TABLE 2

Ki values (μM) obtained with five probe substrates, i.e, (S)-flurbiprofen, (S)-warfarin, phenytoin, tolbutamide, and diclofenac, using CYP2C9.3

Global standard error for data fitting was less than 15% and r2 > 0.9 for each effector.


Inhibitors

Flurbiprofen

Warfarin

Phenytoin

Tolbutamide

Diclofenac
Mibefradil 13.08 1.80 6.90 6.90 14.30
Indomethacin 38.74 5.04 12.66 16.87 25.62
Benzbromarone 1.54 0.01 0.71 0.03 0.04
Sulfaphenazole 0.72 0.15 0.39 0.33 0.36
Nicardipine 0.29 0.01 0.02 0.02 0.02
(S)-Ibuprofen 9.78 3.15 5.50 14.03 14.68
Amiodarone 3.64 1.66 1.87 0.81 2.10
Sulfamethizole 35.04 3.87 24.74 25.93 31.86
Omeprazole 16.24 0.90 1.60 1.46 0.30
Clozapine 10.49 2.80 5.07 5.92 8.04
Gemfibrozil 14.33 1.65 4.95 7.21 14.41
Ketoconazole 1.51 0.08 0.69 0.70 0.79
Progesterone 11.03 1.97 3.27 2.58 7.91
Nifedipine 1.53 0.28 0.61 0.28 1.18
Thiobendazole >100 11.02 26.92 24.54 69.85
Quinine 21.2 18.89 39.68 86.52 96.70
Quercetin 0.25 0.11 0.29 0.08 0.13
Fluvoxamine 4.19 0.67 2.37 1.57 2.53
Tamoxifen 9.77 0.58 6.69 2.72 8.36
Miconazole 0.10 0.02 0.12 0.06 0.07
α-Naphthoflavone 1.13 0.18 0.39 0.24 0.44
Diclofenac 5.34 1.16 3.32 2.58
Flurbiprofen 5.27 23.15 33.49 23.66
Warfarin 2.70 11.12 5.89 12.21
Phenytoin 24.20 5.93 6.99 16.53
Tolbutamide 12.91 2.30 5.51 9.54
Piroxicam 19.38 1.27 8.67 7.40 6.05
Vivid Green 1.59 0.44 0.70 2.53 0.84
Dapsone
>100
0.26
10.47
12.76
15.62