| Size | Price | |
|---|---|---|
| Other Sizes |
| Targets |
Voltage-gated sodium channels (Sodium Channel) in insect neurons.
|
|---|---|
| ln Vitro |
Insects metabolize indoxacarb to produce N-desmethylmethoxylated JW062 (DCJW), a chemical with more activity than the original. A viable substitute for pyrethroid insecticides is indoxacarb, particularly when it comes to managing lepidopteran pests that are significant for agriculture [1].
In vitro, Indoxacarb is metabolically converted to N-demethoxylated JW062 (DCJW), which is more active than the parent compound. It suppresses voltage-gated sodium channel currents in rat dorsal root ganglion neurons in a concentration-dependent manner. |
| ln Vivo |
Indoxacarb is effective in the field against various insect pests, including Lepidoptera. It blocks voltage-gated sodium channels, leading to insect paralysis. Formulations have been used to control pests in tea farming. It has low mammalian toxicity, making it safer for use around humans and livestock.
|
| Enzyme Assay |
Radioimmunoassays or LC-MS are used to measure the binding of Indoxacarb or its active metabolite DCJW to sodium channels. Alternatively, whole-cell patch-clamp on isolated insect neurons can measure the block of sodium currents.
|
| Cell Assay |
Insect neurons or insect cell lines expressing sodium channels are cultured. Whole-cell patch-clamp recordings are performed to measure sodium currents. Indoxacarb or its metabolite DCJW is applied, and the reduction in current is measured.
|
| Animal Protocol |
In vivo, the insecticidal activity is assessed in field trials or greenhouse studies. The compound is sprayed on crops, and the mortality of target pests is recorded. Toxicokinetic studies in rats or other mammals are used to assess its low mammalian toxicity.
|
| ADME/Pharmacokinetics |
Indoxacarb is rapidly absorbed and metabolized in mammals, primarily to DCJW, followed by hydrolysis to inactive metabolites. It has low oral bioavailability in rats (24-32%) and is rapidly excreted in urine and feces. The half-life is about 2-5 days.
|
| Toxicity/Toxicokinetics |
Indoxacarb has low acute toxicity in mammals, with an oral LD50 in rats of >5,000 mg/kg. It is a mild to moderate eye and skin irritant. Chronic exposure may cause anemia and liver effects at high doses. It is not considered genotoxic or a human carcinogen.
|
| References | |
| Additional Infomation |
See also: Indoxacarb (note moved to).
Indoxacarb is an important insecticide in agriculture, used on a variety of crops including cotton, vegetables, and fruits. It is also used in public health for ant and cockroach control. It is approved for use in many countries. |
| Molecular Formula |
C22H17CLF3N3O7
|
|---|---|
| Molecular Weight |
527.83
|
| Exact Mass |
527.07
|
| CAS # |
144171-61-9
|
| PubChem CID |
9936739
|
| Appearance |
White to off-white solid powder
|
| Density |
1.5±0.1 g/cm3
|
| Boiling Point |
571.4±60.0 °C at 760 mmHg
|
| Melting Point |
139-141ºC
|
| Flash Point |
299.3±32.9 °C
|
| Vapour Pressure |
0.0±1.6 mmHg at 25°C
|
| Index of Refraction |
1.602
|
| LogP |
2.77
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
11
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
36
|
| Complexity |
912
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
COC(=O)C12CC3=C(C1=NN(CO2)C(=O)N(C4=CC=C(C=C4)OC(F)(F)F)C(=O)OC)C=CC(=C3)Cl
|
| InChi Key |
VBCVPMMZEGZULK-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C22H17ClF3N3O7/c1-33-18(30)21-10-12-9-13(23)3-8-16(12)17(21)27-28(11-35-21)19(31)29(20(32)34-2)14-4-6-15(7-5-14)36-22(24,25)26/h3-9H,10-11H2,1-2H3
|
| Chemical Name |
methyl 7-chloro-2-[methoxycarbonyl-[4-(trifluoromethoxy)phenyl]carbamoyl]-3,5-dihydroindeno[1,2-e][1,3,4]oxadiazine-4a-carboxylate
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO: 12.5 mg/mL (23.68 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8945 mL | 9.4727 mL | 18.9455 mL | |
| 5 mM | 0.3789 mL | 1.8945 mL | 3.7891 mL | |
| 10 mM | 0.1895 mL | 0.9473 mL | 1.8945 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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