GYKI 52466 dihydrochloride
Tocris Bioscience | Catalog # 1454
Key Product Details
Description
Product Description
GYKI 52466 dihydrochloride is a selective noncompetitive AMPA receptor antagonist (IC50 values are 10-20, ~ 450 and >50 μM for AMPA-, kainate- and NMDA-induced responses respectively). Skeletal muscle relaxant and orally-active anticonvulsant. Has anti-proliferative effects in transformed cells.
Product Specifications for GYKI 52466 dihydrochloride
Molecular Weight
Formula
Storage
Purity
Chemical Name
CAS Number
PubChem ID
InChI Key
SMILES
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 3.3 | 10 | |
| DMSO | 16.49 | 50 |
Preparing Stock Solutions for GYKI 52466 dihydrochloride
The following data is based on the product molecular weight 366.24.
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 5.46 mL | 27.30 mL | 54.61 mL |
| 2.5 mM | 1.09 mL | 5.46 mL | 10.92 mL |
| 5 mM | 0.55 mL | 2.73 mL | 5.46 mL |
| 25 mM | 0.11 mL | 0.55 mL | 1.09 mL |
Calculators
Background References
References are publications that support the biological activity of the product. See our Citations tab to view 12 publications citing the usage of this product.
- Tarnawa Electrophysiological studies with a 2,3-benzodiazepine muscle relaxant: GYKI 52466. Eur.J.Pharmacol. 1989 PMID: 2574112
- Szabados Comparison of anticonvulsive and acute neuroprotective activity of three 2,3-benzodiazepine compounds, GYKI 52466, GYKI 53405, and GYKI 53655. Brain Res.Bull. 2001 PMID: 11489346
- Paternain Selective antagonism of AMPA receptors unmasks kainate receptor-mediated responses in hippocampal neurons. Neuron 1995 PMID: 7826635
- Rzeski Glutamate antagonists limit tumor growth. Proc.Natl.Acad.Sci.USA 2001 PMID: 11331750
- Donevan and Rogawsk GYKI 52466, a 2,3-benzodiazepine, is a highly selective, non-competitive antagonist of AMPA/kainate receptor responses. Neuron 1993 PMID: 7678966
Product Documents for GYKI 52466 dihydrochloride
Certificate of Analysis
To download a Certificate of Analysis, please enter a lot or batch number in the search box below.
Product Specific Notices for GYKI 52466 dihydrochloride
For research use only
Citations for GYKI 52466 dihydrochloride
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Customer Images
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Species: RatAssay Type: In VitroCell Line/Tissue: Cultured rat motor neuronsVerified Customer | Posted 11/15/2021Preincubated 40 micromolar of GYKI 52466 for 10 minutes. The image shows the peak fluorescence intensity of fura2-am up on AMPA stimulation. GYKI 52466 efficiently inhibits AMPA receptor-mediated calcium influx.
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Assay Type: Ex VivoCell Line/Tissue: acute hippocampal brain sliceVerified Customer | Posted 08/21/2018We use GYKI 52466 dihydrochloride at 10uM to inhibit AMPA receptors during our electrophysiology experiments. This allows us to isolate and study the effects of manipulations on other glutamate receptors. In the set of experiments we used this product for we were examining Kainate receptor properties and so the GYKI was used in conjunction with an NMDAR antagonist.
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