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

• Synonim(y): 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
• Wzór empiryczny (zapis Hilla): C₁₃H₁₄ClN₃O₄
• Numer CAS: 501925-31-1
• Masa cząsteczkowa: 311.72
• Numer MDL: MFCD00095313
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Poziom jakości: 100
• Próba: ≥99% (HPLC)
• Postać: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: white
• rozpuszczalność: DMSO: 100 mg/mL, clear, colorless
• Warunki transportu: ambient
• temp. przechowywania: 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)
• Klucz InChI: CEIIEALEIHQDBX-UHFFFAOYSA-N

Opis

Opis ogólny

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.

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Rekonstytucja

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

Inne uwagi

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

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable