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Submit ReviewLY 487379 hydrochloride is a 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.
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 48.89 | 100 | |
ethanol | 24.45 | 50 |
The following data is based on the product molecular weight 488.91. Batch specific molecular weights may vary from batch to batch due to the degree 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 |
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for LY 487379 hydrochloride, please let us know.
View all Glutamate (Metabotropic) Group II Receptor Modulators
Keywords: LY 487379 hydrochloride, LY 487379 hydrochloride supplier, Positive, allosteric, modulators, pam, selective, mGlu2, mGluR2, mGlur, Group, II, Receptors, Glutamate, Metabotropic, LY487379, hydrochloride, (Metabotropic), 3283, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for LY 487379 hydrochloride include:
Scholler (2017) Allosteric nanobodies uncover a role of hippocampal mGlu2 receptor homodimers in contextual fear consolidation. Nat Commun 8 1967 PMID: 29213077
Motolese et al (2015) Targeting type-2 metabotropic glutamate receptors to protect vulnerable hippocampal neurons against ischemic damage. Neuropharmacology 8 66 PMID: 26496940
Copeland et al (2015) Neuronal activity patterns in the mediodorsal thalamus and related cognitive circuits are modulated by metabotropic glutamate receptors. Nat Commun 92 16 PMID: 25576798
Yin et al (2014) Selective actions of novel allosteric modulators reveal functional heteromers of metabotropic glutamate receptors in the CNS. J Neurosci 34 79 PMID: 24381270
Do you know of a great paper that uses LY 487379 hydrochloride from Tocris? Please let us know.
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