Description: Positive allosteric modulator at mGlu₅ Chemical Name: N-Cyclobutyl-6-[2-(3-fluorophenyl)ethynyl]-3-pyridinecarboxamide hydrochloride Purity: ≥98% (HPLC) Biological Activity Technical Data Solubility Calculators DatasheetsReferences

Biological Activity

Positive allosteric modulator of mGlu₅ receptors (EC₅₀ = 16 nM; K_i = 195 nM). Selective for mGlu₅; displays no significant activity at mGlu₁, mGlu₂ or mGlu₄ receptors. Exhibits antipsychotic-like activity in a rodent model. Also reduces spontaneous spike and wave discharges without affecting motor behaviour in a rat model of absence epilepsy.

Compound Libraries

VU 0360172 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	330.78
Formula	C18H15FN2O.HCl
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	1309976-62-2
PubChem ID	53384852
InChI Key	NBGAPTWZQXSEAA-UHFFFAOYSA-N
Smiles	FC1=CC=CC(C#CC2=CC=C(C(NC3CCC3)=O)C=N2)=C1.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	16.54	50
ethanol	8.27	25

Preparing Stock Solutions

The following data is based on the product molecular weight 330.78. 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	3.02 mL	15.12 mL	30.23 mL
5 mM	0.6 mL	3.02 mL	6.05 mL
10 mM	0.3 mL	1.51 mL	3.02 mL
50 mM	0.06 mL	0.3 mL	0.6 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet Safety Datasheet Select another language: English German French Spanish View SDS

References

References are publications that support the products\' biological activity.

Rodriguez et al (2010) Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity. Mol.Pharmacol. 78 1105 PMID: 20923853

D\'Amore et al (2013) Potentiation of mGlu₅ receptors with the novel enhancer, VU0360172, reduces spontaneous absence seizures in WAG/Rij rats. Neuropharmacology 66 330 PMID: 22705340

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