Biological Activity
Positive allosteric modulator at mGlu1 (EC50 values are 356 and 390 nM for rat and human receptors, respectively). Exhibits >25-fold selectivity for mGlu1 over mGlu4. Potentiates the decreased glutamate-induced calcium response in mGlu1 mutant cell models of schizophrenia.
Technical Data
| M. Wt | 446.67 |
| Formula | C20H10Cl3N3O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1623101-11-0 |
| PubChem ID | 91885483 |
| InChI Key | HJQXPBKPTGWZCF-UHFFFAOYSA-N |
| Smiles | ClC1=C2C(C(N(C3=CC=C(NC(C4=C(Cl)C=CC=N4)=O)C=C3Cl)C2=O)=O)=CC=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 | 22.33 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 446.67. 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 | 2.24 mL | 11.19 mL | 22.39 mL |
| 5 mM | 0.45 mL | 2.24 mL | 4.48 mL |
| 10 mM | 0.22 mL | 1.12 mL | 2.24 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.45 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Cho et al (2014) Chemical modulation of mutant mGlu1 receptors derived from deleterious GRM1 mutations found in schizophrenics. ACS Chem.Biol. 9 2334 PMID: 25137254
Keywords: VU 0483605, supplier, VU0483605, positive, allosteric, modulators, PAMs, mglu1, metabotropic, glutamate, receptors, schizophrenia, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience
