TABLE 1

Biochemical characterization of inhibition of SLx-4090 and its M1 metabolite SLx-4099 and CP-346086, a MTP inhibitor reference compound

CompoundAssay TypeValue
MTP-mediated lipid transferaSLx-40908.0 ± 0.8 (3)
SLx-4099262 ± 30 (3)
CP-3460862.0
ApoB secretion (primary hepatocytes)aSLx-409081 ± 15 (5)
SLx-40992720 ± 490 (5)
CP-346086N.D.
ApoB secretion (Caco-2 cells)aSLx-40909.6 ± 1.6 (5)
SLx-4099530 ± 50 (5)
CP-34608610
ApoA1 secretion (primary hepatocytes or Caco-2)bSLx-4090>30,000
SLx-4099>30,000
CP-346086>30,000
Caco-2 drug permeability (apical to basal)cSLx-40900
SLx-40990
CP-34608614
Caco-2 compound permeability (basal to apical)cSLx-40900
SLx-40991.01
CP-34608612

  • N.D., not determined.

  • ↵a IC50 nM ± S.E.M. (n).

  • ↵b Highest concentration tested.

  • ↵c Papp × 10−6 cm/s.