MPX-004

A Potent and Selective Antagonist of GluN2A-containing NMDA Receptors
    Cat #: M-280
    Sizes: 5 mg, 10 mg, 25 mg, 50 mg
  • Lyophilized Powder
  • Bioassay Tested
  • Shipped at Room Temp.
  • Source: Synthetic
    MW: 455.91 Da.
    Purity >99%.
    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.
    Storage before reconstitution Product before reconstitution can be stored at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Reconstitution DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage after reconstitution 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. 
    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
    1. Volkmann, R.A. et al. (2016) PLoS ONE 11, e0148129.
    2. Cercato, M.C. et al. (2017) Front. Behav. Neurosci. 10, 242.
    Target: GluN2A-containing NMDA receptors
    Last update: 25/12/2017

    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.

    Alomone Labs is pleased to offer MPX-004 (#M-280).

    For research purposes only, not for human use