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
References
References are publications that support the products' biological activity.
Felts et 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
