Description: Potent and selective negative allosteric modulator at mGlu5
Chemical Name: 3-Fluoro-N-(4-methyl-2-thiazolyl)-5-(5-pyrimidinyloxy)benzamide
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Potent and selective mGlu5 negative allosteric modulator (IC50 = 49 nM at human mGlu5). Selective for mGlu5 over a panel of GPCRs and ion channels. Exhibits no significant nonspecific binding in rat brain homogenates in vitro. Inhibits marble burying behavior in mice. Brain penetrant.
Technical Data
M. Wt
330.34
Formula
C15H11FN4O2S
Storage
Store at +4°C
Purity
≥98% (HPLC)
CAS Number
1276617-62-9
PubChem ID
50990953
InChI Key
AXVLPJHYYFHCHK-UHFFFAOYSA-N
Smiles
FC1=CC(OC2=CN=CN=C2)=CC(C(NC3=NC(C)=CS3)=O)=C1
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
33.03
100
Preparing Stock Solutions
The following data is based on the product molecular weight 330.34. 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
3.03 mL
15.14 mL
30.27 mL
5 mM
0.61 mL
3.03 mL
6.05 mL
10 mM
0.3 mL
1.51 mL
3.03 mL
50 mM
0.06 mL
0.3 mL
0.61 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.
Feltset al (2013) Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety. Bioorg.Med.Chem.Lett. 23 5779 PMID: 24074843
Keywords: VU 0409106, supplier, VU0409106, metabotropic, glutamate, receptors, negative, allosteric, modulators, NAMs, mGluR5, class, I, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience