Tideglusib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Tideglusib 是一种不可逆、非 ATP 竞争性 GSK-3β 抑制剂，在无细胞测定中 IC50 为 60 nM。

Tideglusib is an irreversible, non ATP-competitive GSK-3β inhibitor with IC50 of 60 nM in a cell-free assay; fails to inhibit kinases with a Cys homologous to Cys-199 located in the active site. Phase 2.(In Vitro):Incubation of both astrocyte and microglial cultures with Tideglusib (NP031112) completely abrogates the induction of TNF-α and COX-2 expression after glutamate treatment. These effects of NP031112 are not caused by a loss of cell viability, because the 24 h exposure of astrocyte and microglial cells to this TDZD does not modify cell viability.(In Vivo):Injection of Tideglusib (NP031112) (50 mg/kg) into the rat hippocampus dramatically reduces kainic acid-induced inflammation, as measured by edema formation using T2-weighted magnetic resonance imaging and glial activation and has a neuroprotective effect in the damaged areas of the hippocampus.

Incubation of both astrocyte and microglial cultures with Tideglusib (NP031112) completely abrogates the induction of TNF-α and COX-2 expression after glutamate treatment. These effects of NP031112 are not caused by a loss of cell viability, because the 24 h exposure of astrocyte and microglial cells to this TDZD does not modify cell viability.

Injection of Tideglusib (NP031112) (50 mg/kg) into the rat hippocampus dramatically reduces kainic acid-induced inflammation, as measured by edema formation using T2-weighted magnetic resonance imaging and glial activation and has a neuroprotective effect in the damaged areas of the hippocampus.

NP031112

PI3K/Akt/mTOR signaling

GSK-3

GSK-3β

Neurological Disease

——

865854-05-3

334.39

C19H14N2O2S

>98% (HPLC)

DMSO: 1 mg/mL (2.99 mM)

O=C(N1CC2=CC=CC=C2)N(C3=C4C=CC=CC4=CC=C3)SC1=O

2-(1-naphthalenyl)-4-(phenylmethyl)-1,2,4-thiadiazolidine-3,5-dione

(-20℃)

With Ice Pack

≥ 2 years