| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
Acetylcholinesterase (ChE). Aldicarb sulfone inhibits acetylcholinesterase activity, preventing the breakdown of acetylcholine at synaptic junctions. This leads to the accumulation of acetylcholine and overstimulation of the nervous system, resulting in cholinergic toxicity. The compound is a carbamate ester that acts as a cholinesterase inhibitor.
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| ln Vitro |
Aldicarb sulfone is a potent acetylcholinesterase inhibitor in vitro. The compound inhibits the enzyme activity in a concentration-dependent manner. Its potency as a ChE inhibitor has been characterized in various in vitro assays using purified enzyme or tissue homogenates. The compound reduces the number of male T cells at 100 µg/mL.
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| ln Vivo |
In vivo, Aldicarb sulfone is highly toxic and may be fatal if inhaled, ingested, or absorbed through the skin. As a metabolite of aldicarb, it contributes to the overall toxicity of the parent pesticide. The compound causes cholinergic toxicity due to acetylcholinesterase inhibition, leading to symptoms such as muscle twitching, respiratory distress, and convulsions.
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| Enzyme Assay |
In vitro acetylcholinesterase inhibition assays for Aldicarb sulfone involve measuring ChE activity in the presence of varying concentrations of the compound. The enzyme is incubated with acetylthiocholine substrate, and the production of thiocholine is measured using Ellman's reagent (DTNB). IC50 values are determined from dose-response curves.
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| Cell Assay |
Cell-based assays are not typically performed with Aldicarb sulfone as it is a pesticide metabolite rather than a therapeutic agent. However, its effects on neuronal cells can be assessed by measuring acetylcholinesterase activity in cell lysates or by assessing cholinergic signaling in cultured neurons.
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| Animal Protocol |
In vivo animal studies for Aldicarb sulfone are typically conducted as part of toxicological evaluations. The compound is administered orally or via other routes, and toxicity endpoints such as mortality, clinical signs, and acetylcholinesterase inhibition are assessed. The compound is highly toxic and requires careful handling.
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| ADME/Pharmacokinetics |
Metabolism / Metabolites
Carbamates are enzymatically hydrolyzed in the liver; degradation products are excreted via the kidneys and liver. (L793) Aldicarb sulfone has a molecular weight of 222.26 and a molecular formula of C7H14N2O4S. It has a purity of ≥95%. The compound is soluble in DMSO at ≥34 mg/mL. It should be stored at -20°C. The compound is also known as Temik sulfone. |
| Toxicity/Toxicokinetics |
Toxicity Summary
Aldehydecarboxamide is a cholinesterase or acetylcholinesterase (AChE) inhibitor. Carbamate compounds carbamate the enzyme's active site, forming an unstable complex with cholinesterase. This inhibition is reversible. Cholinesterase inhibitors suppress the activity of acetylcholinesterase. Because acetylcholinesterase has important physiological functions, chemicals that interfere with its activity are potent neurotoxins, causing excessive salivation and lacrimation even at low doses. High-dose exposure typically results in symptoms such as headache, salivation, nausea, vomiting, abdominal pain, and diarrhea. Acetylcholinesterase breaks down the neurotransmitter acetylcholine, which is released at the neuromuscular junction, causing muscle or organ relaxation. Inhibition of acetylcholinesterase results in the accumulation and sustained action of acetylcholine, leading to continuous nerve impulse transmission and an inability to stop muscle contraction. Toxicity Data LC50 (rat) = 140 mg/m³/4hr Aldicarb sulfone is highly toxic and may be fatal if inhaled, ingested, or absorbed through the skin. It causes cholinergic toxicity due to acetylcholinesterase inhibition. The compound should be handled with extreme caution using appropriate personal protective equipment. Avoid any skin contact. It is a pesticide metabolite and is not intended for human therapeutic use. |
| Additional Infomation |
Aldicarb sulfone is a white crystalline solid belonging to the insecticide class. Aldicarb is a sulfone compound. Aldicarb is a carbamate insecticide. Carbamate insecticides are derived from carbamic acid, and their insecticidal mechanism is similar to that of organophosphate insecticides. They are widely used in homes, gardens, and agriculture. The first carbamate insecticide, Sevin, was introduced in 1956, and its global usage exceeds that of all other carbamate insecticides combined. Because Sevin has relatively low oral and dermal toxicity to mammals and a broad spectrum of control, it is widely used in lawns and gardens. Most carbamate insecticides are highly toxic to hymenopteran insects, so precautions must be taken to prevent contact with insects such as bees or parasitic wasps. Some carbamate insecticides can be transported within plants, making them effective systemic treatments. (L795)
Aldicarb sulfone is a metabolite and degradation product of the carbamate pesticide aldicarb. It is more toxic than the parent compound and inhibits acetylcholinesterase activity. The compound is highly toxic and requires careful handling. It is not a therapeutic agent and is used primarily in toxicological and environmental research. |
| Molecular Formula |
C7H14N2O4S
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|---|---|
| Molecular Weight |
222.26206
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| Exact Mass |
222.067
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| CAS # |
1646-88-4
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| Related CAS # |
Aldicarb sulfone-13C2,d3;1261170-76-6
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| PubChem CID |
9570093
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Melting Point |
132-135ºC
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| Index of Refraction |
1.495
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| LogP |
-0.57
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
14
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| Complexity |
326
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)(/C=N/OC(=O)NC)S(=O)(=O)C
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| InChi Key |
YRRKLBAKDXSTNC-WEVVVXLNSA-N
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| InChi Code |
InChI=1S/C7H14N2O4S/c1-7(2,14(4,11)12)5-9-13-6(10)8-3/h5H,1-4H3,(H,8,10)/b9-5+
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| Chemical Name |
[(E)-(2-methyl-2-methylsulfonylpropylidene)amino] N-methylcarbamate
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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 |
| 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) |
DMSO : ≥ 34 mg/mL (~152.97 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.25 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 25.0 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: ≥ 2.5 mg/mL (11.25 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 25.0 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: ≥ 2.5 mg/mL (11.25 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 | 4.4992 mL | 22.4962 mL | 44.9924 mL | |
| 5 mM | 0.8998 mL | 4.4992 mL | 8.9985 mL | |
| 10 mM | 0.4499 mL | 2.2496 mL | 4.4992 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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