|(R)-2-羟基戊二酸钠|CsnPharm

CAS No.: 103404-90-6

(R)-2-羟基戊二酸二钠盐 Catalog No. CSN10737

Synonyms: Disodium (R)-2-hydroxyglutarate;(R)-2-Hydroxyglutaric acid disodium salt;D-α-Hydroxyglutaric Acid (sodium salt)

D-alpha-Hydroxyglutaric Acid Disodium is a multiple-target inhibitor of KDM4A and α-Ketoglutarate(α-KG)-dependent dioxygenase, as well as an NF-κB activator.

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技术信息

生物活性

描述D-alpha-Hydroxyglutaric acid disodium is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-alpha-Hydroxyglutaric acid ((R)-2-hydroxyglutarate) accumulates in human cancers carrying neomorphic mutations in the isocitrate dehydrogenase (IDH) 1 and 2 genes. Tumor-derived IDH1 and IDH2 mutations reduce alpha-KG and accumulate an α-KG antagonist, 2-HG, leading to genome-wide histone and DNA methylation alterations. D-α-Hydroxyglutaric acid is a weak inhibitor of TET hydroxylases. In the presence of 0.1 mM of alpha-KG, addition of 10 mM D-alpha-Hydroxyglutaric acid results in a partial (33%) inhibition of TET2 and addition of 50 mM D-α-Hydroxyglutaric acid results in more inhibition (83%) of TET2. D-alpha-Hydroxyglutaric acid exhibits a less pronounced inhibitory effect toward TET1^[3]. D-α-Hydroxyglutaric acid strongly inhibits glucose utilization, CO2 production and the respiratory chain in rat cerebral cortex and human skeletal muscle, as well as in submitochondrial particles from bovine heart, suggesting an impairment of the aerobic metabolism. D-α-Hydroxyglutaric acid has also been proposed as an endogenous excitotoxic organic acid because it significantly decreased cell viability in neuronal cultures from chick embryo telencephalons and from neonatal rat hippocampus through stimulation of specific NMDA glutamate receptors^[4].
参考文献

[1] Fu X, Chin RM, et al. 2-Hydroxyglutarate Inhibits ATP Synthase and mTOR Signaling. Cell Metab. 2015 Sep 1;22(3):508-15.
[2] Xu W, Yang H, et al. Oncometabolite 2-hydroxyglutarate is a competitive inhibitor of α-ketoglutarate-dependent dioxygenases. Cancer Cell. 2011 Jan 18;19(1):17-30.
[3] Xu W, Yang H, Liu Y, Yang Y, Wang P, Kim SH, Ito S, Yang C, Wang P, Xiao MT, Liu LX, Jiang WQ, Liu J, Zhang JY, Wang B, Frye S, Zhang Y, Xu YH, Lei QY, Guan KL, Zhao SM, Xiong Y. Oncometabolite 2-hydroxyglutarate is a competitive inhibitor of α-ketoglutarate-dependent dioxygenases. Cancer Cell. 2011 Jan 18;19(1):17-30
[4] Latini A, Scussiato K, Rosa RB, Llesuy S, Belló-Klein A, Dutra-Filho CS, Wajner M. D-2-hydroxyglutaric acid induces oxidative stress in cerebral cortex of young rats. Eur J Neurosci. 2003 May;17(10):2017-22

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
- 5.2062 mL
- 26.0308 mL
- 52.0616 mL
- 5 mM
- 1.0412 mL
- 5.2062 mL
- 10.4123 mL
- 10 mM
- 0.5206 mL
- 2.6031 mL
- 5.2062 mL

技术信息

CAS号

103404-90-6

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C5H6Na2O5

运输

蓝冰

分子量

192.08

别名

Disodium (R)-2-hydroxyglutarate;(R)-2-Hydroxyglutaric acid disodium salt;D-α-Hydroxyglutaric Acid (sodium salt);D-2-HG;D-2-Hydroxyglutaric Acid;MDK-4906;(R)-2-羟基戊二酸二钠盐

溶解度

DMSO	insoluble
Water	310.0 mg/mL (1613.9 mM)

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(R)-2-羟基戊二酸二钠盐 Catalog No. CSN10737

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