Overview
Cat #:
U-110
Alternative Name 3-CBW
Lyophilized Powder yes
Source Synthetic
MW: 333.29
Purity: >99%
Effective concentration 10-200 µM.
Structure
Chemical name 4-[[3-[(2S)-2-amino-2-carboxyethyl]-2,6-dioxopyrimidin-1-yl]methyl]benzoic acid.
Molecular formula C15H15N3O6.
CAS No.: 544697-47-4
PubChem CID 6604912
Activity UBP 282 is an antagonist of AMPA and kainate glutamate receptors. It reduces the AMPA-mediated fast component of dorsal root-evoked ventral root potential with IC50 of 10.3 µM, and fully inhibits AMPA-evoked responses in neonatal motoneurons at 200 µM. It differentially antagonizes kainate-induced responses in dorsal root C-fibres with pA2 of 4.96, but not in spinal neonatal rat motoneurons at 200 µM1,2.
References-Activity
- More, J.C. et al. (2002) Br. J. Pharmacol. 137, 1125.
- More, J.C. et al. (2003) Br. J. Pharmacol. 138, 1093.
Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Solubility Soluble up to 100 mM in 1 eq. NaOH. Centrifuge all products before handling (10000 x g 5 min).
Storage of solutions Store at -20°C. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.
Our bioassay
Alomone Labs UBP 282 inhibits GluA1 channels expressed in Xenopus oocytes.Representative time course of GluA1 current, activated by a continuous application (top dotted line) of 1 µM (S)-AMPA (#A-267), and reversibly inhibited by 10 µM and 100 µM UBP 282 (#U-110), as indicated (bars), at a holding potential of -60 mV.
Scientific background
UBP 282 (3-CBW) is a synthetic willardiine analogue that acts as an antagonist of AMPA and Kainate glutamate receptors. The compound fully inhibits AMPA-evoked responses in neonatal motoneurons at 200 µM and reduces the AMPA-mediated fast component of dorsal root-evoked ventral root potential with IC50 value of 10.3 µM1,2.
The ionotropic glutamate AMPA receptors (AMPARs) are the primary receptors that mediate fast excitatory synaptic transmission in the mammalian brain. This function is essential for synaptic plasticity and learning and memory3,4.
Kainate receptors (KARs) are highly expressed in the developing brain, where they are tonically activated to modulate synaptic transmission, network excitability, and synaptogenesis5.
Target AMPA, Kainate receptors
Lyophilized Powder
For research purposes only, not for human use
Last Update: 02/01/2024
Specifications
Citations
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