence homology with a total of eight subtypes, mGluR1 to mGluR8.

    mGluR1 from group I, plays an important role in the central sensitization of pain and in a variety of physiological functions including regulation of ion channels, synaptic transmission, and plasticity1,2.

    Target mGluR1
    Last update: 06/11/2022

    CPCCOEt (#C-370) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use



    Scientific Background

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