IC50 values of YM758 metabolites for the uptake of MPP by hOCT1–3 and rOct1–3 HEK293 cells
IC50 values were estimated from the mean value of MPP uptake in the presence of each compound (n = 3) by nonlinear regression analysis as described under Materials and Methods.
Compounds | IC50 | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| hOCT1 | hOCT2 | hOCT3 | rOct1 | rOct2 | rOct3 | ||||||
| μM | |||||||||||
| YM-385459 | No inhibition | No inhibition | No inhibition | No inhibition | No inhibition | No inhibition | |||||
| YM-252124 | 145 | 93.9 | 63.4 | 41.9 | 1700 | 22.7 | |||||
| YM-385461 | No inhibition | No inhibition | No inhibition | No inhibition | No inhibition | No inhibition | |||||
| AS2036329 | No inhibition | ∼1000 | >100 | No inhibition | No inhibition | No inhibition | |||||
| YM758 | 40.5* | 456 | 15.9 | 23.8* | 137 | 20.4 | |||||