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MPX-004

A Potent and Selective Antagonist of GluN2A-containing NMDA Receptors

Cat #: M-280
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 455.91
    Purity: >99% (HPLC)
    Effective concentration 0.1-10 µM.
    Structure
    Chemical name (5-(((3-chloro-4-fluoropheyl)sulfonamido)methyl)-N-((2-methylthiazol-5-yl)methyl)pyrazine-2-carboxamide).
    Molecular formula C17H15ClFN5O3S2.
    Activity A novel pyrazine-containing NMDA receptor antagonist, highly selective for NR2A-containing receptors (IC50 = 79 nM in HEK cells) over NR2B and NR2D1.
    References-Activity
    1. Volkmann, R.A. et al. (2016) PLoS ONE 11, e0148129.
    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 DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs MPX-004 inhibits NMDA receptor channels expressed in Xenopus oocytes. 
      Alomone Labs MPX-004 inhibits NMDA receptor channels expressed in Xenopus oocytes. 
      A. Time course of NR1/NR2A currents, elicited by transient stimulations with 200 µM glutamate and 200 µM glycine every 100 sec, while membrane potential was held at -80 mV. 100 nM MPX-004 (#M-280), applied for 7 min (bar), significantly inhibits current amplitude. B. Superimposed current traces from the recording shown in A, upon application of control and of 100 nM MPX-004 (as indicated).
    References - Scientific background
    1. Volkmann, R.A. et al. (2016) PLoS ONE 11, e0148129.
    2. Cercato, M.C. et al. (2017) Front. Behav. Neurosci. 10, 242.
    Scientific background

    MPX-004 is a synthetic compound that acts as a potent and selective GluN2A-containing NMDA receptor antagonist with an IC50 value of 79 nM in HEK cells1.

    MPX-004 is a pyrazine-containing antagonist with optimal halogen substituents on the phenylsulfonamide aryl ring. It is used as a pharmacological tool for studying the physiology of NMDA receptors containing the GluN2A subunit1.

    NMDA receptors are heterotetramers composed by 2 GluN1 obligatory subunits and 2 GluN2 (A-D) or GluN3 (A-B) regulatory subunits. GluN2A is the most abundant subunit in the mammalian CNS. Physiological and genetic evidence show that GluN2A-containing receptors are involved in autism, schizophrenia, childhood epilepsy and neurodevelopmental disorders such as Rett Syndrome1,2.

    Target GluN2A-containing NMDA receptors
    Lyophilized Powder
    Last update: 11/04/2021

    MPX-004 (#M-280) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use

    Applications

    Specifications

    Scientific Background

    Citations

    Citations
    Proliferation/survival/ cytotoxicity
    1. Mouse primary hippocampal neurons.
      Chan, K. et al. (2020) Nat. Commun. 11, 1403.

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