Carboxylesterase (CE) Reaction Phenotyping Assay

Understand if your compound is a substrate of carboxylesterases.

Carboxylesterase (CE) reaction phenotyping is a non-CYP mediated metabolism assay within our portfolio of in vitro ADME screening services. Cyprotex delivers consistent, high quality data with the flexibility to adapt protocols based on specific customer requirements.

• Human carboxylesterases (CE) are Phase I drug-metabolizing enzymes of the serine hydrolase superfamily. They hydrolyze a variety of ester containing drugs and prodrugs.
• hCE1 and hCE2 are the most extensively studied of the human CEs. They differ in their substrate specificity and tissue distribution. hCE1 is expressed in many organs especially in the liver, with low expression in the gastrointestinal tract. hCE2 protein is also expressed in many extrahepatic tissues, especially in the gastrointestinal tract and at lower levels in the liver.
• To improve oral bioavailability, ester prodrugs are often designed so they can be hydrolyzed by carboxylesterases either in the intestine or the liver with the intention of liberating the active drug.
• Cyprotex’s carboxylesterase reaction phenotyping assay identifies if your compound is a substrate for carboxylesterase enzymes.