5.05017
UBP310
别名:
UBP310, GluK1/GluK3 antagonist, UBP310, (S)-1-(2-Amino-2-carboxyethyl)-3-(2-carboxy-thiophene-3-yl-methyl)-5-methylpyrimidine-2,4-dione, UBP-310, UBP 310
InChI key
ZTAZUCRXCRXNSU-VIFPVBQESA-N
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
assay
≥98% (HPLC)
form
solid
potency
10 nM Ki
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 100 mM
Quality Level
General description
A potent antagonist highly selective for GluK1 (Kb = 10 nM), GluK3 (IC50 = 23 nM), and GluK1/K5 (Kb = 8 nM) subtype kainate receptors. Does not interact with GluK2 and GluK2/K5 receptors. Low affinity to AMPA receptors (Kd = 83 µM). Does not interact with mGluR1 or NMDA receptors at concentration less than 10 µM. Often used in studying neuronal excitability and synaptic plasticity.
Biochem/physiol Actions
Primary Target
GluK1
GluK1
Secondary Target
Gluk3
Gluk3
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Pinheiro, S., et al. 2013. Cereb. Cort.23, 323.
Atlason, T., et al. 2010. Mol. Pharmacol.78, 1036.
Perrais, D., et al. 2009. Neuropharmacol.56, 131.
Dolman, P., et al. 2007. J. Med. Chem.50, 1558.
Mayer, L., et al. 2006. J. Neurosci.26, 2852.
Atlason, T., et al. 2010. Mol. Pharmacol.78, 1036.
Perrais, D., et al. 2009. Neuropharmacol.56, 131.
Dolman, P., et al. 2007. J. Med. Chem.50, 1558.
Mayer, L., et al. 2006. J. Neurosci.26, 2852.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
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