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Aminooxyacetic acid hemihydrochloride (Carboxymethoxylamine Hemihydrochloride) Sale

(Synonyms: 氨氧基乙酸半盐酸盐; Carboxymethoxylamine hemihydrochloride; Aminooxyacetate hemihydrochloride) 目录号 : GC34064

A GABA-T inhibitor

Aminooxyacetic acid hemihydrochloride (Carboxymethoxylamine Hemihydrochloride) Chemical Structure

Cas No.:2921-14-4

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥495.00
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1g
¥693.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Kinase experiment:

Enzyme activity of aspartate transaminase is measured by a colorimetric assay assessing formation of pyruvate from oxaloacetate, a product of GOT1/2 (also called AST1/2) activity, as described previously. In brief, cells grown in 6-well plates are collected after 6, 24, or 48 hours of Aminooxyacetic acid hemihydrochloride (AOA) treatment and washed with cold PBS, lysed, and supernatant used for analysis[3].

Cell experiment:

Breast cancer cell lines are used in this study. Cells are plated in 96-well plates at 1,500 to 5,000 cells per well in 100 μL media. New medium with varying concentration of Aminooxyacetic acid hemihydrochloride (AOA) is added after 12 hours. The assay is performed after 48 hours[3].

Animal experiment:

Female albino rats (150 to 200 g) bred at our department are used. Aminooxyacetic acid hemihydrochloride (AOAA) is injected into a tail vein (2 mL/kg body weight). For this purpose the rat is placed in a plastic tube and the tail warmed in water 42°C[2].

References:

[1]. Wang C, et al. Malate-aspartate shuttle inhibitor aminooxyacetic acid leads to decreased intracellular ATP levels and altered cell cycle of C6 glioma cells by 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 in compartments. Naunyn Schmiedebergs Arch Pharmacol. 1983 Apr;322(3):210-5.
[3]. Korangath P, et al. Targeting Glutamine Metabolism in Breast Cancer with Aminooxyacetate. Clin Cancer Res. 2015 Jul 15;21(14):3263-73.

产品描述

Aminooxyacetic acid is a GABA transaminase (GABA-T) inhibitor (Ki = 9.16 μM) that induces GABA accumulation in the brain.1 It also inhibits cystathionine β synthase (CBS) and cystathionine γ lyase (CSE; IC50s = 8.5 and 1.1 μM, respectively).2 Aminooxyacetic acid (100 mg/kg) decreases GABA-T activity, without affecting glutamic acid decarboxylase (GAD) activity, and increases GABA levels in all regions of rat brain.3 It also decreases GABA-T activity and increases GABA in mouse brain when administered at a dose of 13 mg/kg.4 Aminooxyacetic acid inhibits 3-mercaptopropionic acid-, strychnine-, and pentetrazole-induced seizures in mice (ED50s = 53, 130, and 85 mg/kg, respectively), however, it exhibits neurotoxicity in the chimney test (ED50 = 62 mg/kg) and is lethal (LD50 = 105 mg/kg) to mice.

1.Wallach, D.P.Studies on the GABA pathway. I. The inhibition of γ-aminobutyric acid-α-ketoglutaric acid transaminase in vitro and in vivo by U-7524 (amino-oxyacetic acid)Biochem. Pharmacol.5(4)323-331(1961) 2.Asimakopoulou, A., Panopoulos, P., Chasapis, C.T., et al.Selectivity of commonly used pharmacological inhibitors for cystathionine β synthase (CBS) and cystathionine γ lyase (CSE)Br. J. Pharmacol.169(4)922-932(2013) 3.L?scher, W., H?nack, D., and Gramer, M.Use of inhibitors of gamma-aminobutyric acid (GABA) transaminase for the estimation of GABA turnover in various brain regions of rats: A reevaluation of aminooxyacetic acidJ. Neurochem.53(6)1737-1750(1989) 4.L?scher, W.A comparative study of the pharmacology of inhibitors of GABA-metabolismNaunyn Schmiedebergs Arch. Pharmacol.315(2)119-128(1980)

Chemical Properties

Cas No. 2921-14-4 SDF
别名 氨氧基乙酸半盐酸盐; Carboxymethoxylamine hemihydrochloride; Aminooxyacetate hemihydrochloride
Canonical SMILES OC(CON)=O.[H]Cl.OC(CON)=O
分子式 NH2OCH2COOH · 0.5HCl 分子量 109.3
溶解度 DMSO : 42.9 mg/mL (392.50 mM) 储存条件 4°C, protect from light
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1 mM 9.1491 mL 45.7457 mL 91.4913 mL
5 mM 1.8298 mL 9.1491 mL 18.2983 mL
10 mM 0.9149 mL 4.5746 mL 9.1491 mL
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Research Update

Effects of barbiturates on the decerebrate rigidity in rats

J Pharmacobiodyn 1982 Sep;5(9):643-52.PMID:7153837DOI:10.1248/bpb1978.5.643

Effects of barbiturates (phenobarbital, mephobarbital, pentobarbital, hexobarbital and amobarbital) on the tonic and phasic responses of forelimbs were studied in the rats in which rigidity was induced by means of anemic decerebration. The inhibitory pattern of the tonic and phasic responses to phenobarbital was different from those to the other barbiturates, i.e. phenobarbital gradually inhibited both tonic and phasic responses, whereas other barbiturates suppressed significantly only the tonic response immediately after the administration of a relatively low dose (10 mg/kg) but hardly inhibited the phasic response unless at higher doses (20 and 40 mg/kg). Possible involvement of GABA-system in the inhibitory action of phenobarbital and pentobarbital on the rigidity was investigated. Since inhibition of the phasic response to pentobarbital was potentiated by the pretreatment of animals with Carboxymethoxylamine Hemihydrochloride (AOAA) and suppressed by the pretreatment with semicarbazide, it was suggested that GABAergic mechanism may be involved in the particular inhibition of phasic response to pentobarbital. However, the inhibitory action of phenobarbital appeared to be independent of GABA-system.