2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. nAChR
  4. Monepantel

Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.

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Monepantel Chemical Structure

Monepantel Chemical Structure

CAS No. : 887148-69-8

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 365 In-stock
Solution
10 mM * 1 mL in DMSO USD 365 In-stock
Solid
1 mg USD 110 In-stock
5 mg USD 350 In-stock
10 mg USD 500 In-stock
25 mg USD 1000 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Monepantel:

Monepantel Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.

In Vitro

The metallocenyl analogues of monepantel shows nematocidal activity[1]. Monepantel (25 µM) induces accumulation of acidic vacuoles. Ovarian cancer cell lines are highly sensitive to Monepantel with IC50 values of 7.2±0.2 µM (OVCAR-3) and 10.5±0.4 μM (A2780). Monepantel (0, 10 and 25 µM) induces autophagosome formation in these cancer cell lines. Monepantel (0, 10 and 25 µM) exhibits a markedly reduced level of punctate staining indicating the suppression of phosphorylated mTOR at Ser2448. Monepantel also decreases the expression of phosphorylated Raptor at Ser792, which is one of the mTORC1 coMonepantelex members[2]. Monepantel (250 μg/mL) leads multiple ABC transporter genes higher transcription in both worm isolates. Larvae exposed to monepantel at 250 μg/mL shows an increased efflux of rhodamine-123 and a proportion of the larval population shows an ability to subsequently tolerate higher concentrations of IVM in migration assays[3].

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

Monepantel Related Antibodies
In Vivo

Monepantel (10 μM) significantly increased all CYP-related activities and CYP3A24 mRNA in sheep[4].

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

473.39

Formula

C20H13F6N3O2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N[C@@](C)(C#N)COC1=CC(C#N)=CC=C1C(F)(F)F)C2=CC=C(SC(F)(F)F)C=C2
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 : ≥ 100 mg/mL (211.24 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 2.1124 mL 10.5621 mL 21.1242 mL
5 mM 0.4225 mL 2.1124 mL 4.2248 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
=
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: 2.5 mg/mL (5.28 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.28 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:

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
References
Kinase Assay
[2]

Caspase-3 and -8 colorimetric assay kits are used according to the manufacturer’s instructions. Briefly, after treatment the cells with indicated concentration of Monepantel (0, 10 and 25 µM) for 48 and 72 h, cells are harvested, centrifuged at 250 g for 10 min. The cell pellet lysed by the addition of the lyses buffer, then incubated on ice for 10 min followed by centrifugation at 10,000 g for 5 min. The supernatant is used to start the enzymatic reaction in 96 well plates based on manufacturer protocol. Each concentration is tested in replications of 4 and each experiment is repeated twice.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[2]

The effect of monepantel with or without other agents on cell proliferation is assessed using the sulforhodamine B (SRB) assay. Briefly, cells are seeded in 96-well plates (2500 cells/well) overnight followed by treatment with desired concentrations of Monepantel. After 72 h cells are fixed with 200 µL of 0.1% TCA, washed with tap water and stained with 100 µL of 0.4% (w/v) SRB dissolved in 1% acetic acid. Unbound dye is removed by five ishes with 1% acetic acid before air drying. Bound SRB is solubilized with 100 µL of 10 mM Tris base (pH 10.5) and the absorbance read at 570 nm. Each concentration is tested in replications of 8 and each experiment is repeated twice. Data represent mean±SEM from two independent experiments combined.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 2.1124 mL 10.5621 mL 21.1242 mL 52.8106 mL
5 mM 0.4225 mL 2.1124 mL 4.2248 mL 10.5621 mL
10 mM 0.2112 mL 1.0562 mL 2.1124 mL 5.2811 mL
15 mM 0.1408 mL 0.7041 mL 1.4083 mL 3.5207 mL
20 mM 0.1056 mL 0.5281 mL 1.0562 mL 2.6405 mL
25 mM 0.0845 mL 0.4225 mL 0.8450 mL 2.1124 mL
30 mM 0.0704 mL 0.3521 mL 0.7041 mL 1.7604 mL
40 mM 0.0528 mL 0.2641 mL 0.5281 mL 1.3203 mL
50 mM 0.0422 mL 0.2112 mL 0.4225 mL 1.0562 mL
60 mM 0.0352 mL 0.1760 mL 0.3521 mL 0.8802 mL
80 mM 0.0264 mL 0.1320 mL 0.2641 mL 0.6601 mL
100 mM 0.0211 mL 0.1056 mL 0.2112 mL 0.5281 mL
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Monepantel 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:

Monepantel887148-69-8AAD1566AAD 1566AAD-1566nAChRNicotinic acetylcholine receptorsInhibitorinhibitorinhibit

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