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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).
Catalogue Number
506074
Brand Family
Calbiochem®
References
References
Lorrio, S., et al. 2013. ACS Chem. Neurosci.4,1267. de Los Rios, C., et al. 2010. J. Med. Chem.53,5129.
Lorrio, S., et al. 2013. ACS Chem. Neurosci.4,1267. de Los Rios, C., et al. 2010. J. Med. Chem.53,5129.
数据表
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
13-December-2013 JSW
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).
Form
Off-white powder
Intert gas (Yes/No)
Packaged under inert gas
CAS number
1228658-31-8
Chemical formula
C₁₆H₁₉N₃O₂·HCl
Structure formula
Purity
≥98% by HPLC
Solubility
DMSO (100 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
Lorrio, S., et al. 2013. ACS Chem. Neurosci.4,1267. de Los Rios, C., et al. 2010. J. Med. Chem.53,5129.
