Description: Negative allosteric modulator at mGlu5
Chemical Name: 3-Fluoro-5-[2-(6-methyl-2-pyridinyl)ethynyl]benzonitrile hydrochloride
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
High affinity negative allosteric modulator at the mGlu5 receptor (Ki = 0.67 nM). Potently inhibits mGlu5 glutamate-mediated calcium mobilization (IC50 = 1.22 nM). Inhibits cocaine-taking and cocaine-seeking behavior in rats.
Technical Data
M. Wt
272.7
Formula
C15H9FN2.HCl
Storage
Store at +4°C
Purity
≥99% (HPLC)
CAS Number
1224431-15-5
PubChem ID
90488944
InChI Key
WRHOKQFFLQKKNL-UHFFFAOYSA-N
Smiles
CC1=NC(C#CC2=CC(C#N)=CC(F)=C2)=CC=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
27.27
100
ethanol
27.27
100
Preparing Stock Solutions
The following data is based on the product molecular weight 272.7. 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
3.67 mL
18.34 mL
36.67 mL
5 mM
0.73 mL
3.67 mL
7.33 mL
10 mM
0.37 mL
1.83 mL
3.67 mL
50 mM
0.07 mL
0.37 mL
0.73 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.
Alagilleet al (2011) Potent mGluR5 antagonists: pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series. Bioorg.Med.Chem.Lett. 21 3243 PMID: 21546249
Kecket al (2012) Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation. ACS Med.Chem.Lett. 3 544 PMID: 22924094
Kecket al (2014) A novel mGluR5 antagonist, MFZ 10-7, inhibits cocaine-taking and cocaine-seeking behavior in rats. Addict.Biol. 19 195 PMID: 24001208