GluK1 (formerly GluR5) and GluK3 (formerly GluR7) receptor selective antagonist (Kb =10 nM and IC50 = 23 nM, respectively). IC50 values are >100 μM at recombinant human GLUA2 (formerly GluR2), GluK2 (formerly GluR6,) GluK2/GluK5 (formerly GluR6/KA2) and GluK2/GluK3 (formerly GluR6/GluR7). Selective over native AMPA receptors (Kd = 83 μM) and exhibits no activity at NMDA and Group I mGlu receptors at concentrations of up to 10 µM.
Store at +4°C. Store under desiccating conditions. The product can be stored for up to 12 months.
Soluble in DMSO to 100 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Dolman NP et al. Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists. J Med Chem50:1558-70 (2007).
Read more (PubMed: 17348638) »
Mayer ML et al. Crystal structures of the kainate receptor GluR5 ligand binding core dimer with novel GluR5-selective antagonists. J Neurosci26:2852-61 (2006).
Read more (PubMed: 16540562) »