UBP 310

Product Description

UBP 310 is a GluK1 (formerly GLU_K5) kainate receptor antagonist (IC₅₀ = 130 nM); also blocks recombinant homomeric GluK3 (forrmerly GLU_K7) receptors. Displays 12,700-fold selectivity for GluK1 (formerly GLU_K5) over GluK2 (formerly GLU_K6). Exhibits no activity at mGlu group I or NMDA receptors at concentrations of up to 10 μM. Apparent K_D value is 18 ± 4 nM for depression of kainate responses on the dorsal root.

Please refer to IUPHAR Guide to Pharmacology for the most recent naming conventions.

Solubility

Preparing Stock Solutions for UBP 310

The following data is based on the product molecular weight 353.35

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.2 mM	14.15 mL	70.75 mL	141.50 mL
1 mM	2.83 mL	14.15 mL	28.30 mL
2 mM	1.42 mL	7.08 mL	14.15 mL
10 mM	0.28 mL	1.42 mL	2.83 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Dolman 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. 2007 PMID: 17348638
• Perrais Antagonism of recombinant and native GluK3-containing kainate receptors. Neuropharmacology 2009 PMID: 18761361
• Mayer Crystal structures of the kainate receptor GluR5 ligand binding core dimer with novel GluR5-selective antagonists. J.Neurosci. 2006 PMID: 16540562