LY 487379 hydrochloride

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Cat.No. 3283 - LY 487379 hydrochloride | C21H19F3N2O4S.HCl | CAS No. 353229-59-1
Description: Positive allosteric modulator selective for mGlu2
Chemical Name: 2,2,2-Trifluoro-N-[4-(2-methoxyphenoxy)phenyl]-N-(3-pyridinylmethyl)ethanesulfonamide hydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (3)
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

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


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View Related Products by Product Action

View all Glutamate (Metabotropic) Group II Receptor Modulators

Keywords: Positive allosteric modulators pam selective mGlu2 mGluR2 mGlur Group II Receptors Glutamate Metabotropic LY487379 hydrochloride Glutamate (Metabotropic) Group II Receptors

3 Citations for LY 487379 hydrochloride

Citations are publications that use Tocris products. Selected citations for LY 487379 hydrochloride include:

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? If so please let us know.

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Literature in this Area

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