TABLE 2

Estimation of the contribution ratio of RKIP and hCE2 involved in the formation of the thiolactone metabolite from prasugrel in human small intestinal S9 by the enzymatic kinetic parameters

The contents of RKIP and hCE2 in individual human small intestinal S9 (n = 4) were determined using recombinant RKIP and PNGase F-treated hCE2 by Western blotting method. The contribution ratio of RKIP and hCE2 involved in the hydrolysis reaction of prasugrel in human small intestinal S9 was estimated by using the obtained contents data and enzyme kinetic parameters.

Vmax/KmIndividual Human Small Intestinal S9Enzyme ContentsCLintContribution Ratio (%)
μl/min/μg proteinng/human small intestinal S9 μg)μl/min/μg enzyme contents
RKIP283HIS-063-S314.9421752.742.99.82
HIS-067-S312.8362229.4
HIS-084-S315.6441543.4
HIS-111-S37.48211746.2
hCE21101HIS-063-S33.44378747.357.19.82
HIS-067-S37.91870970.6
HIS-084-S35.24576956.6
HIS-111-S32.24246653.8