5.06074

PP2A Activating Ligand, ITH12246

• Sinónimos: PP2A Activating Ligand, ITH12246
• Fórmula empírica (notación de Hill): C₁₆H₁₉N₃O₂ · xHCl
• Número de CAS: 1228658-31-8
• Peso molecular: 285.34 (free base basis)
• UNSPSC Code: 12352200
• NACRES: NA.77

Propiedades

• assay: ≥98% (HPLC)
• Quality Level: 100
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white
• solubility: DMSO: 100 mg/mL
• storage temp.: 2-8°C

Descripción

General description

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).

Biochem/physiol Actions

Primary Target
PP2A

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Información de seguridad

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable