528201

PNU-120596

A urea derivative that acts as a potent, selective, and reversible positive allosteric modulator for the α7 subtype of neural nicotinic acetylcholine receptors

• Sinônimo(s): PNU-120596, α7 Neuronal Nicotinic Acetylcholine Receptor Agonist, PNU-120596, 1-(5-chloro-2,4-dimethoxy-phenyl)-3-(5-methyl-isoxazol-3-yl)-urea, a7 nAChR agonist, PNU-120596
• Fórmula empírica (Notação de Hill): C₁₃H₁₄ClN₃O₄
• Número CAS: 501925-31-1
• Peso molecular: 311.72
• Número MDL: MFCD00095313
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥99% (HPLC)
• forma: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: white
• solubilidade: DMSO: 100 mg/mL, clear, colorless
• Condições de expedição: ambient
• temperatura de armazenamento: 2-8°C
• InChI: 1S/C13H14ClN3O4/c1-7-4-12(17-21-7)16-13(18)15-9-5-8(14)10(19-2)6-11(9)20-3/h4-6H,1-3H3,(H2,15,16,17,18)
• chave InChI: CEIIEALEIHQDBX-UHFFFAOYSA-N

Descrição

Descrição geral

A urea derivative that acts as a potent, selective, and reversible positive allosteric modulator for the α7 subtype of neural nicotinic acetylcholine receptors (EC₅₀ = 216 nM), with no significant effect on α4β2, α3β4 and α9α10 receptors. Specifically increase a-7 nAChR-mediated channel currents and channel mean open time in cultured neurons (~ 1 mM). However, it does neither affect ion selectivity nor unitary conductance. Shown to cross the blood-brain barrier. Causes conformational changes in the ligand binding domain of a7 nicotinic receptors that partially overlap with those caused by acetylcholine. Causes changes in cysteine accessibility at the inner beta sheet, transition zone, and agonist binding site. Also reported to potentiate agonist-evoked GABAergic postsynaptic inward currents in somatodendritic membrane of hippocampal interneurons.

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Reconstituição

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Outras notas

Hurst, R., et al. 2005. J. Neurosci. 25, 4396.
Barron, S., et al. 2009. Mol. Pharm.76, 253.

Informações legais

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable