| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
Fluxametamide targets GABA-gated chloride channels (GABACls) and glutamate-gated chloride channels (GluCls). It shows potent antagonism of M. domestica GABACls and GluCls with IC50 values of 1.95 nM and 225 nM, respectively.
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|---|---|
| ln Vitro |
GABA and glutamate-gated chloride channel antagonist fluxametamide inhibits GABA and glutamate-induced currents in M in a dose-dependent manner. With IC50 values of 1.95 (1.18-3.21) nM and 225 (137-372) nM, respectively, Domestica GABACls and GluCls demonstrate strong antagonistic effect against Tetranychus two-spotted mites' GABACls, with an IC50 of 0.219 (0.127-0.381) nM. With an IC50 value of 1.40 (0.57-3.29) nM for wild-type Biseophora striatellus GABACls and 3.51 (2.17-5.69) nM for A2'N mutant GABACls, fluxametamide suppresses the GABA response. Moreover, at the measured concentrations, 10 μM Fluxametamide had no inhibitory impact on glycine (EC50)-induced currents in human α1 GlyCls and very weakly inhibited GABA (EC50)-induced currents in rat GABACls [1].
In vitro, Fluxametamide dose-dependently inhibits currents induced by GABA and glutamate in M. domestica neurons. It shows negligible antagonistic activity against rat GABACls and human glycine-gated chloride channels, demonstrating high arthropod selectivity. |
| ln Vivo |
At 12.9 ± 4.9 ng/fly (38.7 ± 6.3 ng/fly), flusamide exhibits noteworthy insecticidal action [1].
In vivo, Fluxametamide is effective as an insecticide against a wide range of arthropod pests. It is used in agricultural applications to control insect populations. |
| Enzyme Assay |
GABA- and glutamate-gated chloride channel antagonism is measured using electrophysiological techniques (e.g., two-electrode voltage clamp) in Xenopus oocytes expressing insect or mammalian chloride channels.
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| Cell Assay |
Insect neurons or oocytes expressing insect chloride channels are cultured and exposed to GABA or glutamate in the presence of Fluxametamide. Chloride currents are measured electrophysiologically.
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| Animal Protocol |
Insect pest models are used to evaluate insecticidal efficacy. Fluxametamide is applied topically or orally, and insect mortality is measured. Selectivity is assessed by comparing effects on insects versus mammals.
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| ADME/Pharmacokinetics |
Fluxametamide is an insecticide and is not intended for human therapeutic use. Its pharmacokinetics in mammals are not relevant for its application as a pesticide.
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| Toxicity/Toxicokinetics |
Fluxametamide shows negligible toxicity to mammals due to its high selectivity for arthropod chloride channels. It is considered safe for use in agricultural applications at recommended doses.
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| References | |
| Additional Infomation |
Fluxametamide is registered as an insecticide for agricultural use in several countries. It has no human therapeutic applications or regulatory approval as a drug.
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| Molecular Formula |
C20H16CL2F3N3O3
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|---|---|
| Molecular Weight |
474.260553359985
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| Exact Mass |
473.052
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| CAS # |
928783-29-3
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| PubChem CID |
137159471
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| Appearance |
White to off-white solid powder
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| LogP |
5.03
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
31
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| Complexity |
712
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
BPFUIWLQXNPZHI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H16Cl2F3N3O3/c1-11-5-12(3-4-16(11)18(29)26-10-27-30-2)17-9-19(31-28-17,20(23,24)25)13-6-14(21)8-15(22)7-13/h3-8,10H,9H2,1-2H3,(H,26,27,29)
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| Chemical Name |
4-[5-(3,5-dichlorophenyl)-5-(trifluoromethyl)-4H-1,2-oxazol-3-yl]-N-(methoxyiminomethyl)-2-methylbenzamide
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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 : ~125 mg/mL (~263.57 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.39 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 20.8 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: ≥ 2.08 mg/mL (4.39 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 20.8 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 | 2.1085 mL | 10.5427 mL | 21.0855 mL | |
| 5 mM | 0.4217 mL | 2.1085 mL | 4.2171 mL | |
| 10 mM | 0.2109 mL | 1.0543 mL | 2.1085 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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