Chalepensin
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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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- 純度: 98.98%
- CAS 番号: 13164-03-9
- 分子式: C16H14O3
- 分子量:254.28
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保管条件:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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生物活性
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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) |
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.
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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.
化学情報
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CAS 番号 13164-03-9
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性状 Solid
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分子量 254.28
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)