Name | Tideglusib |
Synonyms | NP-12 NP031112 NP 031112 NP-031112 TIDEGLUSIB Tideglusib Tideglusib(NP-031112) 4-Benzyl-2-(naphthalen-1-yl)-[1,2,4]thiadiazolidine-3,5-dione 1,2,4-Thiadiazolidine-3,5-dione, 2-(1-naphthalenyl)-4-(phenylmethyl)- |
CAS | 865854-05-3 |
EINECS | 640-411-8 |
InChIKey | PMJIHLSCWIDGMD-UHFFFAOYSA-N |
Molecular Formula | C19H14N2O2S |
Molar Mass | 334.39 |
Density | 1.393 |
Melting Point | 148 - 150oC |
Boling Point | 511.3±43.0 °C(Predicted) |
Solubility | DMSO: >15mg/mL |
Appearance | powder |
Color | white to beige |
pKa | -1.51±0.20(Predicted) |
Storage Condition | 2-8°C |
MDL | MFCD18633296 |
Use | Tideglusib |
In vitro study | Irreversible inhibition of Tideglusib by GSK-3 in human neuroblastoma cells and murine primary neurons reduces tau protein phosphorylation levels and prevents apoptosis. Tideglusib (2.5 μm) inhibits glutamate-induced activation of glial cells, evidence for this conclusion is a decrease in the expression levels of TNF-α and COX-2 in rat primary astrocytes or microglia. Tideglusib (2.5 μm) also has a potent protective effect on cortical neurons from glutamate-induced excitotoxicity, evidence for this conclusion is a significant reduction in the number of Annexin-V positive cells in rat primary astrocytes or microglia Tideglusib in human neuroblastoma cells and rat primary neurons irreversible inhibition of GSK-3 thereby reduces the level of tau phosphorylation and prevents apoptosis. Tideglusib (2.5 μm) inhibits glutamate-induced activation of glial cells, evidence for this conclusion is a decrease in the expression levels of TNF-α and COX-2 in rat primary astrocytes or microglia. Tideglusib (2.5 μm) also has a potent protective effect on cortical neurons from glutamate-induced excitotoxicity, evidence for this conclusion is a significant reduction in the number of Annexin-V positive cells in rat primary astrocytes or microglia |
In vivo study | Tideglusib (50 mg/kg) injection into the hippocampus of adult male Wistar rats significantly reduced kainic acid-induced inflammatory responses and had a protective effect on damaged areas of the hippocampus. In APP/tau double transgenic mice, Tideglusib (200 mg/kg, P. O.) reduced tau phosphorylation, reduced amyloid deposition and plaque-associated astrocyte proliferation, protection of neurons in the entorhinal cortex and hippocampal CA1 region from death and prevention of memory loss Tideglusib (50 mg/kg) injection into the hippocampus of adult male Wistar rats can greatly reduce the inflammatory response induced by kainic acid and has a protective effect on the damaged area of the hippocampus. In APP/tau double transgenic mice, Tideglusib (200 mg/kg, P. O.) reduced tau phosphorylation, reduced amyloid deposition and plaque-associated astrocyte proliferation, protection of neurons in the entorhinal cortex and hippocampal CA1 region to prevent death and memory loss |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.991 ml | 14.953 ml | 29.905 ml |
5 mM | 0.598 ml | 2.991 ml | 5.981 ml |
10 mM | 0.299 ml | 1.495 ml | 2.991 ml |
5 mM | 0.06 ml | 0.299 ml | 0.598 ml |