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Catalog #
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DMG-2C9-200
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Size
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200 Reactions
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Store At
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-20°C
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Human cytochrome P450 2C9 (CYP2C9) is a member
of the monooxygenase superfamily of enzymes involved in drug me-tabolism
and the synthesis of cholesterol, steroids, and other lipids. It
is the major member of the CYP2C subfamily and is expressed in the
liver. This subfamily comprises a cluster of four genes coding for
mephenytoin 4-hydroxylases which metabolize many endogenous compounds
and xenobiotics, and are responsible for the metabolism of
approximately 20% of all therapeutic drugs1. Among the various substrates
of CYP2C9 are compounds such as progesterone and arachidonic acid, and drugs such as the anticonvulsant phenytoin, the anti-inflammatory
ibuprofen and the anticoagulant S-warfarin. Some
chemicals can influence the activity of this enzyme. For example,
barbiturates will induce CYP2C9, while sertraline will inhibit2. The
CYP2C9 gene is genetically polymorphic among individuals and ethnic
groups. Genetic changes can influence enzymatic activity, and
the resultant phenotypic changes are characterized into poor, intermediate,
extensive, and ultrarapid metabolism3. Several single nucleotide
polymorphisms (SNPs) have been implicated in
overanticoagulation and bleeding4,
colorectal cancer5, and sudden
infant death syndrome6. The gene is located on chromosome 10q24
and spans approximately 50 kb with 13 exons.
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