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| 25mg |
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| 50mg |
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| Targets |
Fluensulfone targets plant-parasitic nematodes, which are microscopic roundworms that infest crop roots and threaten food security. The compound's mode of action has not been definitively established, but it is thought to disrupt the nervous system of nematodes. A leading hypothesis proposes that fluensulfone disrupts mitochondrial β-oxidation of fatty acids, specifically targeting medium-chain acyl-CoA dehydrogenases (MCADs). Other potential targets include acetylcholinesterase and glutamate-gated chloride channels.
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| ln Vitro |
Fluensulfone at lower concentrations slows down development: 100 μM A small delay is caused by fluensulfone because at 66 hours, fewer worms have reached the adult stage. At 300 μM, however, at 66 hours, no worms have reached the adult stage and some have not reached L4. Egg lay is reduced in adult hermaphrodites when 1 mM fluensulfone is present. It has also been discovered that fluensulfone lowers egg viability.After 3 h incubation with 100 μM to 1 mM Fluensulfone the thrashing rate is significantly inhibited, with maximal inhibition occurring with 1 mM. After 1 h both 300 μM and 1 mM Fluensulfone cause a significant and reversible inhibition of pharyngeal pumping relative to the vehicle control. Fluensulfone (500 μM) inhibits the frequency of body bends in one day old adult hermaphrodites off food after 2 h exposure[1].
In vitro, Fluensulfone inhibits the mobility of nematodes. As a nematicide, it is tested against various nematode species in laboratory assays to determine its potency and spectrum of activity. The compound's ability to disrupt nematode nervous system function or mitochondrial metabolism leads to paralysis and death of the target organisms. It is effective against root-knot, root lesion, and cyst nematodes. |
| ln Vivo |
Fluensulfone (or isoniazid as a positive control) is administered to female mice for three or seven days as part of an in vivo study. A four-fold increase in cell proliferation was observed following treatment with fluensulfone and the positive control drug isoniazid, compared to control, according to a manual count of BrdU-positive and BrdU-negative cells in the bronchiolar epithelium. Three days later, there is an increase in cell proliferation, but by day seven, it has returned to the control level [2].
In vivo, Fluensulfone is applied as a soil treatment to control nematode populations in agricultural settings. It is effective against a range of plant-parasitic nematodes in crops such as potatoes and tomatoes. The compound's nematicidal activity has been demonstrated in field studies. It is also effective against other pests such as mites, thrips, aphids, and whiteflies. Its unique mode of action makes it a valuable tool for nematode management. |
| Enzyme Assay |
In vitro nematicidal assays for Fluensulfone typically use nematodes (e.g., Meloidogyne incognita, Caenorhabditis elegans) in 96-well plates. Various concentrations of Fluensulfone are added to wells containing nematodes in aqueous solution. Nematode motility and viability are assessed microscopically at various time points (24-72 hours). LC50 values are calculated from dose-response curves. Acetylcholinesterase inhibition and other enzymatic activities may be measured to elucidate mechanism.
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| Cell Assay |
Cellular assays for Fluensulfone are not typical for a nematicide, as it targets whole organisms rather than cultured cells. However, mechanistic studies may use nematode cell cultures or biochemical assays to assess effects on mitochondrial function or enzyme activities. For example, medium-chain acyl-CoA dehydrogenase (MCAD) activity may be measured spectrophotometrically in nematode homogenates.
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| Animal Protocol |
In vivo animal studies for Fluensulfone are conducted in agricultural settings or greenhouse conditions. Nematode-infested soil is treated with Fluensulfone at various application rates. Plant health, root galling, and nematode population density in soil and roots are assessed at various time points post-treatment. Efficacy is compared to untreated controls and reference nematicides. Crop yield is measured to assess economic benefit.
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| ADME/Pharmacokinetics |
Fluensulfone has molecular weight of 291.70 g/mol (C₇H₅ClF₃NO₂S₂). As a soil-applied nematicide, its pharmacokinetic properties in the context of environmental fate and behavior are relevant. The compound is applied as a soil fumigant and undergoes degradation in soil and water. Its persistence and mobility in the environment have been characterized for regulatory purposes. The compound is not intended for systemic absorption in animals.
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| Toxicity/Toxicokinetics |
Toxicity of Fluensulfone has been evaluated for regulatory approval as a pesticide. It is classified as a pesticide and is regulated under pesticide laws. The compound's toxicity to non-target organisms, including mammals, birds, fish, and beneficial insects, has been assessed. It is considered a potential persistent organic pollutant (POP) and has been targeted for global phaseout under the Stockholm Convention. Protective measures are required during handling and application.
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| References |
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| Additional Infomation |
Flusulfuron belongs to the 1,3-thiazole class of compounds, with a 3,4,4-trifluorobut-3-ene-1-sulfonyl group and a chlorine substituent at positions 2 and 5, respectively. It is a nematicide effective against a variety of plant-parasitic nematodes in various agricultural and horticultural crops. It can be used both as a nematicide and as an agrochemical. Flusulfuron belongs to the 1,3-thiazole class of compounds, organochlorine pesticides, sulfones, organofluorine pesticides, and olefins.
Fluensulfone is a heterocyclic fluoroalkenyl sulfone nematicide for agricultural use. It controls root-knot, root lesion, and cyst nematodes in crops. Its mode of action is not fully determined but may involve mitochondrial β-oxidation disruption. It is also effective against mites, thrips, aphids, and whiteflies. It is a regulated pesticide, not for human therapeutic use. |
| Molecular Formula |
C7H5CLF3NO2S2
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|---|---|
| Molecular Weight |
291.6872
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| Exact Mass |
290.94
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| Elemental Analysis |
C, 28.82; H, 1.73; Cl, 12.15; F, 19.54; N, 4.80; O, 10.97; S, 21.98
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| CAS # |
318290-98-1
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| PubChem CID |
11534927
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| Appearance |
Yellow to brown oil
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
375.5±52.0 °C at 760 mmHg
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| Flash Point |
180.9±30.7 °C
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| Vapour Pressure |
0.0±0.8 mmHg at 25°C
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| Index of Refraction |
1.503
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| LogP |
3.34
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
16
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| Complexity |
378
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| Defined Atom Stereocenter Count |
0
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| SMILES |
F/C(F)=C(F)\CCS(=O)(C1=NC=C(Cl)S1)=O
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| InChi Key |
XSNMWAPKHUGZGQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C7H5ClF3NO2S2/c8-5-3-12-7(15-5)16(13,14)2-1-4(9)6(10)11/h3H,1-2H2
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| Chemical Name |
5-chloro-2-(3,4,4-trifluorobut-3-ene-1-sulfonyl)-1,3-thiazole
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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 : ~100 mg/mL (~342.82 mM)
H2O : ~0.73 mg/mL (~2.50 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.57 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 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 (8.57 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 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 (8.57 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (8.57 mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4283 mL | 17.1415 mL | 34.2830 mL | |
| 5 mM | 0.6857 mL | 3.4283 mL | 6.8566 mL | |
| 10 mM | 0.3428 mL | 1.7141 mL | 3.4283 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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