TY - JOUR
T1 - Data demonstrating the challenges of determining the kinetic parameters of P-gp mediated transport of low-water soluble substrates
AU - Ozgür, Burak
AU - Saaby, Lasse
AU - Langthaler, Kristine
AU - Brodin, Birger
PY - 2018
Y1 - 2018
N2 - The presented data are related to the research article entitled “Characterization of the IPEC-J2 MDR1 (iP-gp) cell line as a tool for identification of P-gp substrates” by Ozgur et al. (2017). This data report describes the challenges of investigating the concentration-dependent transport of P- glycoprotein (P-gp) substrates with relatively low aqueous solubility. Thus, we provide solubility data on two prototypical P-gp substrates, digoxin and rhodamine 123, representing P-gp substrates with a relatively low and high-aqueous solubility, respectively. We present a hypothetical Michaelis-Menten curve of the P-gp mediated transport of digoxin to demonstrate that the maximal donor concentration, which can be reached in the experimental transport buffer, is too low to yield transport data in the saturable range of the MichaelisMenten relationship. Furthermore, we present data on the bidirectional transport of digoxin and rhodamine 123 across cell monolayers of the MDCK II MDR1 cell line and iP-pg cell line in the presence of the selective P-gp inhibitor, zosuquidar/LY335979.
AB - The presented data are related to the research article entitled “Characterization of the IPEC-J2 MDR1 (iP-gp) cell line as a tool for identification of P-gp substrates” by Ozgur et al. (2017). This data report describes the challenges of investigating the concentration-dependent transport of P- glycoprotein (P-gp) substrates with relatively low aqueous solubility. Thus, we provide solubility data on two prototypical P-gp substrates, digoxin and rhodamine 123, representing P-gp substrates with a relatively low and high-aqueous solubility, respectively. We present a hypothetical Michaelis-Menten curve of the P-gp mediated transport of digoxin to demonstrate that the maximal donor concentration, which can be reached in the experimental transport buffer, is too low to yield transport data in the saturable range of the MichaelisMenten relationship. Furthermore, we present data on the bidirectional transport of digoxin and rhodamine 123 across cell monolayers of the MDCK II MDR1 cell line and iP-pg cell line in the presence of the selective P-gp inhibitor, zosuquidar/LY335979.
U2 - 10.1016/j.dib.2017.11.092
DO - 10.1016/j.dib.2017.11.092
M3 - Journal article
C2 - 29541662
VL - 16
SP - 655
EP - 659
JO - Data in Brief
JF - Data in Brief
SN - 2352-3409
ER -