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However, in several cases the sulfonation reaction can lead to formation of a more active metabolite compared to the parent compound as is the case for the hair follicle stimulant minoxidil (Buhl et al., 1990) or the diuretic agent triamterene (Mutschler et al., 1983)

Although the maximum plasma concentration is lower when compound 2 is administered PO (0.77 M) instead of IP (4.8 M), it is still 4.3-fold higher than LD 50 for ex vivo NTS determined in the commonly used 72 h assay, also indicating that TGR inhibitor 2 is orally bioavailable and the initial prediction of oral bioavailability based on the Lipinski et al