Overview
Cat #:
G-245
Purity: >98%
CAS No.: 732278-52-3
MW: 407.49
Form: Lyophilized
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
MW: 407.49
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.
For research purposes only, not for human use
Specifications
Properties
Technical Specifications
MW 407.49
Purity >98%
Molecular formula C21H21N5O2S.
CAS No. 732278-52-3
Source Synthetic
PubChem CID 10250827
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.
Biological Activity
Target AMPA receptors
Effective concentration 1-50 µM.
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
- Wang, C. et al. (2013) ACS Chem. Neurosci. 5, 138.
Solubility and Storage
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.
Applications
Our Bioassay
Our bioassay
- 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.
Last Update: 08/01/2025