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Cytochrome P450 2C9 (CYP2C9) Inhibitor Screening Kit (Fluorometric)

High-throughput compatible, quick and easy screening for CYP2C9 inhibitors or ligands; Includes human CYP2C9 - NADPH Reductase.
Catalog #: K896

Product Details

Cat # +Size K896-100
Size 100 assays
Detection Method Fluorescence (Ex/Em 415/502 nm)
Species Reactivity Eukaryotes
Applications • Rapid, high-throughput screening of drugs and novel ligands.
• Development of structure-activity relationship (SAR) models to predict CYP2C9 inhibition liability of novel compounds.
• Prediction of adverse drug-drug interaction potential and bioavailability for compounds metabolized by CYP2C9.
Features & Benefits • Simple, convenient, highly sensitive
• Fluorescent assay enables easy determination of CYP1A2 activity in a variety of biological samples
• The substrate shows low background and a high signal-to-noise ratio
• Kit includes CYP1A2 inhibitor (α-naphthoflavone) and a stable, recombinant human CYP1A2 co-expressed with NADPH Reductase as a positive control
Kit Components • CYP2C9 Assay Buffer
• 7-HFC Standard
• CYP2C9 Inhibitor (Tienilic Acid)
• NADPH Generating System (100X)
• β-NADP+ Stock (100X)
• CYP2C9 Substrate
• Recombinant Human CYP2C9
Storage Conditions -20°C
Shipping Conditions Gel Pack
USAGE For Research Use Only! Not For Use in Humans.


Cytochrome P450 2C9 (CYP2C9, EC is a member of the cytochrome P450 monooxidase (CYP) family of microsomal xenobiotic metabolism enzymes. CYPs are membrane-bound hemeproteins responsible for Phase I biotransformation reactions, in which lipophilic drugs and other xenobiotic compounds are converted to more hydrophilic products to facilitate excretion from the body. CYP2C9 is primarily expressed in liver and catalyzes oxidation of small, weakly acidic or hydrophobic molecules containing an aromatic moiety and at least one hydrogen bond donor. Isoforms of the CYP2C subfamily are responsible for metabolism of nearly 20% of all small molecule drugs commonly used by humans. The human CYP2C9 gene is highly polymorphic and CYP2C9 single nucleotide polymorphisms (SNPs) have been implicated in clinical drug/drug interactions involving widely-prescribed drugs with narrow therapeutic indices such as warfarin, phenytoin and indomethacin. In addition, for drugs whose pharmacological activity requires metabolism from a pro-drug form (such as the antihypertensive drug losartan), CYP2C9 inhibition or allelic deficiency can lead to decreased drug efficacy. BioVision’s CYP2C9 Inhibitor Screening Kit enables rapid screening of drugs and other new chemical entities (NCEs) for compound-CYP2C9 interaction in a reliable, high-throughput fluorescence-based assay. The kit provides a yeast microsomal preparation of human CYP2C9 and human cytochrome P450 reductase (CPR) enzymes. The assay utilizes a non-fluorescent CYP2C9 substrate that is converted into a highly fluorescent metabolite detected in the visible range (Ex/Em = 415/502 nm), ensuring a high signal-to-background ratio with little interference by autofluorescence. The kit contains a complete set of reagents sufficient for performing 100 reactions in a 96-well plate format.

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