Cat. No. 3621
Chemical Name: (S)-1-(2-Amino-2-carboxyethyl)-3-(2
Biological ActivityGLUK5 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.
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.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Perrais et al (2009) Antagonism of recombinant and native GluK3-containing kainate receptors. Neuropharmacology 56 131. PMID: 18761361.
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.
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.
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Citations are publications that use Tocris products. Selected citations for UBP 310 include:
Crook et al (2014) A synaptic signature for ON- and OFF-center parasol ganglion cells of the primate retina. Vis Neurosci 31 57. PMID: 24801624.
Buldyrev et al (2012) Synaptic pathways that shape the excitatory drive in an OFF retinal ganglion cell. J Neurophysiol 107 1795. PMID: 22205648.
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Keywords: UBP 310, supplier, UBP310, kainate, receptors, antagonists, GLUK5, iGlu, ionotropic, glutamate, Tocris Bioscience, Kainate Receptor Antagonist products