BSEP inhibition (BSEP-HEK membrane vesicles, taurocholic acid substrate) - US

Background Information:

The human Bile Salt Export Pump (BSEP) is an ABC transporter that uses ATP to transport substrates across the cell membrane (efflux). BSEPs mainly express in hepatocytes. They are the major transporters that clear bile acids from hepatocytes to bile duct. Therefore, the inhibition of the BSEP transporters plays a major role in drug induced liver injury (DILI). An effective way to assess the inhibition of BSEP is using inside-out vesicles prepared from HEK293 cells stably expressing human BSEP. This assay uses LC-MS to quantify the amount of Taurocholic Acid, an endogenous BSEP substrate, accumulated inside the vesicles in the presence and absence of the test compounds in 96-well plates to determine the inhibition effect of the test compounds. The compounds can be tested at 1 concentration (n=2) for screening or at multiple concentrations (n=2) for IC50 determination.

Family:

Transporter

Sub Family:

ABCG

Class:

ABC

Organism:

Human

Cell Type:

HEK293