STP0404 to activate PXR, and thereby to induce CYP3A4 expression in DPX2 cell lines following in vitro administration. DPX2 cells were treated with STP0404 at 0.0977, 0.391, 1.56, 6.25, 25.0 and 100 μM at 37°C for a total of 48 hrs with the change of incubation medium every 24 hrs. After 48 hrs incubation, the cell viability was assessed fluorimetrically via CellTiter-FluorTM. CYP3A-mediated metabolism and PXR activation are measured using luminescence with Luciferin-IPA and ONE-GloTM, respectively. The light intensity is directly proportional to the extent of PXR activation and accompanying gene transcription in the DPX2 cells (Wuxi AppTec, China).

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