Biological Activity
Selective GluR5-subunit containing kainate receptor antagonist (apparent KD = 1.09 μM). Displays ~ 90-fold selectivity over AMPA receptors and recombinant human GluR6- and KA2-containing kainate receptors. Has little or no action at NMDA or group I mGlu receptors. Selectively blocks kainate receptor-mediated LTP induction in rat hippocampal mossy fibers. Active enantiomer UBP 302 (Cat. No. 2079) available.
Technical Data
| M. Wt | 333.3 |
| Formula | C15H15N3O6 |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 745055-86-1 |
| PubChem ID | 11674376 |
| InChI Key | UUIYULWYHDSXHL-UHFFFAOYSA-N |
| Smiles | NC(CN1C=CC(=O)N(CC2=C(C=CC=C2)C(O)=O)C1=O)C(O)=O |
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 | |||
| 1eq. HCl | 1.67 | 5mM with gentle warming | |
| 1eq. NaOH | 3.33 | 10mM with gentle warming | |
| DMSO | 3.33 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 333.3. 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 | 3 mL | 15 mL | 30 mL |
| 5 mM | 0.6 mL | 3 mL | 6 mL |
| 10 mM | 0.3 mL | 1.5 mL | 3 mL |
| 50 mM | 0.06 mL | 0.3 mL | 0.6 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
More et al (2004) Characterisation of UBP296: a novel, potent and selective kainate receptor antagonist. Neuropharmacology 47 46 PMID: 15165833
Dolman et al (2005) Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors. J.Med.Chem. 48 7867 PMID: 16302825
Keywords: UBP 296, supplier, Selective, potent, kainate, antagonists, selective, GluR5-containing, receptors, Glutamate, Kainate, Receptors, iGluR, Ionotropic, UBP296, Kainate, Receptors, Kainate, Receptors, Tocris Bioscience
