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. 2014 Jul 8;2014:431858. doi: 10.1155/2014/431858

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Copyright © 2014 Jeremy H. Toyn et al.

This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

PMC Copyright notice

BMS-869780 caused PXR activation in vitro and lipidosis in rat liver. (a) PXR activation in the presence of BMS-869780 was evaluated in HepG2 cell cultures using a luciferase transcriptional reporter construct (●), or by assay of CYP3A4 mRNA levels in primary human hepatocyte (PHH) cultures from two individual donors (▲ and ▼). Activation in both assays is expressed as % relative to activation in the presence of rifampicin, 10 μM, in parallel cultures. (b) Liver section from vehicle-dosed rats. (c) Liver section from rats given 4 daily doses of BMS-869780 at 100 mg/kg. A summary of the plasma BMS-869780 exposures from this experiment is shown in Table 5.