||Recombinant Human ABCC2 was produced inSf9 cells.
||MRP2 (ABCC2) is an organic anion transporter found in the liver, kidney, and gut epithelium apical membranes. The transport of glucuronate conjugates plays a role in the detoxification of endogenous and xenobiotic substances, and may cause multidrug resistance (MDR) in tumor cells.
||Supplied as isolated Sf9 cell membranes containing human MRP2 suspended in TMEP solution.
||The vesicular transport assay determines the interaction of compounds with the MRP2 transporter. The interaction is detected by changes in the initial rate of 3H-β-estradiol 17-(β-D-glucuronide) transport by MRP2 into membrane vesicles purified from Sf9 cells expressing the transporters. Membrane preparations from infected cells always contain some closed membrane vesicles that have an inside-out orientation (5-10% of total lipid). In the case of these inside-out vesicles, transport of substrates across the membrane takes molecules from the surrounding buffer and transports them into the vesicles.
||The quantity of transported molecules can be determined by methods such as HPLC, LC/MS/MS separation and detection, and also by labeling with fluorescent or radioactive (3H-β-estradiol 17-(β-D-glucuronide) tags. MRP2 mediates the transport of β-estradiol 17-(β-D-glucuronide) (E217βG) very efficiently. Compounds that interact with the transporter modulate the initial rate of E217βG transport measured without any other compounds added. If a substance is a transported substrate of the transporter, it might compete with E217βG, thus reducing the rate of E217βG transport. If a compound is an inhibitor of the transporter, it will block the transport of E217βG into the membrane vesicles. Some compounds can be co-transported with E217βG increasing the rate of E217βG transport compared to the control level.