Compound | Test System | Substrate | IC50 | Reference |
---|---|---|---|---|
µM | ||||
Cyclosporin A | Sf9 vesicles | GCA (2) | 0.93, 1.2 | Kis et al., 2009; Yucha et al., 2017 |
SHHa | TCA (2) | 18.9, 0.5, 2.2 | Kis et al., 2009; Morgan et al., 2013; Yucha et al., 2017 | |
SK-E2 cells | G-CDCA (2) | 9.4 | Kis et al., 2009 | |
T-CDCA (2) | 0.94 | Kis et al., 2009 | ||
GCAb | 0.1, 0.27 | Zhang et al., 2016; Yucha et al., 2017 | ||
TCAb | 0.3 | Yucha et al., 2017 | ||
G-CDCAc | 22.8 | Yucha et al., 2017a | ||
T-CDCAc | 100 | Yuch et al., 2017a | ||
H2FDA (0.2) | 7.8 | Wang et al., 2003 | ||
Itraconazole | Sf9 vesicles | TCA (2) | 18, 22.1 | Morgan et al., 2013; Yucha et al., 2017 |
HEK-293 vesicles | GCA (2) | 4.8 | Yucha et al., 2017 | |
SHHa | TCA (0.1) | 3 | Lempers et al., 2016 | |
GCAb | 100 | Yucha et al., 2017 | ||
TCAb | 100 | Yucha et al., 2017 | ||
G-CDCAc | 100 | Yucha et al., 217a | ||
T-CDCAc | 100 | Yucha et al., 2017a | ||
Reserpine | Sf9 vesicles | TCA (2) | 2.8, 8.4 | Kis et al., 2009; Morgan et al., 2013 |
SK-E2 cells | H2FDA (0.2) | 10.2 | Wang et al., 2003 | |
Troglitazone | Sf9 vesicles | TCA (2) | 9.5, 3 | Kis et al., 2009; Morgan et al., 2013 |
SHHa | GCA (2) | 16 | Yucha et al., 2017 | |
SK-E2 cells | GCAb | 0.48, 1.2 | Zhang et al., 2016; Yucha et al., 2017 | |
TCAb | 0.6 | Yucha et al., 2017 | ||
G-CDCAc | 5.9 | Yucha et al., 2017 | ||
T-CDCAc | 26.6 | Yucha et al., 2017 | ||
H2FDA (0.2) | 66.4 | Wang et al., 2003 | ||
Bosentan | Sf9 vesicles | TCA (2) | 23, 25.4 | Morgan et al., 2013; Yucha et al., 2017 |
SHHa | GCA (2) | 14.4 | Yucha et al., 2017 | |
GCAb | 9.2, 26.5 | Zhang et al., 2016; Yucha et al., 2017 | ||
TCAb | 26.6 | Yucha et al., 2017 | ||
G-CDCAc | 100 | Yucha et al., 2017 | ||
T-CDCAc | 100 | Yucha et al., 2017 | ||
Simvastatin | Sf9 vesicles | TCA (2) | 24.7 | Morgan et al., 2013 |
Loratadine | Sf9 vesicles | TCA (2) | 12 | Morgan et al., 2013 |
Valinomycin | Sf9 vesicles | TCA (2) | 1.56 | Morgan et al., 2013 |
SK-E2 cells | H2FDA (0.2) | 7.2 | Wang et al., 2003 | |
Lovastatin | Sf9 vesicles | TCA (2) | 19.3 | Morgan et al., 2013 |
SHHa | GCAb | 1.7 | Zhang et al., 2016 |
H2FDA, dihydrofluorescein; Sf9, Spodoptera frugiperda.
↵a Suspension human hepatocytes.
↵b Suspension human hepatocytes were incubated with cholic acid (10 µM), and the efflux of GCA or TCA was measured.
↵c Suspension human hepatocytes were incubated with chenodeoxycholic acid (10 µM), and the efflux of G-CDCA or T-CDCA was measured.