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Submit ReviewVU 0483605
Description: Positive allosteric modulator of mGlu1 receptors
Chemical Name: 3-Chloro-N-[3-chloro-4-(4-chloro-1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)phenyl]-2-pyridinecarboxamide
Purity: ≥98% (HPLC)
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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 the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 4.48 mL | 22.39 mL | 44.78 mL |
| 2.5 mM | 0.9 mL | 4.48 mL | 8.96 mL |
| 5 mM | 0.45 mL | 2.24 mL | 4.48 mL |
| 25 mM | 0.09 mL | 0.45 mL | 0.9 mL |
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References
References are publications that support the biological activity of the product.
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
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Keywords: VU 0483605, VU 0483605 supplier, VU0483605, positive, allosteric, modulators, PAMs, mglu1, metabotropic, glutamate, receptors, schizophrenia, Glutamate, (Metabotropic), Group, I, Receptors, 5377, Tocris Bioscience
1 Citation for VU 0483605
Citations are publications that use Tocris products. Selected citations for VU 0483605 include:
Hellyer et al (2018) "Selective" Class C G Protein-Coupled Receptor Modulators Are Neutral or Biased mGlu5 Allosteric Ligands. Mol.Pharmacol. 93 504 PMID: 29514854
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