Chalepensin 

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^[1][2].

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.

254.28

C₁₆H₁₄O₃

13164-03-9

Solid

White to off-white

O=C1C(C(C)(C)C=C)=CC2=CC3=C(OC=C3)C=C2O1

Room temperature in continental US; may vary elsewhere.

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

• [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]