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. Nr.: 544697-47-4
- Formel: C15H15N3O6
- Molecular Weight:333.30
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Speicherung:
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Biologische Aktivität
Beschreibung
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 544697-47-4
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Molecular Weight 333.30
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Reinheit & Dokumentation
Verweise
[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
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
UBP-282 Related Classifications
HY-19432 Related Classifications
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