Biological Activity
A selective mGlu1a receptor antagonist, with an IC50 value of 8.8 μM for blockade of quisqualate-induced phosphoinositide hydrolysis vs. > 100 μM for mGlu5a, and negligible action on group II and III receptors. Also available as part of the Group I mGlu Receptor Tocriset™.
Licensing Information
Sold with the permission of Eli Lilly and Company
Technical Data
| M. Wt | 209.2 |
| Formula | C10H11NO4 |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 198419-91-9 |
| PubChem ID | 5311261 |
| InChI Key | SGIKDIUCJAUSRD-QMMMGPOBSA-N |
| Smiles | N[C@H](C(O)=O)C1=C(C)C=C(C(O)=O)C=C1 |
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 | 1.05 | 5mM with gentle warming | |
| 1.1eq. NaOH | 20.92 | 100 | |
| DMSO | 2.09 | 10mM with gentle warming | |
| water | 1.05 | 5mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 209.2. 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 | 4.78 mL | 23.9 mL | 47.8 mL |
| 5 mM | 0.96 mL | 4.78 mL | 9.56 mL |
| 10 mM | 0.48 mL | 2.39 mL | 4.78 mL |
| 50 mM | 0.1 mL | 0.48 mL | 0.96 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Bruno et al (1999) Neuroprotective activity of the potent and selective mGlu1a metabotropic glutamate receptor antagonist, (+)-2-methyl-4 carboxyphenylglycine (LY367385): comparison with LY357366, a broader spectrum antagonist with equal affinity for mGlu1a and mGlu5 recept Neuropharmacology 38 199 PMID: 10218860
Chapman et al (1999) Anticonvulsant actions of LY 367385 ((+)-methyl-4-carboxyphenylglycine), and AIDA ((RS)-1-aminoindan-1,5-dicarboxylic acid). Eur.J.Pharmacol. 368 17 PMID: 10096765
Salt and Turner (1998) Reduction of sensory and metabotropic glutamate receptor responses in the thalamus by the novel metabotropic glutamate receptor-1-selective antagonist S-2-methyl-4-carboxy-phenylglycine. Neuroscience 85 655 PMID: 9639261
Clark et al (1997) (+)-2-Methyl-4-carboxyphenylglycine (LY 367385) selectively antagonises metabotropic glutamate mGluR1 receptors. Bioorg.Med.Chem.Lett. 7 2777 PMID:
Keywords: LY 367385, supplier, Selective, mGlu1a, mGluR1a, antagonist, Group, I, Receptors, Glutamate, Metabotropic, LY367385, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience
