TABLE 1

Summary of in vitro models used in the present study

In Vitro Model	Transporter	Assay	Compound	Purpose
Parental Caco-2 monolayers	P-gp	Transcellular transport	EPAC, M9, M11, M12	Substrate and inhibition
Knock-out Caco-2 monolayers	P-gp	Transcellular transport	EPAC	Substrate
Knock-out Caco-2 monolayers	BCRP	Transcellular transport	EPAC	Substrate
Transfectant MDCKII monolayers	BCRP	Transcellular transport	EPAC, M9, M11, M12	Substrate and inhibition
Transfectant	OATP1B1, OATP1B3	Uptake	EPAC, M9, M11, M12	Substrate and inhibition
CHO cells	OATP1B1, OATP1B3	Uptake	EPAC, M9, M11, M12	Substrate and inhibition
Transfectant	OAT1, OCT2	Uptake	EPAC, M9, M11, M12	Inhibition
CHO cells		Uptake	EPAC, M9, M11, M12	Inhibition
Transfectant	OAT3	Uptake	EPAC, M9, M11, M12	Inhibition
Human embryonic kidney cells	OAT3	Uptake	EPAC, M9, M11, M12	Inhibition
Membrane vesicles	MRP2, MRP3, BCRP	Uptake	M9	Substrate