Ebelin lactone

Ebelin lactone (0.125 mg/mL; 2 hours) shows intestinal permeability in Caco-2 cells with an absorptive P_app of 121 × 10^-6 cm/s and an efflux ratio of 0.647^[1].
Ebelin lactone is non-toxic to HEK293T kidney epithelial cells (IC₅₀ ~0.9 mg/mL) and HFF-1 skin fibroblast cells (IC₅₀ ~0.862 mg/mL)^[1].
Ebelin lactone exhibits strong estimated binding affinity to 5-HT_1A, 5-HT_2A, D₁, D₂, and M₁ CNS receptors and human AChE via allosteric non-polar interactions, with the lowest binding energy (-11.71 kcal/mol) observed for the M₁ receptor^[3].
Ebelin lactone meets key CNS drug-like criteria and has very high predicted BBB penetration with moderate intestinal absorption^[3].
Ebelin lactone (up to 30 μM) binds to human M₁ (CHO cell-expressed) and 5-HT_2A (CHO cell-expressed) receptors with K_i values of 0.45 μM and 4.21 μM, respectively, and does not bind to 5-HT_1A, D₁, or D_2S receptors^[3].
Ebelin lactone (up to 30 μM; 30 min pre-incubation) does not inhibit human recombinant AChE (HEK293 cell-expressed)^[3].
Ebelin lactone inhibits proliferation of MDA-MB-468 breast cancer cells with an IC₅₀ of 0.210 mg/mL and HCT116 colorectal cancer cells with an IC₅₀ of 0.055 mg/mL^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.