Gavestinel
Tocris Bioscience, part of Bio-Techne | Catalog # 2348
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
Product Description
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 GlaxoSmithKlineProduct Specifications
Molecular Weight
397.19
Formula
C18H11Cl2N2O3Na
Storage
Desiccate at RT
Purity
≥98% (HPLC)
Chemical Name
4,6-Dichloro-3-[(1E)-3-oxo-3-(phenylamino)-1-propenyl]-1H-indole-2-carboxylic acid sodium salt
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for Gavestinel
For research use only
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