TABLE 1

Summary for Km and IC50 values obtained in this study

The concentration-dependent uptake and inhibition profile of YM758 were investigated using mock, rOct1, hOCT1, and OATP1B1-HEK293 cells, LLC-MDR1 cells, and human hepatocytes. The Km and IC50 values were determined by nonlinear regression analysis as described under Material and Methods.


Cell Lines

Substrate

Inhibitor

Km

IC50
μM μM
Mock-HEK293 YM758 135
rOct1-HEK293 MPP YM758 23.8
rOct1-HEK293 Metformin YM758 <10.0
hOCT1-HEK293 MPP YM758 40.5
OATP1B1-HEK293 E217βG YM758 13.0
LLC-MDR1 YM758 20.9
Human hepatocyte YM758 87.9
Human hepatocyte
YM758
Quinidine

147