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GYKI 47409 (BDZ-g)

GYKI47409, (R)-5-(4-amino-3-methyl-phenyl)-8-methyl-7-(5-methyl-1,3,4-thiadiazol-2-yl)-8,9-dihydro-7H-1,3-dioxolo[4,5-h][2,3]benzodiazepine

An Antagonist of AMPA Receptors

Cat #: G-245
Alternative Name GYKI47409, (R)-5-(4-amino-3-methyl-phenyl)-8-methyl-7-(5-methyl-1,3,4-thiadiazol-2-yl)-8,9-dihydro-7H-1,3-dioxolo[4,5-h][2,3]benzodiazepine
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 407.49
    Purity: >98%
    Effective concentration 1-50 µM.
    Structure
    Chemical name 2-methyl-4-[(8~{R})-8-methyl-7-(5-methyl-1,3,4-thiadiazol-2-yl)-8,9-dihydro-[1,3]dioxolo[4,5-h][2,3]benzodiazepin-5-yl]aniline.
    Molecular formula C21H21N5O2S.
    CAS No.: 732278-52-3
    PubChem CID 10250827
    Activity GYKI 47409 (BDZ-g) is a potent and selective noncompetitive antagonist of AMPA glutamate receptors. GYKI 47409 (BDZ-g) was shown to act on both open-channel and closed-channel conformation, and to inhibit the homomeric channels, as well as the GluA2-containing AMPA receptor channels, with no significant activity on kainate and NMDA type glutamate receptors1.
    References-Activity
    1. Wang, C. et al. (2013) ACS Chem. Neurosci. 5, 138.
    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 DMSO. Centrifuge all products before handling (10000 x g 5 min).
    Storage of solutions Store at -20°C for several months. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.
    Our bioassay
    • Alomone Labs GYKI 47409 (BDZ-g) inhibits GluA1 channels expressed in Xenopus oocytes.
      Alomone Labs GYKI 47409 (BDZ-g) inhibits GluA1 channels expressed in Xenopus oocytes.
      Representative time course of GluA1 current, activated by a continuous application (top dotted line) of 5 µM (S)-AMPA (#A-267), and inhibited by 1 µM and 10 µM GYKI 47409 (BDZ-g) (#G-245), as indicated (bars), at a holding potential of -80 mV.
    References - Scientific background
    1. Wang, C. et al. (2013) ACS Chem. Neurosci. 5, 138.
    2. Chizh, B.A. et al. (1994) Br. J. Pharmacol. 112, 843.
    Scientific background

    GYKI 47409 (BDZ-g) is a potent and selective AMPA receptor antagonist and binds to a noncompetitive site of the receptor. GYKI 47409 inhibits the open channel and the closed-channel conformations of AMPA receptors1.

    AMPA receptors are the primary receptors mediating fast excitatory neurotransmission in the mammalian central nervous system. This function is essential for synaptic plasticity, learning and memory1,2.

    Target AMPA receptors
    Lyophilized Powder
    Last update: 02/01/2022

    GYKI 47409 (BDZ-g) (#G-245) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use
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