Biological Activity
Potent allosteric potentiator at the rat mGlu5 receptor (EC50 = 9 nM); binds to the MPEP (Cat. No. 1212) allosteric site (Ki app = 244 nM). Selective for mGlu5 over mGlu1 and mGlu2 receptors (EC50 values are 557 nM and 1.51 μM for mGlu1 and mGlu2 respectively). Potentiates both DHPG-induced LTP and threshold θ-burst stimulation (TBS)-induced LTP in rat hippocampal slices. Analog of CDPPB (Cat. No. 3235).
Compound Libraries
VU 29 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 384.39 |
| Formula | C22H16N4O3 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 890764-36-0 |
| PubChem ID | 11610682 |
| InChI Key | KIALCSMRIHRFPL-UHFFFAOYSA-N |
| Smiles | O=C(C4=CC=C([N+]([O-])=O)C=C4)NC1=CC(C3=CC=CC=C3)=NN1C2=CC=CC=C2 |
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 | 38.44 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 384.39. 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 | 2.6 mL | 13.01 mL | 26.02 mL |
| 5 mM | 0.52 mL | 2.6 mL | 5.2 mL |
| 10 mM | 0.26 mL | 1.3 mL | 2.6 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Chen et al (2007) Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses. Mol.Pharmacol. 71 1389 PMID: 17303702
de Paulis et al (2006) Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes. J.Med.Chem. 49 3332 PMID: 16722652
Ayala et al (2009) mGluR5 positive allosteric modulators facilitate both hippocampal LTP and LTD and enhance spatial learning. Neuropsychopharmacology 34 2057 PMID: 19295507
Keywords: VU 29, supplier, VU29, mGlu5, mGluR5, pams, positive, allosteric, potentiators, modulators, glutamate, receptors, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience
