Plasma Protein & Covalent Binding


Sekisui XenoTech offers covalent binding studies as part of our comprehensive portfolio of drug metabolism services. As a screening tool for the idiosyncratic potential of drug candidates, chemical reactivity of the compound and its metabolites is often evaluated by quantifying covalent binding properties. We offer covalent binding studies to evaluate the binding characteristics of a compound using human and non-human hepatic proteins.

In a typical study, the amount of labeled compound and its metabolite(s) that covalently bind to protein is determined through an in vitro test system using human liver microsomes. Rats are then subjected to the induction of liver metabolic enzymes followed by administration of the labeled compound, with the liver being removed at a specific time point. Radioactivity in the plasma and liver is measured to obtain the amount of labeled compound and its metabolites that covalently bind to protein in these biological samples in vitro.

Discovery Plus™ Protein Binding Service
Sekisui XenoTech's medium-throughput Discovery Plus™ screening service uses Rapid Equilibrium Dialysis to measure fraction unbound (fu), non-specific binding (% recovery) and the plasma stability (% remaining) of your compound. Sekisui XenoTech's study design evaluates up to 15 compounds (plus a positive control) at a single concentration dialyzed against buffer at 37°C for four hours, with plasma from up to six different species and relative quantitation analysis by LC-MS/MS.

For more information on our Discovery Plus™ Protein Binding service, click here.
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