製品の概要

  • 製品名
    UBP310
  • 製品の詳細
    GluK1 and GluK3 selective antagonist
  • 生理活性の詳細
    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.
  • 精製度
    > 98%

製品の特性

参考文献

This product has been referenced in:
  • Perrais D  et al. Antagonism of recombinant and native GluK3-containing kainate receptors. Neuropharmacology 56:131-40 (2009). Read more (PubMed: 18761361) »
  • 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 Chem 50:1558-70 (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 Neurosci 26:2852-61 (2006). Read more (PubMed: 16540562) »

See all 3 Publications for this product

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