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Pralidoxime chloride (2-PAM chloride) Sale

(Synonyms: 氯解磷定,2-PAM chloride) 目录号 : GC33684

An AChE reactivator

Pralidoxime chloride (2-PAM chloride) Chemical Structure

Cas No.:51-15-0

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥491.00
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100mg
¥446.00
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Sample solution is provided at 25 µL, 10mM.

Description

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)

化学性质

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
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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。
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。

溶解性数据

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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
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