氨氧基乙酸半盐酸盐作用机制 - Medchemexpress - MCE中国

1、Product Data SheetAminooxyacetic acid hemihydrochlorideCat. No.: HY-107994CAS No.: 2921-14-4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: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect from light)溶解性数据体外实验 H2O

2、: 100 mg/mL (914.91 mM; Need ultrasonic)DMSO : 42.9 mg/mL (392.50 mM; Need ultrasonic and warming)SolventMass1 mg 5 mg 10 mgConcentration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 9.1491 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；旦配成溶液，请分装保存，避免反复冻融造成的产品失

3、效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month (protect from light)。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。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。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 4

4、0% PEG300 5% Tween-80 45% salineSolubility: 2.58 mg/mL (23.60 mM); Clear solution此案可获得 2.58 mg/mL (23.60 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.8 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.58

5、mg/mL (23.60 mM); Clear solution此案可获得 2.58 mg/mL (23.60 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.8 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合Page 1 of 2 www.MedChemE均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.58 mg/mL (23.60 mM); Clear solution此案可获得 2.58 mg/mL (23.60 mM，饱和度未知) 的澄 溶液，此案不适于

6、实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 25.8 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Aminooxyacetic acid hemihydrochloride是苹果酸-天冬氨酸穿梭 (MAS) 抑制剂, 也能抑制 GABA 降解酶 GABA-T。IC & Target MAS1, GABA-T2体外研究 Aminooxyacetic acid hemihydrochloride (AOAA) dose-dependently decreases the survival of C6 gl

7、ioma cells.Aminooxyacetic acid hemihydrochloride treatment produces a significant increase in the percentage of the cellsarrested in the stage of G0/G1, as well as a significant decrease in the percentage of the cells at S phase and G2/Mphase. Aminooxyacetic acid hemihydrochloride treatment leads to

8、 an obvious decrease in the number of the cells inthe phase of cell division. Aminooxyacetic acid hemihydrochloride significantly increases the percentage of the cells inboth early-stage apoptosis and necrosis. Treatment of the cells with 1 mM or 5 mM Aminooxyacetic acidhemihydrochloride leads to de

9、creased levels of aging of the cells1. Glutamine-dependent cell lines show greaterinhibition of cell growth by Aminooxyacetic acid hemihydrochloride (AOA) compare with cells that are less glutaminedependent3.体内研究 The accumulation of GABA in cerebellum and whole brain is initially very rapid, being s

10、ignificantly increased already 5min after the injection of Aminooxyacetic acid hemihydrochloride (AOAA). The rapid initial accumulation becomesgradually slower and maximal levels (400 to 600 % of the control levels) are reached 2 to 6 h after Aminooxyaceticacid hemihydrochloride. Still 24 h after Am

11、inooxyacetic acid hemihydrochloride the GABA levels are elevated byabout 250%. From 2 to 6 h after Aminooxyacetic acid hemihydrochloride the convulsions are completely blocked.Twenty four hours after Aminooxyacetic acid hemihydrochloride the convulsions are almost identical to the controls2.PROTOCOL

12、Kinase Assay 3 Enzyme activity of aspartate transaminase is measured by a colorimetric assay assessing formation of pyruvate fromoxaloacetate, a product of GOT1/2 (also called AST1/2) activity, as described previously. In brief, cells grown in 6-wellplates are collected after 6, 24, or 48 hours of A

13、minooxyacetic acid hemihydrochloride (AOA) treatment and washedwith cold PBS, lysed, and supernatant used for analysis3.MCE has not independently confirmed 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-

14、well plates at 1,500 to 5,000 cells per well in 100 L media. New medium with varying concentration of Aminooxyacetic acid hemihydrochloride (AOA) is added after 12hours. The assay is performed after 48 hours3.MCE has not independently confirmed the accuracy of these methods. They are for reference o

15、nly.Animal Female albino rats (150 to 200 g) bred at our department are used. Aminooxyacetic acid hemihydrochloride (AOAA)Administration 2 is injected into a tail vein (2 mL/kg body weight). For this purpose the rat is placed in a plastic tube and the tailwarmed in water 42C2.MCE has not independent

16、ly confirmed the accuracy of these methods. They are for reference only.Page 2 of 3 www.MedChemE户使本产品发表的科研献 Am J Transl Res. 2018 Dec 15;10(12):4247-4257.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Wang C, et al. Malate-aspartate shuttle inhibitor aminooxyacetic

17、acid leads to decreased intracellular ATP levels and altered cell cycle of C6 glioma cellsby inhibiting glycolysis. Cancer Lett. 2016 Aug 1;378(1):1-7.2. Pagliusi SR, et al. Aminooxyacetic acid induced accumulation of GABA in the rat brain. Interaction with GABA receptors and distribution incompartments. Naunyn Schmiedebergs Arch Pharmacol. 1983 Apr;322(3):210-5.3. Korangath P, et al. Targeting Glutamine Metabolism in Breast Cancer with Aminooxyacetate. C