Chalepensin
Based on 1 Customer Validation
Chalepensin is a nematicide and CYP inhibitor. Chalepensin inhibits CYP2A6, CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 to varying degrees, with IC50 values of 82.3 μM, 2.86 μM, 3.01 μM, 0.21 μM, 6.58 μM, 1.67 μM, 61.1 μM, and 61.7 μM, respectively. Chalepensin potently and selectively kills third-stage infective larvae of Strongyloides venezuelensis.
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- Reinheit : 98.98%
- CAS. Nr.: 13164-03-9
- Formel: C16H14O3
- Molecular Weight:254.28
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Speicherung:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
CYP2A6 82.3 μM (IC50) |
CYP1A1 2.86 μM (IC50) |
CYP1A2 3.01 μM (IC50) |
CYP2A13 0.21 μM (IC50) |
CYP2C9 6.58 μM (IC50) |
CYP2D6 1.67 μM (IC50) |
CYP2E1 61.1 μM (IC50) |
CYP3A4 61.7 μM (IC50) |
In Vitro
Chalepensin inhibits CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 to varying degrees[1].
Chalepensin (1-50 μM; 24-72 h) potently and selectively kills third-stage infective larvae (L3) of *Strongyloides venezuelensis*, with an LC50 of 3.4 µM at 72 h and a selectivity index of 990.0, exhibiting activity comparable to that of ivermectin[2].
Chalepensin (1-60 μM; 24-72 h) potently and selectively kills parthenogenetic adult females of *Onchocerca volvulus*, with an LC50 of 16.8 μM at 72 h and a selectivity index of 200.4; this compound exhibits superior activity to graveoline and comparable activity to ivermectin at low concentrations[2].
Chalepensin (10 μM-6 mM; 72 h) exhibits extremely low cytotoxicity against Vero cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:African green monkey kidney epithelial (Vero, ATCC CCL-81) cells
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Concentration:10 μM-6 mM
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Incubation Time:72 h
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Result:Showed minimal cytotoxicity to Vero cells with an IC50 of 3365.9 μM at 72 h.
Chemical Information
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CAS. Nr. 13164-03-9
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Appearance Solid
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Molecular Weight 254.28
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Formel C16H14O3
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Color White to off-white
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SMILES
O=C1C(C(C)(C)C=C)=CC2=CC3=C(OC=C3)C=C2O1
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Structure Classification
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Initial Source
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Reinheit & Dokumentation
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Ueng YF, et al. Mechanism-based inhibition of CYP1A1 and CYP3A4 by the furanocoumarin chalepensin. Drug Metab Pharmacokinet. 2013;28(3):229-238. [Content Brief]
[2]. Rodríguez-Garza NE, et al. Antiparasitic Activity of Chalepensin and Graveoline Isolated from Ruta chalepensis L.: In Vitro Evaluation Against Strongyloides venezuelensis. Pathogens. 2025 Apr 25;14(5):419. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)