Tideglusib(NP-031112)

产品编号: DC8607 Featured
Tideglusib(NP-031112)
结构式
865854-05-3
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应用领域
Tideglusib (NP031112) 是一种不可逆的 GSK-3 抑制剂,抑制 GSK-3βWT 和GSK-3βC199A 的 IC50 分别为5 nM,60 nM。
Cas No.: 865854-05-3
名称:
别名: NP-12; NP031112; NP 031112; NP-031112
SMILES: S1C(=O)N(CC2=CC=CC=C2)C(=O)N1C1=C2C(C=CC=C2)=CC=C1
分子式: C19H14N2O2S
分子量: 334.39
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: Tideglusib(NP-031112) is an irreversible, non ATP-competitive GSK-3β inhibitor with IC50 of 60 nM. in vitro: Tideglusib irreversibly inhibits GSK-3, reduces tau phosphorylation, and prevents apoptotic death in human neuroblastoma cells and murineprimary neurons . Tideglusib (2.5 μM) inhibits glutamate-induced glial activation as evidenced by decreased TNF-α and COX-2 expression in rat primary astrocyte or microglial cultures. Tideglusib (2.5 μM) also exerts a potent neuroprotective effect on cortical neurons from glutamate-induced excitotoxicity as evidenced by significant reduction in the number of Annexin-V-positive cells in rat primary astrocyte or microglial cultures. in vivo: Tideglusib (50 mg/kg) injected into the adult male Wistar rats hippocampus dramatically reduces kainic acid-induced inflammation and has a neuroprotective effect in the damaged areas of the hippocampus. Tideglusib (200 mg/kg, oral) results in lower levels of tau phosphorylation, decreased amyloid deposition and plaque-associated astrocytic proliferation, protection of neurons in the entorhinal cortex and CA1 hippocampal subfield against cell death, and prevention of memory deficits in APP/tau double transgenic mice.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
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