Biological Activity
Positive allosteric modulator at mGlu4 receptors (EC50 = 290 nM in mGlu4-expressing HEK 293 cells). Reverses haloperidol-induced catalepsy in rats; prevents attentional deficit and forelimb asymmetry in a rodent model of Parkinson's disease. Exhibits affinity for MAO-B and MAO-A (Ki values are 0.72 μM and 8.5 μM respectively). Brain penetrant.
Technical Data
| M. Wt | 232.67 |
| Formula | C12H9ClN2O |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 61350-00-3 |
| PubChem ID | 836002 |
| InChI Key | SUYUTNCKIOLMAJ-UHFFFAOYSA-N |
| Smiles | O=C(C2=NC=CC=C2)NC1=CC=CC(Cl)=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 | 23.27 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 232.67. 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 | 4.3 mL | 21.49 mL | 42.98 mL |
| 5 mM | 0.86 mL | 4.3 mL | 8.6 mL |
| 10 mM | 0.43 mL | 2.15 mL | 4.3 mL |
| 50 mM | 0.09 mL | 0.43 mL | 0.86 mL |
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References
References are publications that support the products' biological activity.
Jones et al (2012) The metabotropic glutamate receptor 4-positive allosteric modulator VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson's disease. J.Pharmacol.Exp.Ther. 340 404 PMID: 22088953
Keywords: VU 0364770, supplier, VU0364770, glutamate, receptor, Glu, mGlu4, mGluR4, postive, allosteric, modulators, pams, brain, penetrant, Glutamate, (Metabotropic), Group, III, Receptors, Glutamate, (Metabotropic), Group, III, Receptors, Tocris Bioscience
