| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| 2g |
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| 5g | |||
| Other Sizes |
Purity: ≥98%
| Targets |
The primary target of Pralidoxime Chloride is acetylcholinesterase (AChE) that has been inhibited by organophosphate compounds. It reactivates AChE by removing the phosphoryl group from the enzyme's active site, restoring its ability to hydrolyze acetylcholine and normalizing nerve function.
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| ln Vitro |
In vitro, Pralidoxime Chloride reactivates organophosphate-inhibited acetylcholinesterase. The compound is evaluated for its ability to restore AChE activity in enzyme preparations or cell lysates treated with organophosphates. Reactivation efficiency is measured by enzymatic assays.
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| ln Vivo |
Mice that have had their respiratory toxicity caused by paraoxon can recover with a single intramuscular injection of pralidoxime chloride (10–150 mg/kg) [3].
In vivo, Pralidoxime Chloride is used to treat poisoning by organophosphate pesticides and chemicals. It is often administered in combination with atropine to manage pesticide poisoning. It reverses toxic effects such as muscle weakness and respiratory distress by restoring nerve function. |
| Enzyme Assay |
For in vitro enzyme assays, Pralidoxime Chloride is tested against organophosphate-inhibited AChE. Standard protocols involve incubating the inhibited enzyme with varying concentrations of Pralidoxime Chloride (0.1-100 µM) and measuring the recovery of AChE activity using a chromogenic substrate (e.g., Ellman's reagent). Reactivation rates are calculated.
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| Cell Assay |
Cell-based assays for Pralidoxime Chloride are not typically performed as the compound acts extracellularly on AChE. However, neuronal cell lines may be used to assess the compound's ability to restore cholinergic signaling after organophosphate exposure. Standard protocols involve treating cells with organophosphates followed by Pralidoxime Chloride and measuring AChE activity.
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| Animal Protocol |
Animal/Disease Models: F1B6D2 mice (male, subcutaneous injection of diethyl paraoxon) [3]
Doses: 10, 50, 100 and 150 mg/kg Route of Administration: intramuscularadministration, once Experimental Results:50 mg Induction partial but Completely reverses respiratory toxicity/kg and completely reverses diethyl paraoxon-induced respiratory toxicity in mice at a dose of 150 mg/kg. In vivo studies with Pralidoxime Chloride are conducted in animal models of organophosphate poisoning. Typical protocols involve administering the organophosphate followed by Pralidoxime Chloride (10-50 mg/kg) via intravenous or intramuscular injection. Efficacy is assessed by survival, recovery of AChE activity, and reversal of clinical signs. |
| ADME/Pharmacokinetics |
The pharmacokinetic properties of Pralidoxime Chloride have been well characterized. It is administered intravenously or intramuscularly. It has a short half-life and is rapidly excreted in urine. It does not readily cross the blood-brain barrier. PK parameters including Cmax, Tmax, and half-life are established.
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| Toxicity/Toxicokinetics |
Toxicology data for Pralidoxime Chloride are available from preclinical and clinical studies. The compound is generally well-tolerated at therapeutic doses. Common side effects include dizziness, blurred vision, and tachycardia. At high doses, it may cause neuromuscular blockade. Comprehensive toxicology data are available.
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| References | |
| Additional Infomation |
Pralidoxime chloride is a pyridine salt and an organochloride salt. It is a cholinesterase reactivator and a cholinergic drug. It contains the pralidoxime structural unit. See also: pralidoxime (containing the active moiety); atropine; pralidoxime chloride (component).
Pralidoxime Chloride is an antidote to organophosphate poisoning used clinically. It is often administered with atropine. Synonyms include 2-PAM chloride and pyridinium, 2-[(hydroxyimino)methyl]-1-methyl-, chloride. It is available as an FDA-approved drug for the treatment of organophosphate poisoning. |
| Molecular Formula |
C7H9CLN2O
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|---|---|
| Molecular Weight |
172.61
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| Exact Mass |
172.04
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| CAS # |
51-15-0
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| Related CAS # |
Pralidoxime;6735-59-7
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| PubChem CID |
135445761
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| Appearance |
White to off-white solid powder
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| Boiling Point |
189.7ºC at760mmHg
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| Melting Point |
215-225 ºC
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| Flash Point |
68.5ºC
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
11
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| Complexity |
125
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C[N+]1=CC=CC=C1/C=N/O.[Cl-]
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| InChi Key |
HIGSLXSBYYMVKI-NAFXZHHSSA-N
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| InChi Code |
InChI=1S/C7H8N2O.ClH/c1-9-5-3-2-4-7(9)6-8-10/h2-6H,1H31H/b7-6-
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| Chemical Name |
[(E)-(1-methylpyridin-2-ylidene)methyl]-oxoazaniumchloride
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| Synonyms |
Pralidoxime Chloride 2-PAM chloride Pralidoxime Pralidoxine chloride ComboPen Protopam chloride pralidoxime, 14C-labeled pralidoxime methyl sulfate pralidoxime nitrate (1
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ≥ 100 mg/mL (~579.34 mM)
DMSO : ~21.67 mg/mL (~125.54 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.17 mg/mL (12.57 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.17 mg/mL (12.57 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.17 mg/mL (12.57 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.7934 mL | 28.9670 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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