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Caco-2 permeability assay

Understand the suitability of your compound for oral dosing by using our Caco-2 permeability assay to predict human intestinal permeability and to investigate drug efflux.

Caco-2 permeability is included in our portfolio of in vitro ADME screening services. Cyprotex deliver consistent, high quality data with cost-efficiency that comes from a highly automated approach.


Caco-2 permeability assay to investigate intestinal permeability

  • Cyprotex's Caco-2 Permeability assay uses an established method for predicting the in vivo absorption of drugs across the gut wall by measuring the rate of transport of a compound across the Caco-2 cell line.
  • The Caco-2 cell line is derived from a human colon carcinoma. The cells have characteristics that resemble intestinal epithelial cells such as the formation of a polarized monolayer, well-defined brush border on the apical surface and intercellular junctions.
  • Assessing transport in both directions (apical to basolateral (A-B) and basolateral to apical (B-A)) across the cell monolayer enables an efflux ratio to be determined which provides an indicator as to whether a compound undergoes active efflux.
  • The P-glycoprotein (P-gp) inhibitor, verapamil, can be included to identify whether active transport is mediated by P-gp.
  caco-2 permeability assay
‘Studying the permeability of compounds across a Caco-2 cell monolayer is an established in vitro model to screen for oral absorption and to evaluate the mechanism of transport. Using LC-MS/MS for the analysis of samples derived from Caco-2 cell studies allows the rapid and accurate determination of drug transport across the Caco-2 cell monolayer.’
1Wang Z, Hop C.E., Leung K.H. and Pang J. (2000) J Mass Spectrom 35 (1); 71-6
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1 Wang Z et al. (2000) J Mass Spectrom. 35 (1); 71-6
2 Zhao YH et al. (2001) J Pharmaceut Sci 90; 749-784

3 Yazdanian M et al. (1998) Pharmaceut Res 15; 1490-1494
4 Kansy M et al. (2001) Pharmacokinetic optimisation in drug research Ed. Testa et al; 447-464

Caco-2 permeability

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