| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Dinotefuran targets insect nicotinic acetylcholine receptors (nAChRs). It acts as an agonist for nAChRs, blocking neural signaling and inducing neural dysfunction in insects. The compound binds to [³H]epibatidine in the neural cord membrane of American cockroach with an IC50 of 890 nM and to [³H]α-bungarotoxin with an IC50 of 36.1 μM.
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| ln Vitro |
In vitro, Dinotefuran competitively inhibits the binding of [³H]EPI to nAChRs in the neuronal cord membrane of American cockroaches. It exhibits knockdown activity (KD50=0.351 nmol/g) and lethal activity (LD50=0.173 nmol/g) against German cockroach.
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| ln Vivo |
In vivo, Dinotefuran (0.1, 2.0 mg/kg; mixed in artificial soil; 28 days) induces excessive production of reactive oxygen species in Eisenia fetida earthworms, leading to changes in antioxidant enzyme activities and DNA damage. It also leads to prolonged movement time, decreased fertility, and other effects in F0 and F1 generations in animal studies.
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| Enzyme Assay |
In vitro receptor binding assays for Dinotefuran typically use membrane preparations from insect neural tissues. Radiolabeled epibatidine or α-bungarotoxin is displaced by increasing concentrations of the compound to determine binding affinity (Ki). Non-specific binding is determined in the presence of excess unlabeled ligand.
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| Cell Assay |
Cell-based assays for Dinotefuran involve treating insect cell lines or primary neuronal cultures with the compound and measuring nAChR-mediated ion flux or calcium influx. The compound's ability to activate or inhibit nAChRs is assessed using fluorescent dyes or electrophysiology.
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| Animal Protocol |
In vivo insect studies for Dinotefuran involve administering the compound to various insect species via diet or topical application. Mortality, knockdown activity, and neural dysfunction are assessed. Dose-response studies determine LD50 and KD50 values. Environmental toxicology studies assess effects on non-target organisms like earthworms.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Dinotefuran are characteristic of neonicotinoid insecticides. The compound is orally active and absorbed through the gut of insects. It is distributed to tissues, where it binds to nAChRs. Metabolism occurs via oxidation and conjugation.
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| Toxicity/Toxicokinetics |
Dinotefuran is not a skin irritant in rabbits, is slightly irritating to the eye, and is not a skin sensitizer. Neurotoxicity in mammals was not a critical effect after repeated exposure. However, it can induce oxidative stress and reproductive neurotoxicity in earthworms.
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| References | |
| Additional Infomation |
(E)-Fucopyr is a type of fipronil.
Dinotefuran is a neonicotinoid insecticide used for agricultural pest control, targeting piercing-sucking and chewing insects like aphids and planthoppers. It is not approved for therapeutic use in humans. The compound is a valuable tool for studying nAChR function and developing pest control strategies. |
| Molecular Formula |
C7H14N4O3
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|---|---|
| Molecular Weight |
202.2111
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| Exact Mass |
202.106
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| CAS # |
165252-70-0
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| Related CAS # |
Dinotefuran-d3;(R)-Dinotefuran;406466-53-3;(S)-Dinotefuran;322639-07-6
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| PubChem CID |
135418283
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
334.5±34.0 °C at 760 mmHg
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| Melting Point |
107.5ºC
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| Flash Point |
156.1±25.7 °C
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| Vapour Pressure |
0.0±0.7 mmHg at 25°C
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| Index of Refraction |
1.596
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| LogP |
-0.7
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
14
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| Complexity |
226
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN/C(=N\[N+](=O)[O-])/NCC1CCOC1
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| InChi Key |
YKBZOVFACRVRJN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C7H14N4O3/c1-8-7(10-11(12)13)9-4-6-2-3-14-5-6/h6H,2-5H2,1H3,(H2,8,9,10)
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| Chemical Name |
1-methyl-2-nitro-3-(oxolan-3-ylmethyl)guanidine
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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) |
H2O : ~50 mg/mL (~247.27 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 25 mg/mL (123.63 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.9454 mL | 24.7268 mL | 49.4535 mL | |
| 5 mM | 0.9891 mL | 4.9454 mL | 9.8907 mL | |
| 10 mM | 0.4945 mL | 2.4727 mL | 4.9454 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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