2. Membrane Transporter/Ion Channel Neuronal Signaling Anti-infection
  3. GABA Receptor Chloride Channel Parasite
  4. Afoxolaner

Afoxolaner is an orally active isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect γ-aminobutyric acid receptor (GABA) and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod.

For research use only. We do not sell to patients.

Afoxolaner Chemical Structure

Afoxolaner Chemical Structure

CAS No. : 1093861-60-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 62 In-stock
Solution
10 mM * 1 mL in DMSO USD 62 In-stock
Solid
5 mg USD 45 In-stock
10 mg USD 75 In-stock
25 mg USD 145 In-stock
50 mg USD 230 In-stock
100 mg USD 370 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Afoxolaner:

Afoxolaner Related Antibodies

Top Publications Citing Use of Products

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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Afoxolaner is an orally active isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect γ-aminobutyric acid receptor (GABA) and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod[1][2].

IC50 & Target

Mite

 

In Vivo

A single oral treatment with a dose approaching the minimum effective dose of Afoxolaner (2.5mg/kg) eliminated the pre-existing infestations of I. scapularis ticks and controlled weekly re-infestations, with efficacy between 98% and 100% recorded until Day 23 and 94% at Day 30[1].

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

625.87

Formula

C26H17ClF9N3O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C2C=CC=CC2=C(C3=NOC(C(F)(F)F)(C4=CC(C(F)(F)F)=CC(Cl)=C4)C3)C=C1)NCC(NCC(F)(F)F)=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 : ≥ 250 mg/mL (399.44 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5978 mL 7.9889 mL 15.9778 mL
5 mM 0.3196 mL 1.5978 mL 3.1956 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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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: ≥ 2.25 mg/mL (3.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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: ≥ 2.25 mg/mL (3.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.25 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 (22.5 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).
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: 99.95%

COA (248 KB) HNMR (290 KB) LCMS (266 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
DMSO 1 mM 1.5978 mL 7.9889 mL 15.9778 mL 39.9444 mL
5 mM 0.3196 mL 1.5978 mL 3.1956 mL 7.9889 mL
10 mM 0.1598 mL 0.7989 mL 1.5978 mL 3.9944 mL
15 mM 0.1065 mL 0.5326 mL 1.0652 mL 2.6630 mL
20 mM 0.0799 mL 0.3994 mL 0.7989 mL 1.9972 mL
25 mM 0.0639 mL 0.3196 mL 0.6391 mL 1.5978 mL
30 mM 0.0533 mL 0.2663 mL 0.5326 mL 1.3315 mL
40 mM 0.0399 mL 0.1997 mL 0.3994 mL 0.9986 mL
50 mM 0.0320 mL 0.1598 mL 0.3196 mL 0.7989 mL
60 mM 0.0266 mL 0.1331 mL 0.2663 mL 0.6657 mL
80 mM 0.0200 mL 0.0999 mL 0.1997 mL 0.4993 mL
100 mM 0.0160 mL 0.0799 mL 0.1598 mL 0.3994 mL
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Afoxolaner 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:

Afoxolaner1093861-60-9GABA ReceptorChloride ChannelParasiteGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorCl− ChannelsisoxazolineinsecticideacaricideIxodesscapularisinsectdogarthropodInhibitorinhibitorinhibit

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