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

Chemical Name:	4,6-Dichloro-3-[(1E)-3-oxo-3-(phenylamino)-1-propenyl]-1H-indole-2-carboxylic acid sodium salt
Purity:	≥98%
Molecular Weight:	397.19 kDa

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.

Technical Data for Gavestinel

M. Wt	397.19 kDa
Formula	C₁₈H₁₁Cl₂N₂O₃Na
Storage	Desiccate at RT
Purity	≥98%
CAS Number	153436-38-5

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

Solubility

Soluble Soluble to 40 mM in DMSO

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References for Gavestinel

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

Di Fabio et al. Substituted indole-2-carboxylates as in vivo potent antagonists acting at the strychnine-insensitive glycine binding site. J.Med.Chem., 1997;40:841 PMID: 9083472
Mugnaini et al. Receptor binding characteristics of the novel NMDA receptor glycine site antagonist [³H]GV150526A in rat cerebral cortical membranes. Eur.J.Pharmacol., 2000;391:233 PMID: 10729363
Kajbaf et al. Pharmacokinetics, metabolism and excretion of the glycine antagonist GV150526A in rat and dog. Xenobiotica., 2003;33:415 PMID: 12745876