Monepantel - Moligand™, ≥99% , CAS No.887148-69-8

CAS: 887148-69-8 Cat. No.: M648780 Peso molecular: 473.39 Número EC: 639-775-0 PubChem CID: 44449087

GRADE & PURITY Moligand™, ≥99%

Synonyms

AAD1566 | PPL-1

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Descripción general

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. Monepantel (25 µM) induces accumulation of acidic vacuoles. Ovarian cancer cell lines are highly sensitive to Monepantel with IC 50 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. 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. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay

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.

Form:Solid

Specifications

Sinónimos

AAD1566 | PPL-1

Especificaciones y pureza

Moligand™, ≥99%

Mecanismos bioquímicos y fisiológicos

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

Condiciones de almacenamiento de almacenamiento

Store at -20°C

Enviado en

Ice chest + Ice pads

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

AGONIST

Pureza

≥99%

Nombres e identificadores

• Isómeros SMILES: C[C@@](COC1=C(C=CC(=C1)C#N)C(F)(F)F)(C#N)NC(=O)C2=CC=C(C=C2)SC(F)(F)F
• PubChem CID: 44449087
• Peso molecular: 473.39

Objetivos asociados (no humanos)

Haemonchus contortus (724 Activities)

Explore this target

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Trichostrongylus colubriformis (210 Activities)

Explore this target

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Mecanismos de acción

Propiedades químicas y físicas

• Solubilidad: DMSO : ≥ 100 mg/mL (211.24 mM)
• Peso molecular: 473.400 g/mol
• XLogP3: 5.200
• Hydrogen Bond Donor Count: 1
• Hydrogen Bond Acceptor Count: 11
• Rotatable Bond Count: 6
• Exact Mass: 473.063 Da
• Monoisotopic Mass: 473.063 Da
• Topological Polar Surface Area: 111.000 Ų
• Heavy Atom Count: 32
• Formal Charge: 0
• Complexity: 763.000
• Isotope Atom Count: 0
• Defined Atom Stereocenter Count: 1
• Undefined Atom Stereocenter Count: 0
• Defined Bond Stereocenter Count: 0
• Undefined Bond Stereocenter Count: 0
• The total count of all stereochemical bonds: 0
• Covalently-Bonded Unit Count: 1