Description: Selective, potent kainate antagonist; selective for GluR5-containing receptors
Chemical Name: (RS)-1-(2-Amino-2-carboxyethyl)-3-(2-carboxybenzyl)pyrimidine-2,4-dione
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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
Certificate of Analysis / Product Datasheet
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References
References are publications that support the products' biological activity.
Moreet al (2004) Characterisation of UBP296: a novel, potent and selective kainate receptor antagonist. Neuropharmacology 47 46 PMID: 15165833
Dolmanet al (2005) Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors. J.Med.Chem. 48 7867 PMID: 16302825