Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Donevanet al (1998) The methylglutamate, SYM 2081, is a potent and highly selective agonist at kainate receptors. J.Pharmacol.Exp.Ther. 285 539 PMID: 9580595
Joneset al (1997) Desensitization of kainate receptors by kainate, glutamate and diastereomers of 4-methylglutamate. Neuropharmacology 36 853 PMID: 9225313
Savidgeet al (1999) Characterisation of kainate receptor mediated whole-cell currents in rat cultured cerebellar granule cells. Neuropharmacology 38 375 PMID: 10219975
Zhouet 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