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DQP-1105

A Potent Noncompetitive Antagonist of GluN2D/C-Containing NMDA Receptors
Cat #: D-210
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 558.43
    Purity: >98%
    Effective concentration 1-20 µM.
    Structure
    Chemical name 4-[(3Z)-5-(4-bromophenyl)-3-(6-methyl-2-oxo-4-phenylquinolin-3-ylidene)pyrazolidin-1-yl]-4-oxobutanoic acid.
    Molecular formula C29H24BrN3O4.
    CAS No.: 380560-89-4.
    PubChem CID 6044308
    Activity DQP-1105 is a potent, noncompetitive NMDA receptor antagonist, exhibiting significant selectivity for NR2D and NR2C-containing receptors (IC50 = 2.7 µM and 8.5 µM, respectively) over NR2B and NR2A-containing receptors (IC50 = 121 µM and 206 µM, respectively)1.
    References-Activity
    1. Acker, T.M. et al. (2011) Mol. Pharmacol. 80, 782.
    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 up to 100 mM in DMSO. Centrifuge all products before handling (10000 x g 5 min).
    Storage of solutions Store at -20°C. It is recommended to prepare solutions afresh on the day of use, or aliquot stock solutions stored at -20°C to prevent repeated thawing and freezing.
    Our bioassay
    • Alomone Labs DQP-1105 inhibits NMDA receptor channels expressed in Xenopus oocytes.
      Alomone Labs DQP-1105 inhibits NMDA receptor channels expressed in Xenopus oocytes.
      A. Representative time course of NR1/NR2C currents, elicited by transient stimulations with 50 µM glutamate + 50 µM glycine every 50 sec, while membrane potential was held at -80 mV, and reversibly inhibited by 2 µM and 20 µM DQP-1105 (#D-210). B. Superimposed current traces from the recording shown in A, following application of control, 2 µM and 20 µM DQP-1105. Transient stimulation is indicated by an arrow.
    References - Scientific background
    1. Acker, T.M. et al. (2011) Mol. Pharmacol. 80, 782.
    2. Black, S.A. et al. (2014) Front. Cell. Dev. Biol. 2, 45.
    Scientific background

    DQP-1105 is a potent and noncompetitive antagonist of GluN2D and GluN2C-containing N-methyl-d-aspartate (NMDA) receptors displaying IC50 values of 2.7 µM and 8.5 µM towards NR2D and NR2C-containing receptors, respectively1. DQP-1105 exhibits significant selectivity towards these receptors over NR2B and NR2A-containing receptors. DQP-105 inhibits the pregating step without changing the stability of the open pore conformation.

    NMDA receptors are heterotetrameric channels formed by the assembly of two obligatory GluN1 and two GluN2/GluN3 subunits. They play an important role in a variety of cellular processes and brain functions such as synaptic plasticity, addiction and stroke. NMDA receptors mediate physiological functions such as learning and memory formation, glutamate excitotoxicity and are involved in many neurodegenerative conditions including Alzheimer’s disease2.

    Target GluN2D and GluN2C-containing NMDA receptors
    Last update: 23/08/2020

    DQP-1105 (#D-210) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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