TABLE 3

Uptake kinetic parameters of seven OATP substrates estimated in rat hepatocytes by using a two-compartment mechanistic model

Uptake kinetics was measured in freshly isolated rat hepatocytes plated for 2 h over 2 or 45–90 min at 10 concentrations (0.1–300 μM). Data represent mean of three experiments ± S.D.

Drug	K_m,u^{^a}	V_max	P_diff,u^{^a}	fu_cell	CL_active,u^{^a}	Maximal Proportion of Active Transport
	μM	pmol/min/10⁶ cells	μl/min/10⁶ cells		μl/min/10⁶ cells	%
Bosentan
2 min	14.2 ± 1.1	883 ± 108	6.75 ± 0.64	0.104 ± 0.022	62.1 ± 3.8	90.2 ± 0.5
60 min	6.4	488	13.5	0.096	76.6	85.0
Pitavastatin
2 min	11.6 ± 2.1	1055 ± 153	8.12 ± 2.42	0.031 ± 0.033	95.4 ± 34.4	91.4 ± 4.0
90 min	6.3	747	10.9	0.053	119	91.6
Pravastatin
2 min	37.0 ± 20.1	500 ± 412	0.358 ± 0.298	1.0 ± 0.0	12.5 ± 4.1	97.4 ± 1.4
45 min	23.4	223	1.29	0.778	9.5	88.0
Repaglinide
2 min	28.0 ± 17.2	1393 ± 934	4.49 ± 3.82	0.386 ± 0.538	48.8 ± 2.8	92.0 ± 6.8
45 min	8.8	586	24.0	0.050	66.3	73.4
Rosuvastatin
2 min	14.6 ± 1.8	1218 ± 97	0.855 ± 0.459	0.507 ± 0.430	83.8 ± 6.8	99.0 ± 0.6
45 min	11.2	978	1.01	0.477	87.6	98.9
Telmisartan
2 min	3.41 ± 1.95	337 ± 202	21.4 ± 16.0	0.010 ± 0.009	98.8 ± 43.5	80.9 ± 12.4
90 min	2.32	160	22.5	0.024	68.7	75.3
Valsartan
2 min	6.38 ± 0.95	159 ± 70	0.184 ± 0.118	1.0 ± 0.0	26.4 ± 15.2	99.2 ± 0.5
90 min	2.7	117	0.37	1.0	43.3	99.1

↵a Parameters are expressed relative to unbound media drug concentration.