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Corning® Supersomes? Human Carboxylesterase Portfolio

Corning® Supersomes? Human Carboxylesterase Portfolio
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Corning® Supersomes? Human Carboxylesterase Portfolio - 1

Corning® Supersomes™ Human Carboxylesterase Portfolio Human Recombinant Drug Metabolizing Enzymes Human carboxylesterase 1 (hCES1) and carboxylesterase 2 (hCES2) are members of the serine esterase superfamily, exhibiting broad substrate specificity, and involved in xenobiotic and endobiotic metabolism. Human CES1 and CES2 are primarily expressed in the liver and small intestine. Human CES1 is expressed as two major isoforms; hCES1b and hCES1c. Corning Supersomes CES portfolio of human recombinant metabolizing enzymes match the published sequence from the U.S. National Library of Medicine native DNA sequence and provide high levels of enzymatic activity for efficient metabolite production. Features w Facilitates efficient metabolite formation with long linear time course; ideal for slow metabolizing drug compounds. w Ensures hydrolase activity of recombinant enzymes is functionally similar to hCES1 and hCES2 expressed in human liver and small intestine microsomes, respectively. w Delivers high catalytic activity, ideal for robust high-throughput screening assays including drug-drug interaction studies. w Supports essential assays such as reaction phenotyping and enzyme inhibition required for FDA new drug registration and other pharmacokinetic studies appropriate for evaluating pro-drugs and non-CYP pathways of elimination. w Manufactured using baculovirus transfected insect cell expression High enzymatic activity The Corning Supersomes product line is engineered to provide efficient metabolite production with long linear metabolite formation with typical times of >30 minutes, making the products highly suited to identifying metabolites for slowly metabolized compounds. Engineered for native activity Corning’s CES1b, CES1c, and CES2 behave like native carboxylesterases expressed in human liver and intestine as demonstrated by measured hydrolase activity where the Vmax and Km of recombinant hCES1b and hCES2 are similar to those of human liver and small intestine microsomes (shown in Figure 1). Extensive portfolio of Phase 1 and Phase 2 recombinant enzymes Corning Supersomes are recognized worldwide as the “industry gold standard”, with the most extensive portfolio of CYPs, UGTs, FMOs, MAOs, NATs, and now CESs.

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Corning® Supersomes? Human Carboxylesterase Portfolio - 2

Michaelis-Menten Kinetic Parameters 4-NPA (Substrate) Vmax (nmol/mg/min) 836 North St. Building 300, Suite 3401 Tewksbury, MA 01876 t 800.492.1110 t 978.442.2200 f 978.442.2476 www.corning.com/lifesciences HLM: Human Liver Microsomes HIM: Human Intestinal Microsomes Table 1. Michaelis-Menten kinetic parameters of CES1b, CES1c compared to HLM, and CES2 compared to HIM. CES1b and CES2 measured Km values were found to be similar to Km values obtained using human tissue. When 4-Nitrophenyl Acetate (4-NPA) was used as a substrate the measured Km values for CES1b and HLM were approximately 200...

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