Gavestinel

Name: Gavestinel
Brand: Tocris Bioscience
SKU: 2348

Tocris Bioscience, part of Bio-Techne | Catalog # 2348

Citations (6)

COA / SDS

Potent and selective NMDA antagonist; acts at the glycine site

Key Product Details

Description:	Potent and selective NMDA antagonist; acts at the glycine site
Alternative Names:	GV 150526A
Chemical Name:	4,6-Dichloro-3-[(1E)-3-oxo-3-(phenylamino)-1-propenyl]-1H-indole-2-carboxylic acid sodium salt
Purity:	≥98% (HPLC)
Molecular Weight:	397.19

View Full Technical Details for Gavestinel

Technical Data
Citations

Biological Activity for Gavestinel

Gavestinel is a highly potent and selective non-competitive antagonist acting at the strychnine-insensitive glycine binding site of the NMDA receptor-channel complex (K_d = 0.8 nM). Displays > 1000-fold selectivity over NMDA, AMPA and kainate binding sites. Orally bioavailable and active in vivo.

Licensing Information

Sold with the permission of GlaxoSmithKline

Compound Libraries for Gavestinel

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

Technical Data for Gavestinel

M. Wt	397.19
Formula	C₁₈H₁₁Cl₂N₂O₃Na
Storage	Desiccate at RT
Purity	≥98% (HPLC)
CAS Number	153436-38-5
PubChem ID	16759177
InChi Key	GRSDSTMFQHAESM-UHDJGPCESA-M
Smiles	[Na+].[O-]C(=O)C1=C(\C=C\C(=O)NC2=CC=CC=C2)C2=C(N1)C=C(Cl)C=C2Cl

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 Gavestinel

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	15.89	40

Preparing Stock Solutions for Gavestinel

The following data is based on the product molecular weight 397.19.

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
0.4 mM	6.29 mL	31.47 mL	62.94 mL
2 mM	1.26 mL	6.29 mL	12.59 mL
4 mM	0.63 mL	3.15 mL	6.29 mL
20 mM	0.13 mL	0.63 mL	1.26 mL

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References for Gavestinel

References are publications that support the biological activity of the product.

Mugnaini Receptor binding characteristics of the novel NMDA receptor glycine site antagonist [³H]GV150526A in rat cerebral cortical membranes. Eur.J.Pharmacol. 2000 PMID: 10729363
Kajbaf Pharmacokinetics, metabolism and excretion of the glycine antagonist GV150526A in rat and dog. Xenobiotica. 2003 PMID: 12745876
Di Fabio Substituted indole-2-carboxylates as in vivo potent antagonists acting at the strychnine-insensitive glycine binding site. J.Med.Chem. 1997 PMID: 9083472