Biological Activity
Potent and highly selective kainate receptor agonist, with an IC50 for inhibition of [3H]-kainate binding of 35 nM and almost 3,000- and 200-fold selectivity for kainate receptors over AMPA and NMDA receptors respectively. Also selectively inhibits the cloned excitatory amino acid transporter EAAT2 at higher concentrations. Also available as part of the Excitatory Amino Acid Transporter Inhibitor Tocriset™ and Kainate Receptor Tocriset™.
Licensing Information
Sold with the permission of Annovis Inc.
Technical Data
| M. Wt | 161.16 |
| Formula | C6H11NO4 |
| Storage | Store at RT |
| Purity | ≥97% (HPLC) |
| CAS Number | 31137-74-3 |
| PubChem ID | 95883 |
| InChI Key | KRKRAOXTGDJWNI-DMTCNVIQSA-N |
| Smiles | [H][C@@](N)(C(O)=O)C[C@]([H])([C@](O)=O)C |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| phosphate buffered saline | 8.06 | 50 | |
| 1eq. NaOH | 16.12 | 100 | |
| water | 8.06 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 161.16. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 6.21 mL | 31.03 mL | 62.05 mL |
| 5 mM | 1.24 mL | 6.21 mL | 12.41 mL |
| 10 mM | 0.62 mL | 3.1 mL | 6.21 mL |
| 50 mM | 0.12 mL | 0.62 mL | 1.24 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Donevan et al (1998) The methylglutamate, SYM 2081, is a potent and highly selective agonist at kainate receptors. J.Pharmacol.Exp.Ther. 285 539 PMID: 9580595
Jones et al (1997) Desensitization of kainate receptors by kainate, glutamate and diastereomers of 4-methylglutamate. Neuropharmacology 36 853 PMID: 9225313
Savidge et al (1999) Characterisation of kainate receptor mediated whole-cell currents in rat cultured cerebellar granule cells. Neuropharmacology 38 375 PMID: 10219975
Zhou et al (1997) (2S,4R)-4-Methylglutamic acid (SYM 2081): a selective, high affinity ligand for kainate receptors. J.Pharmacol.Exp.Ther. 280 422 PMID: 8996224
Keywords: SYM 2081, supplier, inhibitors, inhibits, EAAT2, kainate, receptors, agonist, selective, EAAT, Excitatory, Amino, Acid, Transporters, GLT-1, Glutamate, Monoamine, Neurotransmitter, iGluR, Ionotropic, SYM2081, Glutamate, Transporters, Kainate, Receptors, Kainate, Receptors, Tocris Bioscience
