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Asoxime (chloride)

 
Catalog No.
C4052
AChE重激活剂
组合的产品项目
规格价格库存 数量
10mg
¥ 1,787.00
Ship with 10-15 days
25mg
¥ 3,683.00
Ship with 10-15 days
50mg
¥ 5,687.00
Ship with 10-15 days

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背景

IC50: 8.9 μM: blocks AChE in human; 126 μM: inhibits acetylcholinesterase (AChE) in bovine; 160 μM: blocks muscarinic acetylcholine receptor M1, M2, M3 and M4 in mouse.

Asoxime, also known as HI-6, is an asymmetric bis-pyridinium aldoxime and reactivates AChE via nucleophilic attack of oximate anions on organophosphate-AChE conjugates.

AChE, one of the primary targets of organophosphates, is inactivated by organophosphates via reacting covalently with the active center serine, which blocks the hydrolyzation of acetylcholine at peripheral and central synapses. Additionally, the accumulation of acetylcholine leads to an over-stimulation of cholinergic receptors, which disrupts a variety of biological functions.

In vitro: HI-6 showed a bacteriostatic effect on Francisella tularensis (F. tularensis) and inhibited the growth of F. tularensis when treated with 100 mM HI-6 [1].

In vivo: Female BALB/c mice, infected by F. tularensis, were administrated subcutaneously with 100 μl HI-6 for ten days. The lower dose of HI-6 yielded in different symptoms and mortality. Compared to mice injected only with tularemia, groups of mice exposed to the lower dose of HI-6 showed a decline in mortality, which can be explained via higher efficacy of bacteriostatic effect while the toxic effect was decreased [1]. Female Wistar rats were treated intramuscularly with HI-6 at a dose of 15.6 or 156 mg/kg for one day. The level of thiobarbituric acid reactive substances was increased, which was triggered by HI-62 [2].

References:
[1].  Pohanka, M., Pavli, O., Pikula, J., Treml, F., & Kuca, K. Modulation of Tularemia Disease Progress by the Bisquaternary Pyridinium Oxime HI-6. Acta Veterinaria Brno. 2010; 79(3): 443-448.
[2].  Pohanka, M., Sobotka, J., Svobodova, H., & Stetina, R. Sulfur mustard induced oxidative stress and its alteration using asoxime (HI-6). Interdisciplinary Toxicology. 2013; 6(4).

化学属性

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt359.2
Cas No.34433-31-3
FormulaC14H16N4O3·2Cl
SynonymsHI-6
Solubility≤10mg/ml in PBS(pH7.2)
Chemical Name1-[[[4-(aminocarbonyl)pyridinio]methoxy]methyl]-2-[(hydroxyimino)methyl]-pyridinium, dichloride
SDFDownload SDF
Canonical SMILESO/N=C\C1=CC=CC=[N+]1COC[N+]2=CC=C(C(N)=O)C=C2.[Cl-].[Cl-]
运输条件 蓝冰运输或根据您的需求运输。
一般建议不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

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化学结构

Asoxime (chloride)