Biological Activity
GLUK5 kainate receptor antagonist (IC50 = 130 nM); also blocks recombinant homomeric GLUK7 receptors. Displays 12,700-fold selectivity for GLUK5 over GLUK6. Exhibits no activity at mGlu group I or NMDA receptors at concentrations of up to 10 μM. Apparent KD value is 18 ± 4 nM for depression of kainate responses on the dorsal root.
Compound Libraries
UBP 310 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 353.35 |
| Formula | C14H15N3O6S |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 902464-46-4 |
| PubChem ID | 6420160 |
| InChI Key | ZTAZUCRXCRXNSU-VIFPVBQESA-N |
| Smiles | CC1=CN(C[C@@H](C(O)=O)N)C(N(CC2=C(C(O)=O)SC=C2)C1=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 | |||
| DMSO | 35.34 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 353.35. 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 | 2.83 mL | 14.15 mL | 28.3 mL |
| 5 mM | 0.57 mL | 2.83 mL | 5.66 mL |
| 10 mM | 0.28 mL | 1.42 mL | 2.83 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.57 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Mayer et al (2006) Crystal structures of the kainate receptor GluR5 ligand binding core dimer with novel GluR5-selective antagonists. J.Neurosci. 26 2852 PMID: 16540562
Dolman et al (2007) Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: Role of the substituent at the 5-position of the uracil ring in development of highly potent and selective GLUK5 kainate receptor antagonists. J.Med.Chem. 50 1558 PMID: 17348638
Perrais et al (2009) Antagonism of recombinant and native GluK3-containing kainate receptors. Neuropharmacology 56 131 PMID: 18761361
Keywords: UBP 310, supplier, UBP310, kainate, receptors, antagonists, GLUK5, iGlu, ionotropic, glutamate, Kainate, Receptors, Kainate, Receptors, Tocris Bioscience
