Intestinal Drug Transporter Knockout Models

Caco-2 cells are human intestinal epithelium cells that express multiple drug transporters and grow in a tight homogenous monolayer. Caco-2 cells are commonly used to predict human intestinal drug permeability and to investigate drug efflux.
To aid in the investigation of drugs¢ absorption across the human intestinal epithelium, Sigma has generated transporter knockout (KO) Caco-2 cell lines using CompoZr Zinc Finger Nuclease (ZFN) technology. Sigma offers Caco-2 control cells and transporter KO cell lines as Assay Ready Plates.

Features and Benefits:
  • Ease of use: Supplied to the customer on day 16 of the 21 day culturing process, in either 24 well or 96 well transwell plate format, to reduce hands on time and permit easy manual or automated processing
  • Reproducible, standardized results: Products are produced in a dedicated facility under a rigorous quality management system to ensure reproducible results
  • Highly predictive: Transporter KO cell lines eliminate the ambiguity from non-specific substrates and inhibitors
  • Meet regulatory guidelines: The drug transporters targeted include those referenced in the regulatory guidance for investigating drug-drug interactions (DDI) from the US Food and Drug Administration (FDA), the European Medicines Agency (EMA), and the Japanese Ministry of Health, Labour, and Welfare (MHLW): MDR1 (P-gp), BCRP, MRP2; and those of emerging clinical importance: MRP1, MRP3, MRP4, MRP5, MRP6 and MRP7