Thiamet G
货号：
13237-1mg 基本售价：
448.0 元 规格：
1 mg
产品信息
概述| 货号 | 13237-1mg |
| 描述 | Hyperphosphorylation of the tau protein leads to its aggregation and formation of neurofibrillary tangles, a hallmark of Alzheimer’s disease and other tauopathic, neurodegenerative disorders. Tau is also dynamically modified by the addition and cleavage of O-linked β-N-acetylglucosamine (O-GlcNAc) moieties, which is mediated in part by O-GlcNAcase. Levels of O-GlcNAcylated proteins from Alzheimer’s disease brain extracts are decreased as compared to that in controls, suggesting that impaired brain glucose metabolism may contribute to pathogenesis.1 Thiamet G is a potent and selective inhibitor of O-GlcNAcase that demonstrates a Ki value of 21 nM.2 It increases cellular O-GlcNAc-modified protein levels (EC50 = 30 nM) and blocks phosphorylation of tau protein both in cultured PC-12 cells and in rats (200 mg/kg/day).2 Thiamet G is the first highly potent O-GlcNAcase inhibitor known to be orally bioavailable and effectively cross the blood brain barrier.2 |
性能| 供应商 | Cayman |
| 应用文献 |
1.Liu, F.,Iqbal, K.,Grundke-Iqbal, I., et al. O-GlnNAcylation regulates phosphorylation of tau: A mechanism involved in Alzheimer’s disease. Proceedings of the National Academy of Sciences of the United States of America 101(29), 10804-10809 (2004).
2.Yuzwa, S.A.,Macauley, M.S.,Heinonen, J.E., et al. A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. Nature Chemical Biology 4(8), 483-490 (2008).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥97% |
| 计算分子量 | 248.3 |
| 分子式 | C9H16N2O4S |
| CAS号 | 1009816-48-1 |
| 稳定性 | ≥ 2 years |
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