Understand if your compound is an inhibitor of carboxylesterases.
Carboxylesterase (CE) inhibition is a non-CYP mediated metabolism assay within our portfolio of in vitro ADME screening services. Cyprotex deliver consistent, high quality data with the flexibility to adapt protocols based on specific customer requirements.
CE inhibitors potentially have dual roles in modulating drug action, by both reducing induced toxicity and/or increasing molecule half-life.
1Hatfield M.J. and Potter P.M. (2011) Expert Opin Ther Patents 21(8); 1159-1171
|Test System||hCE1-b, hCE1-c, hCE2 expressed enzymes|
|Test Article Concentrations||0, 0.4, 1, 4, 10, 40 and 100 µM (different concentrations available)|
|Positive Control Inhibitors||Benzil (hCE1)
|Test Article Requirements||100 µL of a 40 mM DMSO solution (or equivalent amount in solid)|
Standard error of IC50
% Control at each concentration
The experimental design in Figure 1 can be used to identify specificity of hCE inhibitors. For example, it can be shown that rivastigmine demonstrates greater potency (>500 times) for hCE2 than hCE1 isoform.
1Hatfield M.J. and Potter P.M. (2011), Expert Opin Ther Patents 21(8); 1159-1171