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Merck

5.06074

PP2A Activating Ligand, ITH12246

Synonym(s):

PP2A Activating Ligand, ITH12246

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About This Item

Empirical Formula (Hill Notation):
C16H19N3O2 · xHCl
CAS Number:
Molecular Weight:
285.34 (free base basis)
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
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assay

≥98% (HPLC)

Quality Segment

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

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

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)


Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



Certificates of Analysis (COA)

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