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Hepatocyte stability assay

Understand the metabolism of your compounds by using our hepatocyte stability assay to measure in vitro intrinsic clearance or to identify metabolites formed.

The hepatocyte stability assay is one of our portfolio of in vitro ADME screening services. Cyprotex deliver consistent, high quality data with cost-efficiency that comes from a highly automated approach.

 

Measurement of in vitro intrinsic clearance using hepatocytes

  • The liver is the most important site of drug metabolism in the body. Approximately 60% of marketed compounds are cleared by hepatic CYP-mediated metabolism2.
  • Hepatocytes contain the full complement of hepatic drug metabolizing enzymes (both phase I and phase II) maintained within the intact cell.
  • Hepatocytes can be used to determine the in vitro intrinsic clearance of a compound.
  • The use of species-specific cryopreserved hepatocytes can be used to enable an understanding of interspecies differences.
  • Hepatocytes can be used to profile for metabolites formed by both phase I and phase II enzymes.
  hepatocyte stability
‘Human hepatocytes have become the "gold standard" for evaluating hepatic metabolism and toxicity of drugs and other xenobiotics in vitro.’
1LeCluyse EL and Alexandre E (2010) Methods Mol Biol 640; 57-82
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References

1 LeCluyse EL and Alexandre E (2010) Methods Mol Biol 640; 57-82
2 McGinnity DF et al. (2004) Drug Metab Dispos 32; 1247-1253.
3 Soars MG et al. (2002) J Pharmacol Exp Ther 301 (1); 382-90.
4 Shibata Y et al. (2002) Drug Metab Dispos 30 (8); 892-896.
5 Lau YY et al. (2002) Drug Metab Dispos 30 (12); 1446-1454.

6 McGinnity DF and Riley RJ (2004) Drug Metab Rev 36 (S1); 211.
7 Houston JB. (1994) Biochem Pharmacol 47 (9); 1469-1479.
8 Davies B. and Morris T. (1993), Pharma Res 10 (7); 1093-1095.
9 Barter ZE et al. (2007) Curr Drug Metab 8 (1); 33-45.
10 Sohlenius-Sternbeck AK (2006) Toxicol. In Vitro 20; 1582-1586.

 
hepatocyte stability

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on 14th April 2014
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