A selective antagonist of GluR5
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UBP 310

Item No. 21806

Technical Information
Formal Name
(αS)-α-amino-3-[(2-carboxy-3-thienyl)methyl]-3,4-dihydro-5-methyl-2,4-dioxo-1(2H)-pyrimidinepropanoic acid
CAS Number
902464-46-4
Molecular Formula
C14H15N3O6S
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMSO: Slightly soluble
λmax
262 nm
SMILES
O=C(N(C[C@H](N)C(O)=O)C=C1C)N(CC2=C(C(O)=O)SC=C2)C1=O
InChi Code
InChI=1S/C14H15N3O6S/c1-7-4-16(6-9(15)12(19)20)14(23)17(11(7)18)5-8-2-3-24-10(8)13(21)22/h2-4,9H,5-6,15H2,1H3,(H,19,20)(H,21,22)/t9-/m0/s1
InChi Key
ZTAZUCRXCRXNSU-VIFPVBQESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    UBP 310 is an antagonist of ionotropic glutamate receptor 5 (GluR5 or GluK1; Kd = 130 nM).1,2,3 It less potently binds GluR2 (GluA2) and GluR6 (GluK2; Kds = 106 and 1,626 µM, respectively).4,2 UBP 310 is inactive at metabotropic GluR group I and NMDA receptors.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Atlason, P.T., Scholefield, C.L., Eaves, R.J., et alMapping the ligand binding sites of kainate receptors: Molecular determinants of subunit-selective binding of the antagonist 3HUBP310. Mol. Pharmacol. 78(6), 1036-1045 (2010).

    2. Mayer, M.L., Ghosal, A., Dolman, N.P., et alCrystal structures of the kainate receptor GluR5 ligand binding core dimer with novel GluR5-selective antagonists. J. Neurosci. 26(11), 2852-2861 (2006).

    3. Perrais, D., Pinheiro, P.S., Jane, D.E., et alAntagonism of recombinant and native GluK3-containing kainate receptors. Neuropharmacology 56(1), 131-140 (2009).

    4. Du, M., Rambhadran, A., and Jayaraman, V. Luminescence resonance energy transfer investigation of conformational changes in the ligand binding domain of a kainate receptor. The Journal of Biological Chemisty 283(40), 27074-27078 (2008).