Cytochrome P450 2D6 (CYP2D6) Activity Assay Kit (Fluorometric)

Cytochrome P450 2D6 (CYP2D6, EC 1.14.14.1) 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. CYP2D6 catalyzes oxidation of lipophilic bases with an aromatic ring and a nitrogen atom and is highly expressed in liver and brain tissue. The enzyme is responsible for metabolism of nearly 25% of all small molecule drugs commonly used by humans, particularly psychiatric drugs such as antidepressants, antipsychotics and stimulants. The CYP2D6 gene is highly polymorphic in the human population, with CYP2D6 activity ranging from complete metabolic deficiency to ultra-rapid metabolism. Due to this wide phenotypic variability, CYP2D6 is frequently implicated in drug toxicity and clinical drug/drug interactions. In addition, for drugs whose pharmacological activity requires metabolism from a pro-drug form, CYP2D6 inhibition or allelic deficiency can lead to decreased drug efficacy. BioVision’s CYP2D6 Activity Assay Kit enables rapid measurement of native or recombinant CYP2D6 activity in biological samples such as liver microsomes. The assay utilizes a non-fluorescent CYP2D6-selective substrate that is converted into a highly fluorescent metabolite detected in the visible range (Ex/Em = 390/468 nm), ensuring a high signal-to-background ratio with little interference by autofluorescence. CYP2D6 specific activity is calculated by running parallel reactions in the presence and absence of the potent CYP2D6-selective inhibitor quinidine and subtracting any residual activity detected with the inhibitor present. The kit contains a complete set of reagents sufficient for performing 100 sets of paired reactions (in the presence and absence of inhibitor).

• Detection method : Fluorescence (Ex/Em 390/468 nm) • Species reactivity : Eukaryotes • Applications : • Rapid assessment of native/recombinant CYP2D6 activity in lysates or microsomal fractions prepared from tissues, cells. • Screening of drugs and novel ligands for interaction with native/recombinant CYP2D6.

• Simple, convenient, highly sensitive • Fluorescent assay enables easy determination of CYP2D6 activity in a variety of biological samples • The substrate shows low background and a high signal-to-noise ratio • Kit includes CYP2D6 inhibitor Quinidine and a stable, recombinant human CYP2D6 co-expressed with NADPH Reductase as a positive control

Cytochrome P450 2D6, CYP2D6, CYPII2D6, CYP2D, P450 2D, Drug metabolism Assay

none

• CYP2D6 Assay Buffer • AHMC Standard • CYP2D6 Inhibitor (Quinidine) • NADPH Generating System (100X) • β-NADP+ Stock (100X) • CYP2D6 Substrate • Recombinant Human CYP2D6

-20°C

gel pack

12 months

Eukaryotes

• Rapid assessment of native/recombinant CYP2D6 activity in lysates or microsomal fractions prepared from tissues or cells. • Screening of drugs and novel ligands for interaction with native/recombinant CYP2D6.

• Human liver microsomes and liver S9 fractions • Lysates of tissues and cultured cells, primary hepatocytes • Heterologously expressed recombinant CYP2D6 preparations

Biovision supplies other types of Assays as 1.