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DL-AP3

DL-2-Amino-3-phosphonopropionic acid

An Antagonist of mGluR1 Receptors

Cat #: D-275
Alternative Name DL-2-Amino-3-phosphonopropionic acid
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 169.07
    Purity: >97%
    Effective concentration 0.1-10 mM.
    Structure
    Chemical name 2-amino-3-phosphonopropanoic acid.
    Molecular formula C3H8NO5P.
    CAS No.: 5652-28-8
    PubChem CID 3857
    Activity DL-AP3 is a selective competitive antagonist of group I metabotropic glutamate receptors, at 1 mM suppressing mGluR1 response in an agonist dependent manner1.
    References-Activity
    1. Schoepp, D.D. et al. (1999) Neuropharmacology 38, 1431.
    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 Soluble in water, 1eq NaOH and aqueous buffers.
    Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions -20°C.
    Our bioassay
    • Alomone Labs DL-AP3 inhibits mGluR1-mediated Ca2+ mobilization in U2OS cells.
      Alomone Labs DL-AP3 inhibits mGluR1-mediated Ca2+ mobilization in U2OS cells.
      Dose-response of DL-AP3 (#D-275) normalized inhibition of human mGluR1-mediated, L-Glutamate-evoked Ca2+ mobilization. hmGluR1-expressing cells were loaded with calcium-sensitive dye, incubated with a range of DL-AP3 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 295 µM.
    References - Scientific background
    1. Schoepp, D.D. et al. (1999) Neuropharmacology 38, 1431.
    2. Hawkinson, J.E. et al. (1996) Eur. J. Pharmacol. 307, 219.
    3. Eom, H.S. et al. (2016) PLoS One 11, e0147538.
    Scientific background

    DL-AP3 is a racemic compound of 2-amino-3-phosphonopropionic acid that acts as a potent and competitive antagonist of mGluR1 receptors. It demonstrates an IC50 value of 1 mM for rat mGluR1 when challenged with glutamate2. DL-AP3 has neuroprotective effects in the gerbil model of global ischemia1,2.

    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), 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. Type 1 mGluRs are mainly detected on post-synaptic neurons and affect the fate of neuronal progenitor cells and neural stem cells, and are important for the formation of the hippocampus3.

    Target mGluR1
    Last update: 02/01/2022

    DL-AP3 (#D-275) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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