|二氯乙酸钠|CsnPharm

CAS No.: 2156-56-1

二氯乙酸钠 Catalog No. CSN22561

Synonyms: 二氯乙酸钠;2,2-二氯乙酸钠

Sodium 2,2-dichloroacetate is a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50s of 183 and 80 μM for PDK2 and PDK4 respectively, with tumor growth inhibition properties.

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技术信息

生物活性

描述Sodium dichloroacetate (DCA) is a PDK(pyruvate dehydrogenase kinase) inhibitor and activates PDH(pyruvate dehydrogenase), the gatekeeper of glucose oxidation. Using an animal model of insulin-induced hypoglycemia and injected DCA (100 mg/kg, i.v., two days) following hypoglycemic insult. Histological evaluation was performed one week after hypoglycemia. DCA treatment reduced hypoglycemia-induced oxidative stress, microglial activation, blood-brain barrier disruption, and neuronal death compared to the vehicle-treated hypoglycemia group^[1]. DCA-induced neurotoxicity may be mitigated by naturally occurring antioxidants and by a specific class of muscarinic receptor antagonists^[2]. CEM/C1, CCRF/CEM, HL-60, HL-60/MX2 cells were exposed to DCA for 24 h. The sensitivity of each cell line to DCA is different and depends on the concentration. CEM/C1 was the most sensitive with an half-maximal inhibitory concentration (IC50) value of 30 mM, while HL-60/MX2 was the most resistant with an IC50 value of 75 mM^[3]. Combined administration of DCA + MTF (metformin) prolonged life span of animals with glioma by 50%. The positive result of antitumor activity of MTF alone and in combination with DCA correlated with a decrease in the mean platelet volume/platelet count (MPV/PLT) ratio by 75.0%^[4].
参考文献

[1] Kho AR, Choi BY, Lee SH, Hong DK, Jeong JH, Kang BS, Kang DH, Park KH, Park JB, Suh SW. The Effects of Sodium Dichloroacetate on Mitochondrial Dysfunction and Neuronal Death Following Hypoglycemia-Induced Injury. Cells. 2019 May 1;8(5):405
[2] Stacpoole PW, Martyniuk CJ, James MO, Calcutt NA. Dichloroacetate-induced peripheral neuropathy. Int Rev Neurobiol. 2019;145:211-238
[3] Abramek J, Bogucki J, Ziaja-Sołtys M, Stępniewski A, Bogucka-Kocka A. Effect of sodium dichloroacetate on apoptotic gene expression in human leukemia cell lines. Pharmacol Rep. 2019 Apr;71(2):248-256
[4] Prokhorova IV, Pyaskovskaya ON, Kolesnik DL, Solyanik GI. Influence of metformin, sodium dichloroacetate and their combination on the hematological and biochemical blood parameters of rats with gliomas C6. Exp Oncol. 2018 Oct;40(3):205-210

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 6.6259 mL
- 33.1293 mL
- 66.2586 mL
- 5 mM
- 1.3252 mL
- 6.6259 mL
- 13.2517 mL
- 10 mM
- 0.6626 mL
- 3.3129 mL
- 6.6259 mL

技术信息

CAS号

2156-56-1

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C2HCl2NaO2

运输

蓝冰

分子量

150.92

别名

二氯乙酸钠;2,2-二氯乙酸钠

溶解度

DMSO	28.0 mg/mL (185.5 mM)
Water	28.0 mg/mL (185.5 mM)
Ethanol	29.0 mg/mL (192.1 mM)

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二氯乙酸钠 Catalog No. CSN22561

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