2-Deoxy-D-glucose 2-脱氧-D-葡萄糖

生物活性

2-Deoxy-D-glucose (2-DG) 是一种葡萄糖类似物，为葡萄糖代谢抑制剂，通过作用于己糖激酶 (hexokinase) 来抑制糖酵解 (glycolysis)。在所有 16 种肿瘤细胞系中，DG 摄取量与 3-O-MG 转运之间有明显的相关性（p = 0.0012，F 检验），但 DG 摄取量与己糖激酶活性之间没有相关性。肿瘤细胞的己糖激酶活性与处于指数生长期的人类成纤维细胞相当。胰岛素（ED(50) = 0.6 mU/ml）能以剂量依赖的方式增加离体大鼠比目鱼肌中经 2-脱氧葡萄糖（2DG）培养后的 2DG6P 含量，最大反应量约为体外基础含量的 5 倍。2-DG increased mitochondrial dysfunction and upregulated Bax/Bcl-2, promoting cytochrome c release to initiate procaspase 3 cleavage induced by buforin IIb.

2-DG plus BCNU significantly suppressed tumor growth with lower side effects compared with BCNU alone in tumor-bearing mice. 2-DG also exerts anticonvulsant effects in vivo against perforant path kindling in rats.

Rats fed the 2-DG diet exhibited significant reductions in resting BP, attenuated BP responses during stress, and accelerated recovery to baseline after stress. Plasma concentrations of ACTH and corticosterone were elevated under nonstress conditions in rats fed the 2-DG diet and exhibited differential responses to single (enhanced response) and multiple (reduced response) stress sessions compared with rats fed control rat chow ad libitum. The 2-DG diet improved glucose metabolism, as indicated by decreased concentrations of blood glucose and insulin under nonstress conditions, but glucose and insulin responses to stress were maintained.

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化学性质

分子量	164.16
分子式	C6H12O5
CAS号	154-17-6
溶解性（25°C）	Water 30 mg/mL DMSO 15 mg/mL
储存条件	粉末型式       -20°C   3年；4°C   2年 溶于溶剂       -80°C   6个月；-20°C   1个月
运输方式	冰袋运输，根据产品的不同，可能会有相应调整。

储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	6.0916 mL	30.4581 mL	60.9162 mL
5 mM	1.2183 mL	6.0916 mL	12.1832 mL
10 mM	0.6092 mL	3.0458 mL	6.0916 mL

不同实验动物依据体表面积的等效剂量转换表（参考来源于公开文献）

	小鼠	大鼠	兔	豚鼠	仓鼠	狗
重量 (kg)	0.02	0.15	1.8	0.4	0.08	10
体表面积 (m2)	0.007	0.025	0.15	0.05	0.02	0.5
Km 系数	3	6	12	8	5	20

动物 A (mg/kg) = 动物 B (mg/kg) ×	动物 B的Km系数
	动物 A的Km系数

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Ueyama A,et.al. Biol Signals Recept Nonradioisotope assay of glucose uptake activity in rat skeletal muscle using enzymatic measurement of 2-deoxyglucose 6-phosphate in vitro and in vivo.

[2] Waki A,et.al. Nucl Med Biol The importance of glucose transport activity as the rate-limiting step of 2-deoxyglucose uptake in tumor cells in vitro.