氨氧基乙酸半鹽酸鹽作用機制 - Medchemexpress - MCE中國

1、Product Data SheetAminooxyacetic acid hemihydrochlorideCat. No.: HY-107994CAS No.: 2921-14-4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: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect from light)溶解性數(shù)據(jù)體外實驗 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 9.1491 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；旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失

3、效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month (protect from light)。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都請先按?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 4

4、0% PEG300 5% Tween-80 45% salineSolubility: 2.58 mg/mL (23.60 mM); Clear solution此案可獲得 2.58 mg/mL (23.60 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.8 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.58

5、mg/mL (23.60 mM); Clear solution此案可獲得 2.58 mg/mL (23.60 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.8 mg/mL 的澄 DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合Page 1 of 2 www.MedChemE均勻。3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.58 mg/mL (23.60 mM); Clear solution此案可獲得 2.58 mg/mL (23.60 mM，飽和度未知) 的澄 溶液，此案不適于

6、實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 25.8 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Aminooxyacetic acid hemihydrochloride是蘋果酸-天冬氨酸穿梭 (MAS) 抑制劑, 也能抑制 GABA 降解酶 GABA-T。IC & Target MAS1, GABA-T2體外研究 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.體內(nèi)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戶使本產(chǎn)品發(fā)表的科研獻 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