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货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
---|---|---|---|---|
T127039-5mg |
5mg |
现货 ![]() |
| |
T127039-25mg |
25mg |
现货 ![]() |
| |
T127039-100mg |
100mg |
现货 ![]() |
|
别名 | NP-12;NP031112 |
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英文别名 | NP 031112;NP-031112;4-Benzyl-2-(naphthalen-1-yl)-[1,2,4]thiadiazolidine-3,5-dione |
规格或纯度 | ≥98% |
英文名称 | Tideglusib |
生化机理 | Tideglusib, also known as NP031112 or NP-12, is a potent non ATP-competitive inhibitor of glycogen synthase kinase-3 (GSK3), an important kinase studied in stem cell research and neurodegenerative diseases. It is currently in clinical trials for Alzheimer′s disease and Progressive Supranuclear Palsy (PSP). Tideglusib reduces phosphorylation of the tau protein and the accumulation of amyloid plaques, reduces hippocampal and entorhinal cortex neuron loss and improves spatial memory deficits. It has also shown neuroprotective and anti-inflammatory activity in a variety of animal models. |
储存温度 | -20°C储存 |
运输条件 | 超低温冰袋运输 |
备注 | 5mg、100mg卖完停产,不再备货 |
产品介绍 |
Tideglusib(NP-031112)是不可逆的非ATP竞争性GSK-3β抑制剂,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. |
IUPAC Name | 4-benzyl-2-naphthalen-1-yl-1,2,4-thiadiazolidine-3,5-dione |
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INCHI | InChI=1S/C19H14N2O2S/c22-18-20(13-14-7-2-1-3-8-14)19(23)24-21(18)17-12-6-10-15-9-4-5-11-16(15)17/h1-12H,13H2 |
InChi Key | PMJIHLSCWIDGMD-UHFFFAOYSA-N |
Canonical SMILES | C1=CC=C(C=C1)CN2C(=O)N(SC2=O)C3=CC=CC4=CC=CC=C43 |
WGK Germany | 3 |
PubChem CID | 11313622 |
分子量 | 334.39 |
PubChem CID | 11313622 |
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Wikipedia | Tideglusib |
CAS Registry No. | 865854-05-3 |
溶解性 | DMSO 1 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
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WGK Germany | 3 |
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输入批号以搜索COA:
1. Luna-Medina R, Cortes-Canteli M, Sanchez-Galiano S, Morales-Garcia JA, Martinez A, Santos A, Perez-Castillo A. (2007) NP031112, a thiadiazolidinone compound, prevents inflammation and neurodegeneration under excitotoxic conditions: potential therapeutic role in brain disorders.. J Neurosci, 27 (21): (5766-76). [PMID:17522320] |
2. Martinez A, Gil C, Perez DI. (2011) Glycogen synthase kinase 3 inhibitors in the next horizon for Alzheimer's disease treatment.. Int J Alzheimers Dis, 2011 (13): (280502). [PMID:21760986] |
3. Domínguez JM, Fuertes A, Orozco L, del Monte-Millán M, Delgado E, Medina M. (2012) Evidence for irreversible inhibition of glycogen synthase kinase-3β by tideglusib.. J Biol Chem, 287 (2): (893-904). [PMID:22102280] |
4. del Ser T, Steinwachs KC, Gertz HJ, Andrés MV, Gómez-Carrillo B, Medina M, Vericat JA, Redondo P, Fleet D, León T. (2013) Treatment of Alzheimer's disease with the GSK-3 inhibitor tideglusib: a pilot study.. J Alzheimers Dis, 33 (1): (205-15). [PMID:22936007] |
5. Neves VC, Babb R, Chandrasekaran D, Sharpe PT. (2017) Promotion of natural tooth repair by small molecule GSK3 antagonists.. Sci Rep, 7 (13): (39654). [PMID:28067250] |
6. Yang T, Zhang T, Guan XN, Dong Z, Lan L, Yang S, Yang CG. (2020) Tideglusib and Its Analogues As Inhibitors of Staphylococcus aureus SrtA.. J Med Chem, 63 (15): (8442-8457). [PMID:32639734] |