Name: Thiamet G
Brand: TargetMol
SKU: T6056
Price: 286 CNY
Availability: InStock
Rating: 5 (10 reviews)

规格

价格

库存

数量

2 mg

¥ 286

In stock

5 mg

¥ 497

In stock

10 mg

¥ 828

In stock

25 mg

¥ 1,770

In stock

50 mg

¥ 3,210

In stock

100 mg

¥ 4,680

待询

500 mg

¥ 9,820

待询

1 mL x 10 mM (in DMSO)

¥ 516

In stock

产品介绍

生物活性

产品描述	Thiamet G is a potent O-GlcNAcase inhibitor (Ki=20 nM) with selectivity. The role of O-GlcNAcase is to remove O-GlcNAc from the modified protein.
靶点活性	O-GlcNAcase (OGA, human):20 nM (Ki), O-GlcNAcase (OGA):21 nM (Ki), O-GlcNAcase (OGA):30 nM (EC50)
体外活性	方法：PC-12细胞用Thiamet G （1 nM-250 μM）处理后，使用Western Blot检测 O-GlcNAcase水平。PC-12细胞用Thiamet G （100 mM）处理后，使用Western Blot检测 O-GlcNAcase水平。结果：Thiamet G 在PC-12细胞中以剂量和时间依赖性方式抑制O-GlcNAcase，并降低tau蛋白磷酸化水平。[1] 方法：系膜细胞用Thiamet G （12.5 、25 nM）处理后，使用Western Blot检测O-GlcNAcylation水平、p38磷酸化水平。结果： Thiamet G通过增加O-GlcNAcylation，在肾小球系细胞中显著增强p38磷酸化。[2]
体内活性	方法：为研究Thiamet G的神经保护作用，将Thiamet G（20 mg/kg）腹腔注射给小鼠，连续3天。结果：Thiamet G通过抑制O-GlcNAcase表现出神经保护作用。[3] 方法：为研究Thiamet G的抗癫痫作用，将Thiamet G（10 mg/kg）腹腔注射给癫痫大鼠模型,每天一次，连续三天。结果：Thiamet G显著减少了癫痫发作的持续时间和发作间期尖峰频率。[4]
激酶实验	All enzymatic assays are performed in triplicate at 37°C using 4-methylumbelliferyl N-acetyl-β-d-glucosaminide dehydrate as substrate. 1 nM of purified OGA is incubated with the compounds for 5 min, and then 0.2 mM of the substrate is added. The liberation of 4-methylumbellifery is monitored by kinetic reading at excitation/emission 355/460 nm using a Tecan M200 plate in a mode of 60 s/cycle and 15 cycles in total.
细胞实验	Jurkat cells are seeded at 6000 cells/well in a 96-well plate, and 12 h later, cells are treated with compounds for the indicated time. Cell viability is determined by XTT assay.
别名	TMG

化学信息

分子量	248.3
分子式	C₉H₁₆N₂O₄S
CAS No.	1009816-48-1
Smiles	[H][C@]12O[C@H](CO)[C@@H](O)[C@H](O)[C@@]1([H])N=C(NCC)S2
密度	1.74 g/cm3 (Predicted)

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

H2O: 50 mg/mL (201.37 mM), Sonication is recommended.

DMSO: 100 mg/mL (402.74 mM), Sonication is recommended.

溶液配制表

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	4.0274 mL	20.1369 mL	40.2739 mL	201.3693 mL
5 mM	0.8055 mL	4.0274 mL	8.0548 mL	40.2739 mL
10 mM	0.4027 mL	2.0137 mL	4.0274 mL	20.1369 mL
20 mM	0.2014 mL	1.0068 mL	2.0137 mL	10.0685 mL
50 mM	0.0805 mL	0.4027 mL	0.8055 mL	4.0274 mL
100 mM	0.0403 mL	0.2014 mL	0.4027 mL	2.0137 mL

体内实验配液计算器