Microsomes

A further insight into the metabolic profile of the nuclear receptor Rev-erb agonist, SR9009

The reactions involved in the metabolic pathways of SR9009 were characterized by liquid chromatography–mass spectrometry (LC–MS) to identify the most appropriate marker(s) of use. The effects of gender, genetic polymorphism, and drug–drug interaction on the metabolic profile of SR9009 were also evaluated. In vitro approaches were based on the use of human liver microsomes and cytochrome P450 isoforms. Sample preparation included an enzymatic hydrolysis (performed only for the phase II investigation) followed by liquid–liquid extraction.

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