Biological Activity
Positive allosteric modulator selective for mGlu2 receptors. Potentiates glutamate-stimulated [35S]GTPγS binding (EC50 values are 1.7 and > 10 μM for mGlu2 and mGlu3 receptors respectively). Devoid of any activity at mGlu5 and mGlu7 receptors. Promotes cognitive flexibility in a rat model.
Technical Data
| M. Wt | 488.91 |
| Formula | C21H19F3N2O4S.HCl |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 353229-59-1 |
| PubChem ID | 56972206 |
| InChI Key | LPWFRDWTOKLHJC-UHFFFAOYSA-N |
| Smiles | O=S(N(CC3=CC=CN=C3)C1=CC=C(OC2=CC=CC=C2OC)C=C1)(CC(F)(F)F)=O.Cl |
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 | |||
| DMSO | 48.89 | 100 | |
| ethanol | 24.45 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 488.91. 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 | 2.05 mL | 10.23 mL | 20.45 mL |
| 5 mM | 0.41 mL | 2.05 mL | 4.09 mL |
| 10 mM | 0.2 mL | 1.02 mL | 2.05 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.41 mL |
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References
References are publications that support the products' biological activity.
Johnson et al (2003) Discovery of allosteric potentiators for the metabotropic glutamate 2 receptor: synthesis and subtype selectivity of N-(4-(2-methoxyphenoxy)phenyl)-N-(2,2,-trifluoroethylsulfonyl)pyrid-3-ylmethyl-amine. J.Med.Chem. 46 3189 PMID: 12852748
Schaffhauser et al (2003) Pharmacological characterization and identification of amino acids involved in the positive modulation of metabotropic glutamate receptor subtype 2. Mol.Pharmacol. 64 798 PMID: 14500736
Poisik et al (2005) Metabotropic glutamate receptor 2 modulates excitatory synaptic transmission in the rat globus pallidus. Neuropharmacology 49 57 PMID: 15993439
Nikiforuk et al (2010) Effects of a positive allosteric modulator of group II metabotropic glutamate receptors, LY487379, on cognitive flexibility and impulsive-like responding in rats. J.Pharmacol.Exp.Ther. 335 665 PMID: 20739457
Keywords: LY 487379 hydrochloride, supplier, Positive, allosteric, modulators, pam, selective, mGlu2, mGluR2, mGlur, Group, II, Receptors, Glutamate, Metabotropic, LY487379, hydrochloride, Glutamate, (Metabotropic), Group, II, Receptors, Glutamate, (Metabotropic), Group, II, Receptors, Tocris Bioscience
