UBP-282
UBP-282 is a potent, selective and competitive AMPA and kainate receptor antagonist. UBP-282 inhibits the fast component of the dorsal root-evoked ventral root potential (fDR-VRP) with an IC50 value of 10.3 μM. UBP-282 antagonizes kainate-induced depolarisations of dorsal roots with a pA2 value of 4.96.
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- CAS No.: 544697-47-4
- Formula: C15H15N3O6
- Molecular Weight:333.30
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
IC50: 10.3 μM (fast component of the dorsal root-evoked ventral root potential (fDR-VRP))[1]
pA2: 4.96 (Kainate<-induced depolarisations of dorsal roots)[1]
UBP-282 (3-CBW) is selective for AMPA- and GluR5-containing kainate receptors vs NMDA, mGlu and kainate receptors expressed on motor neurones[1][2].
UBP-282 (3-CBW), at a concentration of 200 μM, blocks AMPA evoked depolarizations on motoneurones while responses to equi-effective doses of NMDA and DHPG were relatively unaffected. In the presence of 200 μM UBP-282, a concentration that completely abolishes AMPA-evoked depolarizations on motoneurones and kainate-evoked responses on dorsal root, there is still a noticeable depolarization evoked by kainate on motoneurones[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 544697-47-4
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Molecular Weight 333.30
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Formula C15H15N3O6
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SMILES
O=C(O)[C@@H](N)CN(C(N1CC2=CC=C(C(O)=O)C=C2)=O)C=CC1=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Julia C A More, et al. The novel antagonist 3-CBW discriminates between kainate receptors expressed on neonatal rat motoneurones and those on dorsal root C-fibres. Br J Pharmacol. 2002 Dec;137(7):1125-33. [Content Brief]
[2]. Julia C A More, et al. Structural requirements for novel willardiine derivatives acting as AMPA and kainate receptor antagonists. Br J Pharmacol. 2003 Mar;138(6):1093-100. [Content Brief]
Calculators
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