GYKI 52466 dihydrochloride

Name: GYKI 52466 dihydrochloride
Brand: Tocris Bioscience
SKU: 1454
Rating: 5 (1 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 1454

(1)

Citations (8)

COA / SDS

Selective non-competitive AMPA antagonist

Key Product Details

Description:	Selective non-competitive AMPA antagonist
Chemical Name:	4-(8-Methyl-9H-1,3-dioxolo[4,5-h][2,3]benzodiazepin-5-yl)-benzenamine dihydrochloride
Purity:	≥98% (HPLC)
Molecular Weight:	366.24

View Full Technical Details for GYKI 52466 dihydrochloride

Technical Data
Citations / Reviews (1)

Biological Activity for GYKI 52466 dihydrochloride

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.

Compound Libraries for GYKI 52466 dihydrochloride

GYKI 52466 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for GYKI 52466 dihydrochloride

M. Wt	366.24
Formula	C₁₇H₁₅N₃O₂.2HCl
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	2319722-40-0
PubChem ID	10042240
InChi Key	RUBSCPARMVJNKX-UHFFFAOYSA-N
Smiles	Cl.Cl.CC1=NN=C(C2=CC=C(N)C=C2)C2=C(C1)C=C1OCOC1=C2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for GYKI 52466 dihydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	16.49	50
	water	3.3	10

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 will 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

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References for GYKI 52466 dihydrochloride

References are publications that support the biological activity of the 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