描述
AOAA Hemihydrochloride 氨氧基乙酸半盐酸盐
产品标签
AOAA Hemihydrochloride 氨氧基乙酸半盐酸盐；AOA Hemihydrochloride；WSP-1 (Washington State Probe-1)；WSP-5；CBS抑制剂； GABA转氨酶抑制剂；CAS NO. 2921-14-4；
产品信息
|
产品名称 |
产品编号 | 规格 | 价格（元） |
|
Aminooxyacetic Acid Hemihydrochloride (AOAA Hemihydrochloride) 氨氧基乙酸半盐酸盐 |
MX5314-500MG |
500mg | 283 |
| MX5314-1G | 1g |
423 |
|
| MX5314-5G | 5g |
993 |
产品描述
氨氧基乙酸半盐酸盐（Aminooxyacetic Acid Hemihydrochloride, AOAA Hemihydrochloride）是GABA转氨酶抑制剂（Ki= 9.16μM），诱导大脑内GABA累积[1]。AOAA还能抑制胱硫醚β合成酶（CBS）和胱硫醚γ裂解酶（CSE）活性，IC50分别是8.5μM和1.1μM[2]。AOAA（100mg/kg）降低GABA转氨酶活性，不会对谷氨酸脱羧酶（GAD）活性产生影响，并且能提高大鼠大脑所有区域的GABA水平[3]。AOAA（13mg/kg）还能减低小鼠大脑的GABA转氨酶活性，以及增加GABA水平。AOAA抑制3-巯基丙酸、马钱子碱和戊四氮唑诱导的小鼠癫痫发作，ED50s分别是53、130和85mg/kg，然而，AOAA在烟囱试验中呈现神经毒性（ED50= 62mg/kg），且对小鼠有致命性（LD50=105mg/kg）[4]。AOAA还普遍用作苹果酸-天冬氨酸穿梭（Malate-aspartate shuttle, MAS）抑制剂，抑制C6胶质细胞的胞内ATP水平和改变细胞周期，还能减少糖酵解速率、胞外乳酸和丙酮酸水平[5]。
产品特性
| 同义名：Carboxymethoxylamine hemihydrochloride, AOAA hemihydrochloride, AOA hemihydrochloride, Aminooxyacetate hemihydrochloride; Aminooxyacetic Acid (hydrochloride);羧甲氧基胺半盐酸盐；羧基甲氧基胺半盐酸盐；氨氧基乙酸半盐酸盐； | |
| CAS NO：2921-14-4 | 化学名：2-(aminooxy)-acetic acid hemihydrochloride |
| 分子式：C2H5NO3• 1/2HCl |
分子量：109.3 |
纯度：≥95% |
外观：固体 |
| 溶解性：溶于DMSO（≥10mg/ml）、H2O（≥10mg/ml）、不溶于乙醇 | |
| 化学结构式： | |
保存与运输方法
保存：-20℃干燥保存，至少2年有效。
运输：室温运输。
注意事项
1）本品并非商业化的临床药物，仅用作科研用途，不得用作临床诊断或治疗，不得用于食品或药品，绝对禁止用在人身上。
2）为了您的安全和健康，请穿实验服并戴一次性手套操作。
储存液制备
| 质量
溶剂体积 浓度 |
1mg | 5mg | 10mg |
| 1mM | 9.1491 mL | 45.7457 mL | 91.4913 mL |
| 5mM | 1.8298 mL | 9.1491 mL | 18.2983 mL |
| 10mM | 0.9149 mL | 4.5746 mL | 9.1491 mL |
【温馨提示】：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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液置于-80°C密封避光干燥保存，约6个月有效；-20°C密封避光干燥保存，约1个月有效。
使用方法【源自文献，仅作参考】
| 文献1，Yang B, Su Y, Han S, Chen R, Sun R, Rong K, Long F, Teng H, Zhao J, Liu Q, Qin A. Aminooxyacetic acid hemihydrochloride inhibits osteoclast differentiation and bone resorption by attenuating oxidative phosphorylation. Front Pharmacol. 2022 Sep 30;13:980678. doi: 10.3389/fphar.2022.980678. PMID: 36249744; PMCID: PMC9561130.
体外研究（In Vitro Assay）： 细胞类型（Cell type）：Bone marrow-derived macrophages (BMMs) 配制方法（Formulation）：AOAA was dissolved in phosphate-buffered saline at a concentration of 20 mM at−20°C, and further diluted to working concentration using culture medium. 实验方法（Cell viability assay）：BMMs (7 × 103cells/well) were seeded into 96-well plates and cultured in complete α-MEM containing 30 ng/ml M-CSF andAOAA (0, 0.1, 0.2, 0.3, 0.4, and 0.5 mM) for 48 and 96 h.CCK-8 was used to measure cell viability. 体内研究（In Vivo Assay）： 动物模型（Animal Model）：Ovariectomized mouse model 实验方法（Assay）：Twenty-four C57BL/6J mice (females, 11-week-old) were randomly divided into four groups containing six mice each: sham (injected PBS), OVX + PBS (injected PBS), OVX + estrogen (injected 100 ng/kg E2), and OVX + AOAA (injected 5 mg/kg AOAA). The mice were anesthetized with 3% tribromoethanol; next, both the ovaries of all mice except those in the sham group were surgically excised.A week later, the mice received intraperitoneal injections of PBS, E2, or AOAA every 2 days for 6 weeks. |
| 文献2，Yan, J. et al. Inhibition of cystathionine β-synthetase suppresses sodium channel activities of dorsal root ganglion neurons of rats with lumbar disc herniation. Sci. Rep. 6, 38188; doi: 10.1038/srep38188 (2016).
体内研究（In Vivo Assay）： 动物模型（Animal Model）：LDH rats 实验方法（Assay）：Immediately after resolved in NS,AOAA was injected intrathecally at 10μg/kg body weight, once daily for 7 consecutive days. Same volume of NS was used as control.L5-6DRGs from LDH rats after AOAA treatment were collected either for measurement of NaV1.7 and NaV1.8 expression or for patch clamping studies. |
参考文献
[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] Löscher, W., Hönack, 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 acid. J. Neurochem. 53(6), 1737-1750 (1989)
[4]Löscher, W. A comparative study of the pharmacology of inhibitors of GABA-metabolism. Naunyn Schmiedebergs Arch. Pharmacol. 315(2), 119-128 (1980).
[5] Wang C., Chen H., Zhang M., Zhang J., Wei X., Ying W. (2016). 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. 378, 1–7. 10.1016/j.canlet.2016.05.001
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