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Submit ReviewVU 0483605
Discontinued Product
VU 0483605 (Cat. No. 5377) has been withdrawn from sale for commercial reasons.
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 for VU 0483605
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 for VU 0483605
| 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.
Product Datasheets for VU 0483605
References for VU 0483605
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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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Metabotropic Glutamate Receptors Scientific Review
Written by Francine Acher, this review discusses the pharmacology and therapeutic potential of mGlu receptors, and the compounds acting upon them; compounds available from Tocris are listed.
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