TABLE 2

Summary of kinetic data for DF and DF-AG for various human transporters in vitro

TransporterSystemKm ± S.E. of the Parameter Estimate
DFDF-AG
µMµM
OAT2HEK-293 Cells46.8 ± 12.28.6 ± 1.9
OATP1B1HEK-293 Cellsa34.0 ± 8.6
OAT1HEK-293 Cellsa60.2 ± 13.5
OAT4HEK-293 Cellsa103.9 ± 29.0
OATP2B1HEK-293 Cellsa104.6 ± 16.7
OAT3HEK-293 Cellsa114.1 ± 8.1
MRP2Vesiclesa145.0 ± 7.8b
BCRPVesiclesa152.0 ± 54.9
MRP3Vesiclesa196.3 ± 58.0
OATP1B3HEK-293 Cellsa
  • a No detectable transport.

  • b Reported as S50; Hill Coefficient = 3.19 ± 0.34.