2. Others Neuronal Signaling Membrane Transporter/Ion Channel Metabolic Enzyme/Protease Apoptosis
  3. Environmental Pollutants GABA Receptor Apoptosis Cytochrome P450
  4. Fipronil

Fipronil is a broad-spectrum insecticide effective against Lepidoptera species as well as thrips, locusts, ants, cockroaches, fleas and ticks. Fipronil selectively inhibits GABA receptor with IC50s of 30 nM and 1600 nM for cockroach and rat GABA receptors, respectively. Glutamate-gated chloride channels (GluCls), which are present in cockroaches but not in mammals, are sensitive to the blocking effect of Fipronil. Fipronil also induces apoptosis in HepG2 cells and promotes the expression of CYP1A1 and CYP3A4 mRNA in human hepatocytes.

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Fipronil

Fipronil Estructura química

No. CAS : 120068-37-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
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Fipronil Related Antibodies

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

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Descripciòn

Fipronil is a broad-spectrum insecticide effective against Lepidoptera species as well as thrips, locusts, ants, cockroaches, fleas and ticks. Fipronil selectively inhibits GABA receptor with IC50s of 30 nM and 1600 nM for cockroach and rat GABA receptors, respectively. Glutamate-gated chloride channels (GluCls), which are present in cockroaches but not in mammals, are sensitive to the blocking effect of Fipronil. Fipronil also induces apoptosis in HepG2 cells and promotes the expression of CYP1A1 and CYP3A4 mRNA in human hepatocytes[1][2].

IC50 & Target

CYP1

 

CYP2

 

CYP3

 

In Vitro

Fipronil (0.1-25 µM; 72 h) dose-dependently induces expression of CYP1A1 and CYP3A4 mRNA in human hepatocytes[1].
Fipronil (0.1-25 µM; 72 h) induces caspase-3/7 activity in a time- and dose-dependent manner, in HepG2 cells (caspase-3/7 activity is an important marker of the cellular apoptotic process)[1].

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

Fipronil Related Antibodies

RT-PCR[1]

Cell Line: Human hepatocytes
Concentration: 0.1-25 µM
Incubation Time: 72 h
Result: Remarkably increased the expression of CYP1A1 and CYP3A4 mRNA in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: HepG2 cells
Concentration: 0.05, 0.1, 0.5, 1, 3.125, 6.25, 12.5, 25, 50 µM
Incubation Time: 24, 48, 72 h
Result: Exhibited time- and dose-dependent induction of caspase-3/7 activity from 0.1 to 6.25 µM, while slowly decreasing from 12.5 to 50 µM.
In Vivo

Fipronil inhibits two types of glutamate-induced chloride desensitizing and non-desensitizing current with IC50 values of 800 and 10 nM, respectively[2].
Fipronil is more selective for cockroach GABA receptors than for rat GABA[2].
Fipronil blocks cockroach GABA receptors in both resting and activated states, with IC50s of 28 and 35 nM, respectively[2].

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

437.15

Fòrmula

C12H4Cl2F6N4OS
No. CAS
Appearance

Solid

Color

White to off-white

SMILES

N#CC1=NN(C2=C(Cl)C=C(C(F)(F)F)C=C2Cl)C(N)=C1S(C(F)(F)F)=O
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvente y solubilidad
In Vitro: 

DMSO : 250 mg/mL (571.89 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 2.2875 mL 11.4377 mL 22.8754 mL
5 mM 0.4575 mL 2.2875 mL 4.5751 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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Calculadora de molaridad

  • Calculadora de dilución

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.76 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.76 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(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:
%
DMSO +
% 
+
%
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

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.
Pureza y Documentación
Referencias

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 (protect from light, stored under nitrogen). 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 2.2875 mL 11.4377 mL 22.8754 mL 57.1886 mL
5 mM 0.4575 mL 2.2875 mL 4.5751 mL 11.4377 mL
10 mM 0.2288 mL 1.1438 mL 2.2875 mL 5.7189 mL
15 mM 0.1525 mL 0.7625 mL 1.5250 mL 3.8126 mL
20 mM 0.1144 mL 0.5719 mL 1.1438 mL 2.8594 mL
25 mM 0.0915 mL 0.4575 mL 0.9150 mL 2.2875 mL
30 mM 0.0763 mL 0.3813 mL 0.7625 mL 1.9063 mL
40 mM 0.0572 mL 0.2859 mL 0.5719 mL 1.4297 mL
50 mM 0.0458 mL 0.2288 mL 0.4575 mL 1.1438 mL
60 mM 0.0381 mL 0.1906 mL 0.3813 mL 0.9531 mL
80 mM 0.0286 mL 0.1430 mL 0.2859 mL 0.7149 mL
100 mM 0.0229 mL 0.1144 mL 0.2288 mL 0.5719 mL
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Fipronil Related Classifications

Help & FAQs
  • 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:

Fipronil120068-37-3Environmental PollutantsGABA ReceptorApoptosisCytochrome P450Environmental ContaminantsGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorCYPsapoptosisCYP1A1CYP3A4human hepatocytesHepG2GluClsInhibitorinhibitorinhibit

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