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Tocris/LY 487379 hydrochloride/3283/10/10 mg

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货号: 3283/10

品牌: Tocris

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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)

Biological Activity Technical Data Solubility Calculators Datasheets References

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

Product Datasheets

Certificate of Analysis / Product Datasheet

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

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

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