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2-Deoxy-D-glucose 是一種葡萄糖類似物,為葡萄糖代謝抑制劑,通過作用于己糖激酶 (hexokinase) 來抑制糖酵解 (glycolysis)。
生物活性
2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase[1].
IC50 & Target:HSV-1
體外研究(In Vitro)
2-Deoxy-D-glucose (2-DG, 4, 8, or 16 mM) significantly reduces the level of ATP in MCF-7 cells in a dose- and time-dependent manner that paralleles the effects of 2-DG on cell growth. The levels of phosphorylated Akt are significantly decreased, whereas the levels of phosphorylated AMPK and Sirt-1 are significantly increased in MCF-7 cells exposed to 2-Deoxy-D-glucose at 4, 8, or 16 mM for 1, 3, or 5 days in a dose- and time-dependent manner[1]. 2-DG treatment increases the levels of pentose phosphate pathway (PPP) metabolites and augments the generation of NADPH by glucose-6-phosphate dehydrogenase. An increase in NADPH and upregulation of glutathione synthetase expression resultes in the increase in the reduced form of glutathione by 2-DG in NB4 cells[3].
體內(nèi)研究(In Vivo)
2-Deoxy-D-glucose (0.03%, w/w) causes a 7% decrease in final weight that is statistically significant, and delayes the appearance of palpable mammary carcinomas[1]. 2-Deoxy-D-glucose (3 mmol/kg, i.v.) is decreased in a dose-dependent manner in rat muscle[2].
Clinical Trial
NCT Number | Sponsor | Condition | Start Date | Phase |
---|---|---|---|---|
NCT00247403 | University of Iowa | October 2005 | Phase 1 | |
NCT00096707 | Threshold Pharmaceuticals | February 2004 | Phase 1 |
分子量:164.16
Formula:C6H12O5
CAS 號:154-17-6
中文名稱:2-脫氧-D-葡萄糖
運輸條件:Room temperature in continental US; may vary elsewhere.
儲存方式
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
溶解性數(shù)據(jù)
H2O : ≥ 24 mg/mL (146.20 mM)
* "≥" means soluble, but saturation unknown.
濃度溶劑體積質(zhì)量 | 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 |
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 儲存時,請在 6 個月內(nèi)使用,-20°C 儲存時,請在 1 個月內(nèi)使用。
請根據(jù)您的實驗動物和給藥方式選擇適當?shù)娜芙夥桨?。以下溶解方案都請先按?nbsp;In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)配,當天使用; 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶
請依序添加每種溶劑: PBS
Solubility: 130 mg/mL (791.91 mM); Clear solution; Need ultrasonic
參考文獻
2-Deoxy-D-glucose 是一種葡萄糖類似物,為葡萄糖代謝抑制劑,通過作用于己糖激酶 (hexokinase) 來抑制糖酵解 (glycolysis)。
生物活性
2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase[1].
IC50 & Target:HSV-1
體外研究(In Vitro)
2-Deoxy-D-glucose (2-DG, 4, 8, or 16 mM) significantly reduces the level of ATP in MCF-7 cells in a dose- and time-dependent manner that paralleles the effects of 2-DG on cell growth. The levels of phosphorylated Akt are significantly decreased, whereas the levels of phosphorylated AMPK and Sirt-1 are significantly increased in MCF-7 cells exposed to 2-Deoxy-D-glucose at 4, 8, or 16 mM for 1, 3, or 5 days in a dose- and time-dependent manner[1]. 2-DG treatment increases the levels of pentose phosphate pathway (PPP) metabolites and augments the generation of NADPH by glucose-6-phosphate dehydrogenase. An increase in NADPH and upregulation of glutathione synthetase expression resultes in the increase in the reduced form of glutathione by 2-DG in NB4 cells[3].
體內(nèi)研究(In Vivo)
2-Deoxy-D-glucose (0.03%, w/w) causes a 7% decrease in final weight that is statistically significant, and delayes the appearance of palpable mammary carcinomas[1]. 2-Deoxy-D-glucose (3 mmol/kg, i.v.) is decreased in a dose-dependent manner in rat muscle[2].
Clinical Trial
NCT Number | Sponsor | Condition | Start Date | Phase |
---|---|---|---|---|
NCT00247403 | University of Iowa | October 2005 | Phase 1 | |
NCT00096707 | Threshold Pharmaceuticals | February 2004 | Phase 1 |
分子量:164.16
Formula:C6H12O5
CAS 號:154-17-6
中文名稱:2-脫氧-D-葡萄糖
運輸條件:Room temperature in continental US; may vary elsewhere.
儲存方式
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
溶解性數(shù)據(jù)
H2O : ≥ 24 mg/mL (146.20 mM)
* "≥" means soluble, but saturation unknown.
濃度溶劑體積質(zhì)量 | 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 |
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 儲存時,請在 6 個月內(nèi)使用,-20°C 儲存時,請在 1 個月內(nèi)使用。
請根據(jù)您的實驗動物和給藥方式選擇適當?shù)娜芙夥桨浮R韵氯芙夥桨付颊埾劝凑?nbsp;In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)配,當天使用; 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶
請依序添加每種溶劑: PBS
Solubility: 130 mg/mL (791.91 mM); Clear solution; Need ultrasonic
參考文獻