TABLE 1

Km and Ki for rOat1, rOat3, and RFC-1 The Km and Ki values for the uptake by rOat1- and rOat3-LLC-PK1 cells, and by RFC-1-MDCKII cells was determined by nonlinear regression analysis. Compounds in parentheses represent substrates for determination of Ki values.


Substrate/Inhibitor

rOat1

rOat3

RFC-1
μM μM μM
PAH Km = 47.0a, 59.9b Ki = 398a (PCG), 1350b (pravastatin) Ki > 1000 (MTX)
PCG Ki = 418b, 800a (PAH) Km = 82.6a Ki = 52.8b (pravastatin) Ki > 1000 (MTX)
5-MTHF
Ki > 1000 (MTX)
Ki > 1000 (MTX)
Ki = 5.03 ± 3.05c (MTX)