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DM-PPP

CHEMBL232052, GTPL1383, BDBM50204428

A Selective Antagonist of mGluR1 Receptors

Cat #: D-255
Alternative Name CHEMBL232052, GTPL1383, BDBM50204428
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 309.19
    Purity: >97%
    Effective concentration 1 nM – 1 µM.
    Structure
    Chemical name 4-O-[(2S)-3,3-dimethylbutan-2-yl] 2-O-propyl 3,5-dimethyl-1H-pyrrole-2,4-dicarboxylate.
    Molecular formula C17H27NO4.
    Activity DM-PPP is a selective and non-competitive antagonist of mGluR1 receptors. It inhibits the receptor in CHO cells with an IC50 of 15.8 nM1.
    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 100 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions -20°C.
    Our bioassay
    • Alomone Labs DM-PPP inhibits mGluR1 mediated Ca2+ mobilization in U2OS cells.
      Alomone Labs DM-PPP inhibits mGluR1 mediated Ca2+ mobilization in U2OS cells.
      Dose response of normalized inhibition of human mGluR1 mediated, L-Glutamate evoked Ca2+ mobilization by DM-PPP (#D-255). IC50 was determined at 144 nM. hmGluR1-expressing cells were loaded with Ca2+-sensitive dye, incubated with different concentrations of DM-PPP, 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. Micheli, F. et al. (2003) Bioorg. Med. Chem. 11, 171.
    2. Eom, H.S. et al. (2016) PLoS One 11, e0147538.
    Scientific background

    DM-PPP is a synthetic compound that acts as a selective and non-competitive antagonist of mGluR1 receptors with an IC50 value of 15.8 nM1. The compound interacts with the 7 transmembrane (7TM) domain of the receptor. In several animal models DM-PPP shows antinociceptive properties1.

    Metabotropic glutamate receptors (mGluRs) are G-protein coupled receptors (GPCR) 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 expressed on post-synaptic neurons and are known to affect the fate of neuronal progenitor cells and neural stem cell and the formation of the hippocampus2.

    Target mGluR1
    Lyophilized Powder
    Last update: 12/08/2021

    DM-PPP (#D-255) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use

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