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MTOXCE1A2

Sigma-Aldrich

CypExpress 1A2 Cytochrome P450 human

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Synonym(s):
CP12, CYP1A2, P3-450, P450 1A2, P450(PA)
EC Number:
NACRES:
NA.77

biological source

human

recombinant

expressed in Pichia pastoris

form

dry powder

UniProt accession no.

application(s)

cell analysis

shipped in

dry ice

storage temp.

−70°C

Gene Information

human ... CYP1A2(1544)

Biochem/physiol Actions

Cytochrome P450 enzymes are heme containing monooxygenases which are found primarily in the mammalian liver. They catalyze the oxidative metabolism of xenobiotics. This metabolism is the initial step in the biotransformation and elimination of a wide variety of drugs and environmental pollutants from the body. Furafylline and α-naphthoflavone are inhibitors, whereas omeprazole and lansoprazole are inducers of the enzyme. The isozyme CYP1A2 is a major pathway for the in vivo conversion of phenacetin into acetaminophen via O-deethylation. This isozyme also catalyzes the 5-hydroxylation of thiabendazole.
Cytochrome P450 is a heterogeneous family of isozymes whose primary function is to oxidize small molecules, both as a function of intermediary metabolism (e.g., fatty acids) and to detoxify exogenous compounds (drugs or toxins). Some isoforms have narrow substrate specificity, while others are promiscuous.

Features and Benefits

CypExpress 1A2 is a permeabilized and stabilized dried yeast powder preparation containing full length, unmodified, human CYP 1A2 and recombinant human NADPH oxidoreductase. Using proprietary processes, CypExpress are expressed in Pichia yeast. Following optimal expression, the cells are inactivated, permeabilized and dried to a fine powder. CypExpress retains the cellular mechanisms to provide the P450 enzymes with the energy and cofactors to continue to function for long experiments, and can generate larger amounts of metabolite than mammalian microsomes or other genetically engineered expression systems. It is designed for rapid screening of drug metabolites and for scaling up metabolite generation.

Unit Definition

A reaction mixture containing 500 μM phenacetin and 100 mg/mL of CypExpress 1A2 will produce 35 μM acetaminophen in 4 hours at 30°C under the conditions described.

Physical form

Light yellow, very fine powder

Reconstitution

Per Protocol/Variable

Legal Information

6538 is a trademark of American Type Culture Collection
CypExpress is a trademark of Oxford Biomedical Research

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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R.Scott ObachA.S.Kalgutkar
Comprehensive Toxicology (2010)
Furafylline is a potent and selective inhibitor of cytochrome P450IA2 in man.
D Sesardic
British Journal of Clinical Pharmacology (1990)
Chapter 4 - Oxidant Stress, Antioxidant Defense, and Liver Injury
Mitchell R.McGill and HartmutJaeschke
Drug-Induced Liver Disease (2013)
Cytochrome P450 enzymes in drug metabolism and chemical toxicology: An introduction
Laura Lowe Furge and F. Peter Guengerich
Current Protocols in Cell Biology (2006)

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