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Thiamet G

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Chemical Structure| 1009816-48-1 同义名 : -
CAS号 : 1009816-48-1
货号 : A333018
分子式 : C9H16N2O4S
纯度 : 99%+
分子量 : 248.299
MDL号 : MFCD15144964
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 45 mg/mL(181.23 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(201.37 mM)
动物实验配方：
生物活性
描述 Oligomerization of tau is a key process contributing to the progressive death of neurons in Alzheimer's disease. Tau is modified by O-linked N-acetylglucosamine (O-GlcNAc), and O-GlcNAc can influence tau phosphorylation in certain cases. Thiamet G is a selective and potent inhibitor of O-GlcNAcase (OGA), which can remove O-GlcNAc from modified proteins, with Ki of 20 nM for human OGA[3]. In Pc-12 cells, Thiamet G increased the level of O-GlcNAc by inhibiting OGA with an EC50 value of 30 nM. Thiamet G (100 mM) decreased tau phosphorylation at Ser396, Thr231, Ser422, and Ser262 by 2.1, 2.7, 1.2, and 1.3 times, respectively. Thiamet G was injected intravenously at a dose of 50 mg/kg in rats. It could increase the O-GlcNAc level in brain in a dose- and time-dependent manner and reduce tau phosphorylation in brain after crossing the blood brain barrier[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.03mL

0.81mL

0.40mL

20.14mL

4.03mL

2.01mL

40.27mL

8.05mL

4.03mL
参考文献

[1]Goldberg H, Whiteside C, et al. O-linked β-N-acetylglucosamine supports p38 MAPK activation by high glucose in glomerular mesangial cells. Am J Physiol Endocrinol Metab. 2011 Oct;301(4):E713-26.

[2]Yuzwa SA, Macauley MS, et al. A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. Nat Chem Biol. 2008 Aug;4(8):483-90.

[3]Yuzwa SA, Shan X, Macauley MS, Clark T, Skorobogatko Y, Vosseller K, Vocadlo DJ. Increasing O-GlcNAc slows neurodegeneration and stabilizes tau against aggregation. Nat Chem Biol. 2012 Feb 26;8(4):393-9. doi: 10.1038/nchembio.797. PMID: 22366723.

[4]Yuzwa SA, Macauley MS, Heinonen JE, Shan X, Dennis RJ, He Y, Whitworth GE, Stubbs KA, McEachern EJ, Davies GJ, Vocadlo DJ. A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo. Nat Chem Biol. 2008 Aug;4(8):483-90. doi: 10.1038/nchembio.96. Epub 2008 Jun 29. PMID: 18587388.