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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAminooxyacetic acid hemihydrochlorideCat. No.: HY-107994CAS No.: 2921-14-4Synonyms: Carboxymethoxylamine Hemihydrochloride分式: NHOCHCOOH .HCl分量: 109.3作靶点: GABA Receptor作通路: Membrane Transporter/Ion Channel; Neuronal Signaling储存式:

2、 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性数据体外实验 DMSO : 42.9 mg/mL (392.50 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 9.1491 mL 45.7457 mL 91.4913 mL5 mM 1.8298 mL 9.1491 mL 18.2983 mL10 mM 0.9149 mL 4.5746 mL 9.

3、1491 mL请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液,并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案,配制前请先配制澄清的储备液,再依次添加助溶剂(为保证实验结果的可靠性,体内实验的作液,建议您现现配,当天使;澄清的储备液可以根据储存条件,适当保存;以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占):1. 请依序添加每种溶剂: 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.58 mg/mL (23.60 mM); Clear solution2. 请依序添加每种溶剂: 10

4、% DMSO 90% (20% SBE-CD in saline)Solubility: 2.58 mg/mL (23.60 mM); Clear solution3. 请依序添加每种溶剂: 10% DMSO 90% corn oilSolubility: 2.58 mg/mL (23.60 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Aminooxyacetic acid hemihydrochloride是苹果酸-天冬氨酸穿梭 (MAS) 抑制剂, 也能

5、抑制 GABA 降解酶GABA-T。IC50 & Target MAS 1, GABA-T 2体外研究 Aminooxyacetic acid hemihydrochloride (AOAA) dose-dependently decreases the survival of C6 glioma cells.Aminooxyacetic acid hemihydrochloride treatment produces a significant increase in the percentage of thecells arrested in the stage of G0/G1, as

6、 well as a significant decrease in the percentage of the cells at Sphase and G2/M phase. Aminooxyacetic acid hemihydrochloride treatment leads to an obvious decrease inthe number of the cells in the phase of cell division. Aminooxyacetic acid hemihydrochloride significantlyincreases the percentage o

7、f the cells in both early-stage apoptosis and necrosis. Treatment of the cells with1mM or 5mM Aminooxyacetic acid hemihydrochloride leads to decreased levels of aging of the cells 1.Glutamine-dependent cell lines show greater inhibition of cell growth by Aminooxyacetic acidhemihydrochloride (AOA) co

8、mpare with cells that are less glutamine dependent 3.体内研究 The accumulation of GABA in cerebellum and whole brain is initially very rapid, being significantly increasedalready 5 min after the injection of Aminooxyacetic acid hemihydrochloride (AOAA). The rapid initialaccumulation becomes gradually sl

9、ower and maximal levels (400 to 600 % of the control levels) are reached2 to 6 h after Aminooxyacetic acid hemihydrochloride. Still 24 h after Aminooxyacetic acid hemihydrochloridethe GABA levels are elevated by about 250%. From 2 to 6 h after Aminooxyacetic acid hemihydrochloride theconvulsions are

10、 completely blocked. Twenty four hours after Aminooxyacetic acid hemihydrochloride theconvulsions are almost identical to the controls 2.PROTOCOLKinase Assay 3 Enzyme activity of aspartate transaminase is measured by a colorimetric assay assessing formation ofpyruvate from oxaloacetate, a product of

11、 GOT1/2 (also called AST1/2) activity, as described previously. Inbrief, cells grown in 6-well plates are collected after 6, 24, or 48 hours of Aminooxyacetic acidhemihydrochloride (AOA) treatment and washed with cold PBS, lysed, and supernatant used for analysis 3.MCE has not independently confirme

12、d the accuracy of these methods. They are for reference only.Cell Assay 3 Breast cancer cell lines are used in this study. Cells are plated in 96-well plates at 1,500 to 5,000 cells perwell in 100 L media. New medium with varying concentration of Aminooxyacetic acid hemihydrochloride(AOA) is added a

13、fter 12 hours. The assay is performed after 48 hours 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Female albino rats (150 to 200 g) bred at our department are used. Aminooxyacetic acid hemihydrochlorideAdministration 2 (AOAA) is injected int

14、o a tail vein (2 mL/kg body weight). For this purpose the rat is placed in a plastic tubeand the tail warmed in water 42C 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE户使本产品发表的科研献 Am J Transl Res. 201

15、8 Dec 15;10(12):4247-4257.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Wang C, et al. Malate-aspartate shuttle inhibitor aminooxyacetic acid leads to decreased intracellular ATP levels and altered cell cycle ofC6 glioma cells by inhibiting glycolysis. Cancer Lett. 2016 Aug 1

16、;378(1):1-7.2. Pagliusi SR, et al. Aminooxyacetic acid induced accumulation of GABA in the rat brain. Interaction with GABA receptors and distributionin compartments. Naunyn Schmiedebergs Arch Pharmacol. 1983 Apr;322(3):210-5.3. Korangath P, et al. Targeting Glutamine Metabolism in Breast Cancer with Aminooxyacetate. Cli

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