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Submit ReviewHighly 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.
Sold with the permission of GlaxoSmithKline
Gavestinel is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 15.89 | 40 |
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 |
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
If you know of a relevant reference for Gavestinel, please let us know.
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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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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