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

Monepantel (Synonyms: AAD1566)

Cat. No.: HY-14774 Purity: 99.91%
Handling Instructions

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

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

Monepantel Chemical Structure

Monepantel Chemical Structure

CAS No. : 887148-69-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 437 In-stock
Estimated Time of Arrival: December 31
1 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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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].

In Vivo

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

Molecular Weight

473.39

Formula

C₂₀H₁₃F₆N₃O₂S

CAS No.

887148-69-8

SMILES

O=C(N[[email protected]@](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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (211.24 mM)

*"≥" 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
10 mM 0.2112 mL 1.0562 mL 2.1124 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.28 mM); Clear solution

*All of the co-solvents are provided by MCE.
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
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Monepantel
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