| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| Other Sizes |
| Targets |
Metaflumizone's primary target is the sodium channel, specifically the honeybee NaV 1 channel. It blocks sodium channels, affecting the action potential propagation in neurons and muscle cells, which is crucial for neurological and muscular function. Metaflumizone (10 μM) completely inhibits the Para/TipE sodium currents in Xenopus oocytes. By blocking sodium channels, it disrupts nerve impulse transmission, leading to paralysis and death of the target pests.
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| ln Vitro |
In Xenopus laevis oocytes, Para/TipE sodium currents are totally inhibited by metaflumizone (10 μM) [1].
In vitro, metaflumizone (10 μM) completely inhibits the Para/TipE sodium currents in Xenopus oocytes. Its activity is characterized by its ability to block sodium channel function, as assessed by electrophysiological techniques such as patch-clamp recording. The compound's potency as a sodium channel blocker is evaluated by measuring the inhibition of sodium currents in cells expressing the target sodium channels. Specific IC50 values are not detailed in the provided search results. |
| ln Vivo |
In vivo, metaflumizone is used as a veterinary drug for the treatment and prevention of flea infestations in cats. It is effective against Ctenocephalides canis and Ctenocephalides felis (cat and dog fleas). The compound can be used as part of a treatment regimen for flea allergic dermatitis (FAD). Its insecticidal activity is due to its potent sodium channel blocking action, which causes paralysis and death of fleas.
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| Enzyme Assay |
The in vitro activity of metaflumizone is assessed using electrophysiological techniques, such as the patch-clamp technique, on Xenopus oocytes expressing the Para/TipE sodium channels. Oocytes are voltage-clamped, and sodium currents are elicited by depolarizing voltage steps. Various concentrations of metaflumizone (typically 0.1-100 µM) are applied, and the inhibition of the sodium current is measured to determine the IC50. For insecticidal activity, the compound's effect on insect nerve function can be assessed using nerve cord preparations or by measuring mortality in insect bioassays.
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| Cell Assay |
For cellular assays, insect cell lines expressing sodium channels or Xenopus oocytes injected with sodium channel mRNA are used. Cells are treated with various concentrations of metaflumizone for defined periods. Sodium channel function is assessed using patch-clamp electrophysiology. Cell viability is assessed using standard assays. For insecticidal activity, insect larvae or adult insects are exposed to various concentrations of metaflumizone, and mortality is assessed over time.
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| Animal Protocol |
In vivo, metaflumizone is typically applied topically or orally to animals for flea control. In veterinary studies, the compound is administered to cats or dogs at recommended doses, and the reduction in flea burden is assessed by counting fleas on the animals at various time points after treatment. The compound's efficacy is evaluated by measuring the percentage reduction in flea counts compared to untreated controls. In toxicological studies, metaflumizone is administered to animals, and various toxicity endpoints are assessed.
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| ADME/Pharmacokinetics |
Metaflumizone has a molecular weight and formula consistent with its chemical structure. The compound is soluble in DMSO and should be stored as a powder at -20°C under desiccated conditions. Specific pharmacokinetic parameters such as bioavailability, half-life, and volume of distribution are not detailed in the provided search results. The compound's lipophilicity may influence its distribution and persistence in the environment.
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| Toxicity/Toxicokinetics |
Metaflumizone has low toxicity in mammals but is highly toxic to aquatic organisms. The compound should be used with caution near water bodies. In veterinary use, it is generally well-tolerated at recommended doses. Side effects may include local irritation at the application site. The compound's use is regulated, and it should be used according to label instructions. Comprehensive toxicological studies are required to establish its full safety profile.
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| References | |
| Additional Infomation |
Metaflumizone is a stilbene compound and an aminourea compound.
Drug Indications For the treatment and prevention of flea infestations in cats (Ctenophora canis and Ctenophora felis). This veterinary drug can be used as part of a treatment regimen for flea allergic dermatitis (FAD). Metaflumizone is a veterinary insecticide used for flea control in cats and dogs. It is a potent sodium channel blocker that is effective against fleas and other pests. The compound is available as a topical solution for veterinary use. Its development represents an advance in flea control, providing an alternative to other insecticides. Metaflumizone is not approved for human use and is intended for veterinary applications only. |
| Molecular Formula |
C24H16F6N4O2
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|---|---|
| Molecular Weight |
506.41
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| Exact Mass |
506.117
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| CAS # |
139968-49-3
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| Related CAS # |
Metaflumizone-d4
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| PubChem CID |
9827529
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.547
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| LogP |
6.05
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
36
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| Complexity |
806
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC(=C1)C(F)(F)F)/C(=N\NC(=O)NC2=CC=C(C=C2)OC(F)(F)F)/CC3=CC=C(C=C3)C#N
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| InChi Key |
MIFOMMKAVSCNKQ-HWIUFGAZSA-N
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| InChi Code |
InChI=1S/C24H16F6N4O2/c25-23(26,27)18-3-1-2-17(13-18)21(12-15-4-6-16(14-31)7-5-15)33-34-22(35)32-19-8-10-20(11-9-19)36-24(28,29)30/h1-11,13H,12H2,(H2,32,34,35)/b33-21-
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| Chemical Name |
1-[(Z)-[2-(4-cyanophenyl)-1-[3-(trifluoromethyl)phenyl]ethylidene]amino]-3-[4-(trifluoromethoxy)phenyl]urea
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| Synonyms |
BAS 320021; BAS 320001; Metaflumizone
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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 : ~300 mg/mL (~592.42 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9747 mL | 9.8734 mL | 19.7468 mL | |
| 5 mM | 0.3949 mL | 1.9747 mL | 3.9494 mL | |
| 10 mM | 0.1975 mL | 0.9873 mL | 1.9747 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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