TABLE 3

The effect of different inhibitors on creatinine transport by OAT2, or metformin transport by OCT2, MATE1, and MATE2K

Data are expressed as mean ± SD (n = 3).

DrugIC50 (µM)a,b
OAT2OCT2MATE1MATE2K
CMD62.3 ± 25.1 (0.67)200.4 ± 55.1 (1.18)2.3 ± 0.3 (1.14)13.5 ± 4.1 (0.78)
BSP1.3 ± 0.4 (0.87)>100>100>100
IMC2.1 ± 0.4 (0.90)>200>200>200
Pyrimethamine>505.1 ± 0.8 (1.26)0.11 ± 0.04 (0.94)0.15 ± 0.01 (0.96)
Cyslosporine A>11.1>11.1>11.1>11.1
Metformin>1100NDNDND
Rosuvastatin33.6 ± 5.1 (0.93)NDNDND

  • ND, not determined.

  • ↵a IC50 values were determined at 2 µM creatinine-d3 (OAT2) or 2 µM [14C]metformin (OCT2, MATE1, and MATE2K).

  • ↵b Hill coefficients that describe the steepness of inhibition curves are listed in parentheses.