5.06074

PP2A Activating Ligand, ITH12246

• Sinonimo/i: PP2A Activating Ligand, ITH12246
• Formula empirica (notazione di Hill): C₁₆H₁₉N₃O₂ · xHCl
• Numero CAS: 1228658-31-8
• Peso molecolare: 285.34 (free base basis)
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Saggio: ≥98% (HPLC)
• Livello qualitativo: 100
• Stato: powder
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: off-white
• Solubilità: DMSO: 100 mg/mL
• Temperatura di conservazione: 2-8°C

Descrizione

Descrizione generale

A cell-permeable, relatively non-toxic, 1,8-naphthyridine derived compound that blocks the inhibitory effect of protein phosphatase inhibitors, such as okadaic acid, on protein phosphatase 2A (PP2A). Exhibits blood-brain barrier permeability. Protects neurons against β-amyloid peptides (Ab1-42) toxicity and okadaic acid (Cat. No. 459620)-induced tau hyperphosphorylation. Also protects against rotenone and oligomycin A induced neurotoxicity in SH-SY5Y neuroblastoma cells (at ~300 nM). Prevents the development of glutamate-induced neuronal lesions in rat hippocampal slices by up-regulating PP2A (~ 3.0 µM). Shown to reverse the scopolamine-induced memory loss in mice (~10 mg/kg i.p) and significantly reduces the infarct volume in an animal model of stroke (~2.5 mg/kg). Also acts as an inhibitor of acetylcholinesterase activity in Electrophorus electricus (IC₅₀ = 60 nM) and human erythrocytes (IC₅₀ = 780 nM).

Azioni biochim/fisiol

Primary Target
PP2A

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

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

Altre note

Lorrio, S., et al. 2013. ACS Chem. Neurosci.4,1267.
de Los Rios, C., et al. 2010. J. Med. Chem.53,5129.

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable