Art. -Nr.: HY-14774

Monepantel

(Synonyms: AAD1566; NUZ-001)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

Monepantel (AAD1566, NUZ-001), an antiparasitic agent, is an orally active mTOR inhibitor. Monepantel triggers autophagy through the deactivation of mTOR/p70S6K signalling pathway. Monepantel is a positive allosteric modulator of a nematode-specific clade of nAChR subunits. Monepantel can be used for the study of amyotrophic lateral sclerosis (ALS) and ovarian cancer.

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Reinheit: 99.98%
CAS. Nr.: 887148-69-8
Formel: C₂₀H₁₃F₆N₃O₂S
Molecular Weight:473.39

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Monepantel Chemical Structure

CAS. Nr.: 887148-69-8

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle mTOR Isoform-spezifische Produkte anzeigen :

Alle Parasite Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MCF-10A	IC₅₀	26.9 μM Compound: Monepantel	Cytotoxicity against human MCF-10A cells assessed as inhibition of cell viability measured after 48 hrs by DAPI staining based analysis Cytotoxicity against human MCF-10A cells assessed as inhibition of cell viability measured after 48 hrs by DAPI staining based analysis	[PMID: 32018095]

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.

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 887148-69-8
Appearance Solid
Molecular Weight 473.39
Formel C₂₀H₁₃F₆N₃O₂S
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
Synonyms

AAD1566; NUZ-001
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Journal Impact Factor

bioRxiv

2025 May 19.

Lösungsmittel & Löslichkeit

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1124 mL

10.5621 mL

21.1242 mL

5 mM

0.4225 mL

2.1124 mL

4.2248 mL

10 mM

0.2112 mL

1.0562 mL

2.1124 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protokoll

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.

MedChemExpress (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.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Hess J, et al. Assessment of the nematocidal activity of metallocenyl analogues of monepantel. Dalton Trans. 2016 Nov 28;45(44):17662-17671 [Content Brief]

[2]. Bahrami F, et al. Monepantel induces autophagy in human ovarian cancer cells through disruption of the mTOR/p70S6K signalling pathway. Am J Cancer Res. 2014 Sep 6;4(5):558-71. [Content Brief]

[3]. Raza A, et al. Increased expression of ATP binding cassette transporter genes following exposure of Haemonchus contortus larvae to a high concentration of monepantel in vitro. Parasit Vectors. 2016 Sep 29;9(1):522. [Content Brief]

[4]. Stuchlikova, et al. Monepantel induces hepatic cytochromes p450 in sheep in vitro and in vivo. Chem Biol Interact. 2015 Feb 5;227:63-8. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Monepantel

1 Cited Publications

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Monepantel

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Publications Citing Use of MedChemExpress (MCE) Monepantel

Alle mTOR Isoform-spezifische Produkte anzeigen

Alle Parasite Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Monepantel Related Classifications

HY-14774 Related Classifications