E0412
Carboxylesterase 2 human
recombinant, expressed in baculovirus infected BTI insect cells
Sinonimo/i:
Carboxylesterase 2 human, CES2, CES2A1
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CHF 469.00
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Prodotti consigliati
Ricombinante
expressed in baculovirus infected BTI insect cells
Livello qualitativo
Stato
liquid
Attività specifica
≥500 units/mg protein
PM
60 kDa
Peso
(0.5 ml)
Condizioni di spedizione
dry ice
Temperatura di conservazione
−70°C
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Descrizione generale
Carboxylesterase 2 human gene is mapped to human chromosome 16q22.1.[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.[2][3] It has two glycosylation sites at 103 and 267 residues with molecular mass 60kDa.[4]
Applicazioni
Carboxylesterase 2 human has been used:
- in the in vitro enzyme-based inhibitor screening assay[5]
- in substrate selectivity assay with emission ratiometric two-photon probe (SE1)[6]
- as a reference standard in the enzyme assay with various 4-nitrophenyl and 1-naphthyl based substrates[7]
Carboxylesterase 2 may play a key role in biotransformation of a variety of ester containing drugs and prodrugs.[3]
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.
Azioni biochim/fisiol
Carboxylesterase 2 human identifies the site containing a large alcohol and small acyl group.[8] It shows less transesterification activity due to presence of conformational interference in active site.[3]
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.
Definizione di unità
One unit will produce 1 nanomole of 4-nitrophenol from 4-nitrophenyl acetate per minute at pH 7.4 at 37 deg C.
Codice della classe di stoccaggio
10 - Combustible liquids
Classe di pericolosità dell'acqua (WGK)
nwg
Punto d’infiammabilità (°F)
Not applicable
Punto d’infiammabilità (°C)
Not applicable
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T Satoh et al.
Annual review of pharmacology and toxicology, 38, 257-288 (1998-05-23)
Multiple carboxylesterases (EC 3.1.1.1) play an important role in the hydrolytic biotransformation of a vast number of structurally diverse drugs. These enzymes are major determinants of the pharmacokinetic behavior of most therapeutic agents containing ester or amide bonds. Carboxylesterase activity
S Omedes et al.
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Tetsuo Satoh et al.
Drug metabolism and disposition: the biological fate of chemicals, 30(5), 488-493 (2002-04-16)
This article reports on a symposium sponsored by the American Society for Pharmacology and Experimental Therapeutics and held at the April 2001 Experimental Biology meeting. Current developments in molecular-based studies into the structure and function of cholinesterases, carboxylesterases, and paraoxonases
Human liver carboxylesterase. Purification and molecular properties.
W Junge et al.
Archives of biochemistry and biophysics, 165(2), 749-763 (1974-12-01)
Sang Jun Park et al.
Chemical science, 7(6), 3703-3709 (2016-06-01)
Carboxylesterases (CEs) are widely distributed enzymes in the human body that catalyze hydrolysis of various endogenous and exogenous substrates. They are directly linked to hepatic drug metabolisms and steatosis, and their regulations are important issues in pharmacological and clinical applications.
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