In vitro characteristics of the study compounds FXRA/sEHi DM and sEHi MH. (a) Effects of the study compounds
on expression levels of selected FXR-regulated genes in human hepatocytes
(HepG2). Data are mean ± S.E.M. fold mRNA induction compared
to DMSO (0.1%) treated cells, n = 5. *, p < 0.05; **, p < 0.01; and ***, p < 0.001 (t-test) vs DMSO (0.1%). CDCA vs CDCA+MH were not statistically different. (b) Selectivity profiles
of the study compounds over relevant members of the nuclear receptor
family. The heat map shows mean relative activation compared to the
respective reference agonist, n = 5. (c) Microsomal
stability of the study compounds. Data are mean ± S.E.M. remaining
parent compound, n = 5.