TABLE 1

Michaelis-Menten kinetics parameters of bosentan hydroxylase activity of mutant CYP2C9 alleles in recombinant microsomes compared with that of wild-type CYP2C9^*1

Variant	V_max	K_m	Clearance	Relative clearance (/CYP2C9^*1)
	nmol/min per pmol of CYP2C9	μM	V_max/K_m	%
CYP2C9^*1	52.110 ± 1.000	36.840 ± 2.694	1.089 ± 0.091	100.00
CYP2C9^*2	38.380 ± 1.579^*	15.110 ± 3.049	2.598 ± 0.310^*	238.57
CYP2C9^*3	37.930 ± 0.289^*	17.540 ± 0.625	2.152 ± 0.078^*	197.61
CYP2C9^*8	7.463 ± 0.317^*	25.020 ± 4.485	0.315 ± 0.030^*	28.93
CYP2C9^*11	32.750 ± 0.553^*	15.430 ± 1.269	2.141 ± 0.192^*	196.60
CYP2C9^*13	1.878 ± 0.221^*	199.600 ± 56.320^*	0.010 ± 0.002^*	0.92
CYP2C9^*14	25.800 ± 0.522^*	15.590 ± 1.530	1.672 ± 0.107	153.54
CYP2C9^*16	22.420 ± 0.451^*	37.090 ± 2.839	0.611 ± 0.025	56.11
CYP2C9^*19	1.080 ± 0.051^*	58.860 ± 9.328	0.018 ± 0.002^*	1.65
CYP2C9^*23	25.980 ± 0.786^*	30.430 ± 3.685	0.919 ± 0.040	84.39
CYP2C9^*27	126.600 ± 4.216^*	48.590 ± 5.753	2.628 ± 0.089^*	241.32
CYP2C9^*29	34.410 ± 0.574^*	50.120 ± 2.950	0.691 ± 0.020	63.45
CYP2C9^*31	23.530 ± 0.817^*	53.630 ± 6.455	0.442 ± 0.006	40.59
CYP2C9^*33	2.933 ± 0.073^*	24.730 ± 2.620	0.118 ± 0.001^*	10.84
CYP2C9^*34	26.790 ± 0.935^*	36.160 ± 4.832	0.744 ± 0.062	68.32
CYP2C9^*36	104.900 ± 3.468^*	28.280 ± 3.815	4.448 ± 1.286^*	408.45
CYP2C9^*37	20.600 ± 0.443^*	28.330 ± 2.486	0.729 ± 0.014	66.94
CYP2C9^*38	47.900 ± 0.892^*	28.390 ± 2.154	1.692 ± 0.111	155.37
CYP2C9^*39	2.456 ± 0.086^*	23.910 ± 3.580	0.104 ± 0.006^*	9.55
CYP2C9^*40	22.090 ± 0.112^*	17.580 ± 0.415	1.253 ± 0.024	115.06
CYP2C9^*41	40.610 ± 0.958	33.300 ± 3.072	1.223 ± 0.049	112.30
CYP2C9^*42	3.110 ± 0.065^*	27.250 ± 2.360	0.113 ± 0.005^*	10.38
CYP2C9^*43	0.632 ± 0.069^*	232.300 ± 57.720^*	0.006 ± 0.000^*	0.55
CYP2C9^*44	33.950 ± 1.822^*	33.910 ± 7.081	1.004 ± 0.072	92.19
CYP2C9^*45	24.790 ± 1.713^*	26.950 ± 7.698	0.918 ± 0.008	84.30
CYP2C9^*46	38.900 ± 0.770^*	39.840 ± 2.944	0.977 ± 0.008	89.72
CYP2C9^*47	47.830 ± 1.156	28.180 ± 2.781	1.698 ± 0.017	155.92
CYP2C9^*48	62.080 ± 1.792^*	33.380 ± 3.765	1.866 ± 0.108^*	171.35
CYP2C9^*49	27.080 ± 0.511^*	26.840 ± 2.093	1.014 ± 0.011	93.11
CYP2C9^*50	44.230 ± 1.991	51.840 ± 8.159	0.855 ± 0.032	78.51
CYP2C9^*51	55.560 ± 0.682^*	26.290 ± 1.342	2.116 ± 0.070^*	194.31
CYP2C9^*52	4.615 ± 0.066^*	25.880 ± 1.538	0.178 ± 0.002^*	16.35
CYP2C9^*53	40.220 ± 0.942^*	23.300 ± 2.348	1.737 ± 0.035	159.50
CYP2C9^*54	37.650 ± 0.535^*	46.710 ± 2.381	0.809 ± 0.035	74.29
CYP2C9^*55	66.040 ± 2.726^*	12.320 ± 2.676	5.324 ± 0.114^*	488.89
CYP2C9^*56	69.980 ± 1.566^*	35.140 ± 3.032	1.954 ± 0.070^*	179.43
CYP2C9^*58	32.090 ± 2.946^*	45.240 ± 15.030	0.521 ± 0.013	47.84
CYP2C9^*59	7.691 ± 0.408^*	27.200 ± 5.943	0.154 ± 0.008^*	14.14
CYP2C9^*60	13.590 ± 0.399^*	18.220 ± 2.476	1.263 ± 0.007	115.98

↵* Significantly different from wild-type CYP2C9, *P < 0.05.