CES1 Human
Sf9, Baculovirus cells.
Liver carboxylesterase 1 isoform a, CES1, ACAT, CE-1, CEH, CES2, hCE-1, HMSE, HMSE1, PCE-1, REH, SES1, TGH, Acyl-coenzyme A:cholesterol acyltransferase, Brain carboxylesterase hBr1.
Greater than 90.0% as determined by SDS-PAGE.
Description
CES1 Human produced in Sf9 Insect cells is a single, glycosylated polypeptide chain containing 559 amino acids (19-568 a.a.) and having a molecular mass of 61.7kDa (Molecular size on SDS-PAGE will appear at approximately 50-70kDa).
CES1 is expressed with a 9 amino acid His tag at C-Terminus and purified by proprietary chromatographic techniques.
Product Specs
Liver carboxylesterase 1 isoform a, CES1, ACAT, CE-1, CEH, CES2, hCE-1, HMSE, HMSE1, PCE-1, REH, SES1, TGH, Acyl-coenzyme A:cholesterol acyltransferase, Brain carboxylesterase hBr1.
Sf9, Baculovirus cells.
ADLGHPSSPP VVDTVHGKVL GKFVSLEGFA QPVAIFLGIP FAKPPLGPLR FTPPQPAEPW
SFVKNATSYP PMCTQDPKAG QLLSELFTNR KENIPLKLSE DCLYLNIYTP ADLTKKNRLP
VMVWIHGGGL MVGAASTYDG LALAAHENVV VVTIQYRLGI WGFFSTGDEH SRGNWGHLDQ
VAALRWVQDN IASFGGNPGS VTIFGESAGG ESVSVLVLSP LAKNLFHRAI SESGVALTSV
LVKKGDVKPL AEQIAITAGC KTTTSAVMVH CLRQKTEEEL LETTLKMKFL SLDLQGDPRE
SQPLLGTVID GMLLLKTPEE LQAERNFHTV PYMVGINKQE FGWLIPMQLM SYPLSEGQLD
QKTAMSLLWK SYPLVCIAKE LIPEATEKYL GGTDDTVKKK DLFLDLIADV MFGVPSVIVA
RNHRDAGAPT YMYEFQYRPS FSSDMKPKTV IGDHGDELFS VFGAPFLKEG ASEEEIRLSK
MVMKFWANFA RNGNPNGEGL PHWPEYNQKE GYLQIGANTQ AAQKLKDKEV AFWTNLFAKK AVEKPPQTEH IELHHHHHH.
Product Science Overview
Carboxylesterase 1 is a serine esterase and part of the alpha/beta fold hydrolase family . It is encoded by the CES1 gene located on chromosome 16q22.2 in humans . The enzyme is primarily found in the liver, where it constitutes approximately 1% of the entire liver proteome . CES1 is responsible for 80%–95% of total hydrolytic activity in the liver .
CES1 plays a crucial role in the metabolism of a wide range of drugs, including ester-prodrugs, pesticides, environmental pollutants, and endogenous compounds . It is particularly important in the hydrolysis of ester- and amide-bond-containing drugs such as cocaine and heroin . The enzyme’s activity can lead to the biotransformation of pharmacologically active drugs into their inactive metabolites, as exemplified by the hydrolysis of methylphenidate in the liver .
The expression and activity of CES1 vary significantly among individuals, contributing to interindividual variability in the pharmacokinetics and pharmacodynamics of drugs metabolized by CES1 . Both genetic and nongenetic factors influence CES1 functionality. Genetic polymorphisms, including single-nucleotide polymorphisms (SNPs) and copy number variants, as well as nongenetic factors such as developmental status, gender, and drug-drug interactions, can affect CES1 expression and activity .
Recombinant human Carboxylesterase 1 is produced using a mouse myeloma cell line, NS0-derived human CES1 protein . The recombinant protein is typically supplied as a filtered solution in sodium acetate and sodium chloride . It is used in various research applications, including the study of drug metabolism and the development of precision pharmacotherapy strategies .
The clinical relevance of CES1 has been demonstrated in various clinical trials. Predicting hepatic CES1 function can provide clinical guidance to optimize the pharmacotherapy of numerous medications metabolized by CES1 . Understanding the regulation of CES1 expression and activity, as well as identifying biomarkers for CES1 function in vivo, could lead to the development of precision pharmacotherapy strategies to improve the efficacy and safety of many CES1 substrate drugs .
