Merck, E0412-1VL, Carboxylesterase 2 human

General description
Carboxylesterase 2 human gene is mapped to human chromosome 16q22.1.
Carboxylesterase belongs to the α/β hydrolase fold family and is involved in drug metabolism and activation. It is present in colon, liver, small intestine, heart, brain and testis. The hydrolase activity of small intestine is attributed to carboxylesterase 2 human. It has two glycosylation sites at 103 and 267 residues with molecular mass 60kDa.
Application
Carboxylesterase 2 human has been used:
in the in vitro enzyme-based inhibitor screening assay
in substrate selectivity assay with emission ratiometric two-photon probe (SE1)
as a reference standard in the enzyme assay with various 4-nitrophenyl and 1-naphthyl based substrates

Carboxylesterase 2 may play a key role in biotransformation of a variety of ester containing drugs and prodrugs.
Delivers high catalytic activity, ideal for robust high-throughput screening assays including drug-drug interaction studies, and pharmacokinetic studies for evaluating pro-drugs and non-CYP pathways of elimination.
Biochem/physiol Actions
Carboxylesterase 2 human identifies the site containing a large alcohol and small acyl group. It shows less transesterification activity due to presence of conformational interference in active site.
Member of a serine esterase family that hydrolyze ester and amide bonds. Carboxylesterase 2 is an endoplasmic reticulum-bound hydrolase that plays a critical role in xenobiotic detoxification and activation for ester-containing therapeutics. Carboxylesterase 2 is also involved in the detoxification of drugs such as heroin and cocaine. This enzyme is thought to play a role in lipid metabolism.
Other Notes
One unit will produce 1 nanomole of 4-nitrophenol from 4-nitrophenyl acetate per minute at pH 7.4 at 37 deg C.