产品描述: Tideglusib (NP031112) is an irreversible GSK-3 inhibitor with IC50s of 5 nM and 60 nM for GSK-3βWT (1 h preincubation) and GSK-3βC199A (1 h preincubation), respectively. |
靶点:
GSK-3β(WT):5 nM (IC50);GSK-3β(C199A):60 nM (IC50);GSK-3 |
体内研究:
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 |
参考文献:
1. Domínguez JM, et al. Evidence for irreversible inhibition of glycogen synthase kinase-3β by tideglusib. J Biol Chem, 2012, 287(2), 893-90 2. Luna-Medina R, et al. NP031112, a thiadiazolidinone compound, prevents inflammation and neurodegeneration under excitotoxic conditions: potential therapeutic role in brain disorders. J Neurosci, 2007, 27(21), 5766-5776. |
溶解性:
DMSO : 33.33 mg/mL (99.67 mM; Need ultrasonic) H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble) |
保存条件:
-20℃ |
配置溶液浓度参考:
|
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 |
50 mM |
0.06 ml |
0.299 ml |
0.598 ml |
|
注意: |
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