Gavestinel

Pricing Availability   Qty
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)
Datasheet
Citations
Reviews
Literature (5)

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 (Kd = 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 Data for Gavestinel

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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.

Di Fabio et al (1997) Substituted indole-2-carboxylates as in vivo potent antagonists acting at the strychnine-insensitive glycine binding site. J.Med.Chem. 40 841 PMID: 9083472

Mugnaini et al (2000) Receptor binding characteristics of the novel NMDA receptor glycine site antagonist [3H]GV150526A in rat cerebral cortical membranes. Eur.J.Pharmacol. 391 233 PMID: 10729363

Kajbaf et al (2003) Pharmacokinetics, metabolism and excretion of the glycine antagonist GV150526A in rat and dog. Xenobiotica. 33 415 PMID: 12745876


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Keywords: Gavestinel, Gavestinel supplier, Potent, selective, glycine, site, antagonists, Orally, available, active, vivo, Glutamate, NMDA, Receptors, N-Methyl-D-Aspartate, iGluR, Ionotropic, GV150526A, GlaxoSmithKline, GSK, GV, 150526A, 2348, Tocris Bioscience

Citations for Gavestinel

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Literature in this Area

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