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  2. nAChR Environmental Pollutants Insecticide
  3. Thiacloprid

Thiacloprid is an orally active neurotoxic insecticide and also a nAChR agonist. Thiacloprid reduces the viability of healthy cells, depletes reduced glutathione, and increases MDA levels, thereby inducing cytotoxicity and oxidative stress damage. In practical applications, Thiacloprid has lower acute toxicity to honeybees than other compounds of the same class such as Imidacloprid (HY-B0838), but it still significantly impairs the learning and memory function, immune capacity and survival status of honeybees. Thiacloprid induces intestinal microbial dysbiosis and reduces survival rate in middle-aged honeybees, increases the risk of premature collapse in bumblebee colonies, and significantly decreases the final colony weight and reproductive output. Thiacloprid is used in broad-spectrum agricultural pest control, often alone or in combination with Deltamethrin (HY-B1971), and meets the pest management needs of various crops including potatoes, cabbages, various fruits and vegetables, and nuts.

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Thiacloprid

Thiacloprid Chemical Structure

CAS No. : 111988-49-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Thiacloprid:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Thiacloprid

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Thiacloprid is an orally active neurotoxic insecticide and also a nAChR agonist. Thiacloprid reduces the viability of healthy cells, depletes reduced glutathione, and increases MDA levels, thereby inducing cytotoxicity and oxidative stress damage. In practical applications, Thiacloprid has lower acute toxicity to honeybees than other compounds of the same class such as Imidacloprid (HY-B0838), but it still significantly impairs the learning and memory function, immune capacity and survival status of honeybees. Thiacloprid induces intestinal microbial dysbiosis and reduces survival rate in middle-aged honeybees, increases the risk of premature collapse in bumblebee colonies, and significantly decreases the final colony weight and reproductive output. Thiacloprid is used in broad-spectrum agricultural pest control, often alone or in combination with Deltamethrin (HY-B1971), and meets the pest management needs of various crops including potatoes, cabbages, various fruits and vegetables, and nuts[1][2][3].

Cellular Effect
Cell Line Type Value Description References
SH-SY5Y IC50
100 μM
Compound: THIA
Inhibition of [3H]alpha-BGT binding to alpha7 nicotinic acetylcholine receptor in Homo sapiens (human) SH-SY5Y cells
Inhibition of [3H]alpha-BGT binding to alpha7 nicotinic acetylcholine receptor in Homo sapiens (human) SH-SY5Y cells
[PMID: 11312774]
TE-671 IC50
120 μM
Compound: THIA
Inhibition of [3H]alpha-BGT binding to alpha1 nicotinic acetylcholine receptor in Homo sapiens (human) TE671 cells co-expressing gammaalpha1deltabeta1 nicotinic acetylcholine receptor subunits
Inhibition of [3H]alpha-BGT binding to alpha1 nicotinic acetylcholine receptor in Homo sapiens (human) TE671 cells co-expressing gammaalpha1deltabeta1 nicotinic acetylcholine receptor subunits
[PMID: 11312774]
In Vitro

Combination treatment with Thiacloprid (7.5-3000 μM; 24-72 h) and Deltamethrin (HY-B1971) reduces the viability of human lung fibroblast cell line WTHBF-6 in a time- and concentration-dependent manner. Specifically, significant viability reduction is observed at concentrations of 1500 μM, 2250 μM and 3000 μM after 48 h and 72 h of treatment, as well as at 750 μM after 72 h of treatment[1].
Thiacloprid (75-375 μM; 24-72 h) significantly reduces the level of GSH, increases the level of malondialdehyde (MDA), and induces cellular lipid peroxidation damage in human lung fibroblast cell line WTHBF-6[1].

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

Cell Viability AssayWestern Blot AnalysisCell Proliferation AssayApoptosis AnalysisCell Cytotoxicity AssayCell Cycle AnalysisRT-PCRCell Autophagy AssayImmunofluorescenceCell Differentiation AssayCell Invasion AssayCell Migration Assay Real Time qPCRELISA Assay[1]

Cell Line: WTHBF-6 (human telomerase reverse transcriptase (hTERT)-expressing human lung fibroblasts)
Concentration: 7.5 μM, 18.75 μM, 37.5 μM, 75 μM, 187.5 μM, 375 μM, 750 μM, 1500 μM, 2250 μM, 3000 μM
Incubation Time: 24 h, 48 h, 72 h
Result: Co-administered with Deltamethrin at a fixed concentration ratio of 7.5:1.
Reduced the viability of WTHBF-6 cells in a time- and concentration-dependent manner.
Significantly decreased cell viability at the concentrations of 1500 μM, 2250 μM and 3000 μM of Thiacloprid after 48 h and 72 h treatment, and at 750 μM of Thiacloprid (HY-B1953) after 72 h treatment, compared with the 0.1% DMSO vehicle control group.
In Vivo

Thiacloprid (0.2-2.0 mg/L; oral; daily; 13 consecutive days) continuous oral exposure of middle-aged honeybees to 0.6 mg/L and 2.0 mg/L thiacloprid for 13 days significantly reduces survival by up to 25%, impairs weight gain, alters sucrose consumption at the highest dose, induces dose-dependent gut microbiome dysbiosis on day 7, and is associated with gut microbiome recovery by day 13[2].
Thiacloprid (recommended manufacturer spray rate; free foraging on treated crop flowers) under field-realistic exposure to treated raspberry crops leads to accumulation of thiacloprid residues in bumblebee colony food stores, with maximum concentrations of 771 ppb in pollen and 561 ppb in nectar[3].

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

Animal Model: Bombus terrestris audax (commercially reared colonies)[3]
Dosage: recommended manufacturer spray rate
Administration: free foraging on treated crop flowers
Result: Detected thiacloprid residues in pollen and nectar stores up to 771 ppb in pollen and 561 ppb in nectar 2-4 weeks postspraying.
Detected no thiacloprid in nectar and only minimal levels in pollen at 4 weeks (pre-spraying).
Molecular Weight

252.72

Formula

C10H9ClN4S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N#C/N=C1N(CCS/1)CC(C=C2)=CN=C2Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (197.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.9569 mL 19.7847 mL 39.5695 mL
5 mM 0.7914 mL 3.9569 mL 7.9139 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • 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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
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:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (9.89 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

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(per animal)

g

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.66%

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.9569 mL 19.7847 mL 39.5695 mL 98.9237 mL
5 mM 0.7914 mL 3.9569 mL 7.9139 mL 19.7847 mL
10 mM 0.3957 mL 1.9785 mL 3.9569 mL 9.8924 mL
15 mM 0.2638 mL 1.3190 mL 2.6380 mL 6.5949 mL
20 mM 0.1978 mL 0.9892 mL 1.9785 mL 4.9462 mL
25 mM 0.1583 mL 0.7914 mL 1.5828 mL 3.9569 mL
30 mM 0.1319 mL 0.6595 mL 1.3190 mL 3.2975 mL
40 mM 0.0989 mL 0.4946 mL 0.9892 mL 2.4731 mL
50 mM 0.0791 mL 0.3957 mL 0.7914 mL 1.9785 mL
60 mM 0.0659 mL 0.3297 mL 0.6595 mL 1.6487 mL
80 mM 0.0495 mL 0.2473 mL 0.4946 mL 1.2365 mL
100 mM 0.0396 mL 0.1978 mL 0.3957 mL 0.9892 mL
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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.

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Thiacloprid
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HY-B1953
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