2. Neuronal Signaling Membrane Transporter/Ion Channel Anti-infection
  3. nAChR Parasite
  4. Dinotefuran

Dinotefuran is an orally active and competitive inhibitor and insecticide targeting insect nicotinic acetylcholine receptors (nAChRs). Dinotefuran blocks neural signaling and induces neural dysfunction in insects. Dinotefuran 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. Dinotefuran exhibits knockdown activity (KD50=0.351 nmol/g) and lethal activity (LD50=0.173 nmol/g) against German cockroach. Dinotefuran is mainly used for agricultural pest control, such as field control of piercing-sucking and chewing insects (e.g., aphids, planthoppers), while its environmental toxicological effects (e.g., oxidative stress and reproductive neurotoxicity on earthworms) are also a research focus to assess ecological risks.

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Dinotefuran Chemical Structure

Dinotefuran Chemical Structure

CAS No. : 165252-70-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 3 publication(s) in Google Scholar

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Description

Dinotefuran is an orally active and competitive inhibitor and insecticide targeting insect nicotinic acetylcholine receptors (nAChRs). Dinotefuran blocks neural signaling and induces neural dysfunction in insects. Dinotefuran 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. Dinotefuran exhibits knockdown activity (KD50=0.351 nmol/g) and lethal activity (LD50=0.173 nmol/g) against German cockroach. Dinotefuran is mainly used for agricultural pest control, such as field control of piercing-sucking and chewing insects (e.g., aphids, planthoppers), while its environmental toxicological effects (e.g., oxidative stress and reproductive neurotoxicity on earthworms) are also a research focus to assess ecological risks[1][2][3].

In Vitro

Dinotefuran (1 μM; 120 min) competitively inhibits the binding of [3H]EPI to nicotinic acetylcholine receptors (nAChRs) in the neuronal cord membrane of American cockroaches[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Dinotefuran Related Antibodies

Cell Viability Assay[1]

Cell Line: Periplaneta americana nerve cord membrane preparations
Concentration: IC50: 890 nM ((±)-Dinotefuran); 856 nM ((+)-Dinotefuran); 1890 nM ((-)-Dinotefuran)
Incubation Time: 120 minutes
Result: Inhibited [3H]EPI binding with an IC50 of 890 nM, with (+)-enantiomer being ~2-fold more potent than (-)-enantiomer.
In Vivo

Dinotefuran (0.1, 2.0 mg/kg; mixed in artificial soil; 28 days) induces excessive production of reactive oxygen species (ROS) in Eisenia fetida earthworms, leading to significant changes in antioxidant enzyme activities (SOD, CAT, GPX, GR) and functional gene (MT, HSP70) expression, accompanied by lipid peroxidation (increased MDA), protein carbonylation (increased PCO) and DNA damage (increased comet assay tail moment), and dose- and time-dependent toxicity[1].
Dinotefuran (0.015%-0.06%; mixed in feed; daily intake) leads to prolonged movement time of F0 males, decreased fertility of females, increases birth weight and imbalanced sex ratio of F1 pups, delayes olfactory orientation of female offspring, decreases movement distance and speed of male offspring, and increased urination frequency[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Toxicity model in CD-1 mouse (4-week-old)[2]
Dosage: 0% (control), 0.015%, 0.03%, and 0.06%
Administration: Oral, given in the basal diets (CE-2); 5 weeks of age of the F0 generation to 11 weeks of age of the F1 generation in mice.
Result: In F0 adult males, movement time during exploratory behavior significantly increased with dose-related trends), while rearing time and average rearing time decreased.
In F1 offspring, litter size and weight at birth increased in dose-related trends), but sex ratio (male/female) decreased significantly.
On postnatal day (PND) 21, offspring body weight increased in both sexes for males, for females).
Female offspring showed delayed olfactory orientation time on PND 14, while male offspring exhibited reduced total distance, average speed, and increased defecation frequency and urination.
Molecular Weight

202.21

Formula

C7H14N4O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=[N+](N/C(NC)=N/CC1COCC1)[O-]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 66.67 mg/mL (329.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 50 mg/mL (247.27 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 25 mg/mL (123.63 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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g

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.74%

SDS (761 KB)

COA (246 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 4.9454 mL 24.7268 mL 49.4535 mL 123.6338 mL
5 mM 0.9891 mL 4.9454 mL 9.8907 mL 24.7268 mL
10 mM 0.4945 mL 2.4727 mL 4.9454 mL 12.3634 mL
15 mM 0.3297 mL 1.6485 mL 3.2969 mL 8.2423 mL
20 mM 0.2473 mL 1.2363 mL 2.4727 mL 6.1817 mL
25 mM 0.1978 mL 0.9891 mL 1.9781 mL 4.9454 mL
30 mM 0.1648 mL 0.8242 mL 1.6485 mL 4.1211 mL
40 mM 0.1236 mL 0.6182 mL 1.2363 mL 3.0908 mL
50 mM 0.0989 mL 0.4945 mL 0.9891 mL 2.4727 mL
60 mM 0.0824 mL 0.4121 mL 0.8242 mL 2.0606 mL
80 mM 0.0618 mL 0.3091 mL 0.6182 mL 1.5454 mL
100 mM 0.0495 mL 0.2473 mL 0.4945 mL 1.2363 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Dinotefuran Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Dinotefuran165252-70-0MTI-446MTI446MTI 446nAChRParasiteNicotinic acetylcholine receptorsInhibitorinhibitorinhibit

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