Biological Activity
Potent and selective GLUK5 (GluR5)-subunit containing kainate receptor antagonist (apparent KD = 402 nM); active enantiomer of UBP 296 (Cat. No. 2078). Displays ~ 260-fold selectivity over AMPA receptors, ~ 90-fold selectivity over recombinant human GLUK6- and GLUK2-containing kainate receptors and has little or no action at NMDA or group I mGlu receptors. Selectively blocks kainate receptor-mediated LTP induction in rat hippocampal mossy fibers. Also protects against soman-induced seizures and neuronal degeneration for up to 30 days when administered one hour after soman exposure.
Compound Libraries
UBP 302 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 333.3 |
| Formula | C15H15N3O6 |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 745055-91-8 |
| PubChem ID | 6420161 |
| InChI Key | UUIYULWYHDSXHL-NSHDSACASA-N |
| Smiles | O=C(C=CN(C[C@H](N)C(O)=O)C2=O)N2CC1=CC=CC=C1C(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. NaOH | 8.33 | 25 | |
| DMSO | 6.67 | 20mM with gentle warming |
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
Apland et al (2014) The Limitations of Diazepam as a Treatment for Nerve Agent-Induced Seizures and Neuropathology in Rats: Comparison with UBP302. J.Pharmacol.Exp.Ther. 351 359 PMID: 25157087
Keywords: UBP 302, supplier, Selective, potent, kainate, antagonists, Glutamate, Kainate, Receptors, iGluR, Ionotropic, UBP302, neurodegeneration, Kainate, Receptors, Kainate, Receptors, Tocris Bioscience
