1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. iGluR
  3. UBP-282

UBP-282 

Cat. No.: HY-19432
Handling Instructions

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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UBP-282 Chemical Structure

UBP-282 Chemical Structure

CAS No. : 544697-47-4

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Description

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[1][2].

IC50 & Target

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]

In Vitro

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].

In Vivo

On neonatal rat motoneurones UBP-282 (3-CBW) (200 μM) almost completely abolished responses to AMPA while responses to NMDA, kainate and DHPG were 101.6%, 39.4% and 110.5% of control, respectively. UBP-282 can therefore be used to isolate kainate receptor responses from those mediated by AMPA receptors[1].

Molecular Weight

333.30

Formula

C₁₅H₁₅N₃O₆

CAS No.

544697-47-4

SMILES

O=C(O)[[email protected]@H](N)CN(C(N1CC2=CC=C(C(O)=O)C=C2)=O)C=CC1=O

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

UBP-282UBP282UBP 282iGluRIonotropic glutamate receptorsGluR5AMPAkainatewillardiinefDR-VRPdepolarisationsmotoneuronesInhibitorinhibitorinhibit

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UBP-282
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HY-19432
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