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Microsomal stability assay

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

Microsomal stability is one of Cyprotex's 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 microsomes

  • The liver is the most important site of drug metabolism in the body. Approximately 60 % of marketed compounds are cleared by hepatic CYP-mediated metabolism1.
  • Liver microsomes are subcellular fractions which contain membrane bound drug metabolizing enzymes.
  • Microsomes can be used to determine the in vitro intrinsic clearance of a compound.
  • The use of species-specific microsomes can be used to enable an understanding of interspecies differences in drug metabolism.
  • Easy to prepare, use and store enabling cost efficiencies over whole cell models.
  • Microsomes are pooled from multiple donors to minimize the effect of interindividual variability.
  • Microsomes are fully characterized using probe substrates to ensure activity is maintained between batches.
  microsomal stability
‘The liver microsomal in vitro T1/2 approach can be a suitable approach to measure in vitro CLint, which can be scaled up to the in vivo situation and used in the prediction of human clearance.’
2Obach RS. (1999) Drug Metab Dispos 27 (11); 1350-1359.
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References

5 Davies B. and Morris T. (1993) Pharma Res 10 (7); 1093-1095.
6 Barter ZE et al. (2007) Curr Drug Metab 8 (1); 33-45.
7 Iwatsubo T et al. (1997) JPET 283 (2); 462-469

1 McGinnity DF et al. (2004) Drug Metab Dispos 32; 1247-1253.
2 Obach RS. (1999) Drug Metab Dispos 27 (11); 1350-1359.
3 Riley RJ et al. (2005) Drug Metab Dispos 33; 1304-1311.
4 Houston JB. (1994)Biochem Pharmacol 47 (9); 1469-1479.

 
microsomal stability

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