CYP450 BASED ASSAYS
Over the years, various liver-derived in vitro model systems have been developed to enable investigation of the potential adverse effects of chemicals and drugs. The gold standard toxicological approach for evaluating chemical toxicity involves complex in vivo studies which are both time consuming and costly.
Due to concerns about animal welfare, time and cost constraints, and the ever increasing number of chemicals that need testing, establishing workable in vitro culture systems has become a priority for the toxicology community.
Of the various families that are present in human beings the most interesting in this respect are the 1, 2 and 3, and the most important enzymes are CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4. The majority of the enzymes are also involved in the metabolism of endogenous substances, such as steroids or sex hormones, which is also important should there be interference with these substances.
Hepatocytes are nowadays the current gold standard in the study of toxicity, although different in vitro approaches using cell lines or microsomes are available. Using ReadyCell tools, toxicity could not only be addressed but dissected, identifying particular isoforms responsible for bioactivation.
Human hepatocytes in Ready-to-Use Format
Cultured human hepatocytes are considered up to date the gold standard model to anticipate in vivo metabolic pathways of drugs and new chemical entities. They represent an accepted in vitro model by the FDA for ADME-Tox studies.
- Fresh plated hepatocyte monolayer (24-well plates) subjected to availability.
- Cryopreserved hepatocyte (either frozen or pre-plated) under development.
HepatoReady kits contain 24-well plates with high-viability and metabolically-active human hepatocytes. The innovative shipping medium, developed and patented by ReadyCell, preserves the properties of the plated hepatocytes throughout transportation.
A novel cell based and ready-to-use concept
for in vitro evaluation of biotransformation-mediated metabolic toxicity
IsoCyp-Tox is an innovative cell-based and ready-to-use kit. The kit consists of 96-well plates seeded with the hepatic cell line HepG2 transiently transduced with individual human CYP450 isoforms, making these cells metabolically competent.
IsoCyp-Tox allows in vitro detection and screening of biotransformation-mediated toxicity of lead and drug targets in just one single experiment.
IsoCyp-Tox is powerful as well as time and cost-saving tool during hit to lead and lead optimization phases in early stage of drug discovery and development.