Pralidoxime chloride (2-PAM chloride)
(Synonyms: 氯解磷定,2-PAM chloride) 目录号 : GC33684An AChE reactivator
Cas No.:51-15-0
Sample solution is provided at 25 µL, 10mM.
Pralidoxime reactivates acetylcholinesterase (AChE) that has been deactivated by binding of organophosphates to its esteratic site.1 Pralidoxime binds to the anionic site of AChE and displaces the phosphate from the esteratic site through formation of phosphate-pralidoxime conjugates. It reactivates paraoxon- and diisopropyl fluorophosphate-inactivated human red blood cell (RBC) AChE with IC50 shifts of 0.3 and 0.8 nM per μM of pralidoxime, respectively.2,3 At a concentration of 10 μM, it reactivates human RBC AChE that has been inactivated by chlorpyrifos , diazinon , and malathion by 17, 61, and 36%, respectively.4 Pralidoxime binds to sarin-bound hAChE (Kd = 25.72 μM) and inhibits sarin-induced AChE deactivation (IC50 = 1.21 mM) in hemoglobin-free erythrocyte ghosts.5 Formulations containing pralidoxime have been used to treat organophosphate poisoning.1
1.Jokanovi?, M., and Stojiljkovi?, M.P.Current understanding of the application of pyridinium oximes as cholinesterase reactivators in treatment of organophosphate poisoningEur. J. Pharmacol.553(1-3)10-17(2006) 2.Petroianu, G.A., Arafat, K., Kuca, K., et al.Five oximes (K-27, K-33, K-48, BI-6 and methoxime) in comparison with pralidoxime: In vitro reactivation of red blood cell acetylcholinesterase inhibited by paraoxonJ. Appl. Toxicol.26(1)64-71(2006) 3.Lorke, D.E., Hasan, M.Y., Arafat, K., et al.In vitro oxime protection of human red blood cell acetylcholinesterase inhibited by diisopropyl-fluorophosphateJ. Appl. Toxicol.28(4)422-429(2008) 4.Costa, M.D., Freitas, M.L., Soares, F.A., et al.Potential of two new oximes in reactivate human acetylcholinesterase and butyrylcholinesterase inhibited by organophosphate compounds: An in vitro studyToxicol. In Vitro25(8)2120-2123(2011) 5.Karade, H.N., Raviraju, G., Acharya, B.N., et al.Synthesis and in vitro reactivation study of isonicotinamide derivatives of 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide as reactivators of Sarin and VX inhibited human acetylcholinesterase (hAChE)Bioorg. Med. Chem.24(18)4171-4176(2016)
Cas No. | 51-15-0 | SDF | |
别名 | 氯解磷定,2-PAM chloride | ||
Canonical SMILES | C[N+]1=CC=CC=C1/C=N/O.[Cl-] | ||
分子式 | C7H9ClN2O | 分子量 | 172.61 |
溶解度 | DMSO : 11.33 mg/mL (65.64 mM) | 储存条件 | Store at -20°C |
General tips | 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。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 5.7934 mL | 28.967 mL | 57.9341 mL |
5 mM | 1.1587 mL | 5.7934 mL | 11.5868 mL |
10 mM | 0.5793 mL | 2.8967 mL | 5.7934 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet