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5,7-Dichlorokynurenic acid monohydrate

An Antagonist of NMDA Receptors

Cat #: D-191
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 276.07
    Purity: >98%
    Form Lyophilized powder.
    Effective concentration 0.5-20 µM.
    Chemical name 5,7-dichloro-4-oxo-1H-quinoline-2-carboxylic acid; hydrate.
    Molecular formula C10H7Cl2NO4.
    CAS No.: 190908-40-8
    PubChem CID 23723057
    Activity 5,7-Dichlorokynurenic acid is an NMDA receptor antagonist acting at the glycine site1.
    1. Baron, B.M. et al. (1990) Mol. Pharmacol. 38, 554.
    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 200 mM in DMSO. Centrifuge all product preparations before use (10000 x g for 1 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs 5, 7-Dichlorokynurenic acid nonohydrate inhibits NMDA (NR1+NR2A) channels expressed in Xenopus oocytes. 
      Alomone Labs 5, 7-Dichlorokynurenic acid nonohydrate inhibits NMDA (NR1+NR2A) channels expressed in Xenopus oocytes. 
      A. Time course of NMDA currents that were elicited by stimulation with 10 µM glutamate and 10 µM Glycine, every 50 sec, while membrane potential was held at -80 mV. 5 and 20 µM 5, 7-Dichlorokynurenic acid monohydrate (#D-191), applied for 2.5 min each, as indicated, inhibited the current amplitude in a reversible manner. B. superimposed current traces taken from the experiment described in A.
    References - Scientific background
    1. Baron, B.M. et al. (1990) Mol. Pharmacol. 38, 554.
    2. Kvist, T. et al. (2013) Neuropharmacology 75, 324.
    3. Black, S.A. et al. (2014) Front. Cell. Dev. Biol. 2, 45.
    4. Baron, B.M. et al. (1991) Eur. J. Pharmacol. 206, 149.
    Scientific background

    5,7-Dichlorokynurenic acid (5,7-DCKA), is a derivative of kynurenic acid, an extremely potent excitatory amino acid receptor antagonist of N-methyl-D-aspartate (NMDA) receptors. 5,7-DCKA binds with high affinity to a strychnine-insensitive glycine binding site located on the NMDA receptor. This site is considered to be used as a therapeutic target for acute focal ischemia. The compound exhibits strong selectivity for binding to GluN1 subunit over GluN3A1,2 with an IC50 value of 79 nM in rat cortical and hippocampal membranes4.

    Small concentrations of 5,7-DCKA have the ability to inhibit several processes including NMDA-stimulated elevation of cytosolic calcium in cultured hippocampal neurons, cGMP accumulation in cerebellar slices, and norepinephrine release from hippocampal regions1.

    Several different studies have demonstrated potent anticonvulsant features of 5,7-DCKA when the compound is administrated intra-cerebroventricularly directly to the brain1.

    NMDA receptors play an important role in a variety of cellular processes and brain functions such as synaptic plasticity, addiction and stroke. They mediate several physiological functions including learning and memory formation; they play a role in glutamate excitotoxicity and are involved in many neurodegenerative conditions including Alzheimer’s disease.

    Target NMDA receptors
    Last update: 06/11/2022

    5,7-Dichlorokynurenic acid monohydrate (#D-191) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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