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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)
Biological Activity
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
Gavestinel is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| 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
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 15.89 | 40 |
Preparing Stock Solutions
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
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
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