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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作靶點: GABA Receptor作通路: Membrane Transporter/Ion Channel; Neuronal Signaling儲存式:

2、 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性數(shù)據(jù)體外實驗 DMSO : 42.9 mg/mL (392.50 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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,并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?,配制前請先配制澄清的儲備液,再依次添加助溶?為保證實驗結(jié)果的可靠性,體內(nèi)實驗的作液,建議您現(xiàn)現(xiàn)配,當天使;澄清的儲備液可以根據(jù)儲存條件,適當保存;以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占):1. 請依序添加每種溶劑: 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.58 mg/mL (23.60 mM); Clear solution2. 請依序添加每種溶劑: 10

4、% DMSO 90% (20% SBE-CD in saline)Solubility: 2.58 mg/mL (23.60 mM); Clear solution3. 請依序添加每種溶劑: 10% DMSO 90% corn oilSolubility: 2.58 mg/mL (23.60 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Aminooxyacetic acid hemihydrochloride是蘋果酸-天冬氨酸穿梭 (MAS) 抑制劑, 也能

5、抑制 GABA 降解酶GABA-T。IC50 & Target MAS 1, GABA-T 2體外研究 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.體內(nèi)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 您邊的抑制劑師www.MedChemE戶使本產(chǎn)品發(fā)表的科研獻 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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