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
Datasheets
References
Biological Activity
Positive allosteric modulator of mGlu5 receptors (EC50 = 16 nM; Ki = 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
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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
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References
References are publications that support the products' biological activity.
Rodriguezet 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'Amoreet 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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