TABLE 1

Kinetic parameters of vildagliptin-hydrolyzing activity

Enzyme Source	Affinity Site	K_m	V_max
		µM	pmol/h/mg protein
Human liver S9 fraction^{^a}	High	1.95 ± 0.57	0.25 ± 0.04
	Low	335 ± 9.59	4.97 ± 0.10
Human liver cytosol^{^a}	High	2.34 ± 0.96	0.18 ± 0.04
	Low	189 ± 5.04	3.18 ± 0.07
Human liver microsomes^{^a}	High	0.75 ± 0.42	0.69 ± 0.08
	Low	448 ± 104	10.8 ± 2.82
hDPP-4^{^b}	High	0.62 ± 0.10	11.4 ± 0.79
	Low	151 ± 71.2	11.5 ± 1.55