Cytochrome P450 2D6 (CYP2D6) Inhibitor Screening 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 resulting CYP2D6 activity ranging from complete metabolic deficiency to ultra-rapid metabolism depending upon allelic variation and gene copy number. 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 Inhibitor Screening Kit enables rapid screening of drugs and other new chemical entities (NCEs) for compound-CYP2D6 interaction in a reliable, high-throughput fluorescence-based assay. The kit provides a yeast microsomal preparation of human CYP2D6 and cytochrome P450 reductase (CPR) enzymes. 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. The kit contains a complete set of reagents sufficient for performing 200 reactions in a 96-well plate format.

• Detection method : Fluorescence (Ex/Em 390/468 nm) • Species reactivity : Eukaryotes • Applications : • Rapid, high:throughput screening of drugs and novel ligands. • Development of structure:activity relationship (SAR) models to predict CYP2D6 inhibition liability of novel compounds. • Prediction of adverse drug:drug interaction potential and bioavailability for compounds metabolized by CYP2D6.

• Simple, highly sensitive, high-throughput compatible • Rapid screening of CYP2D6 inhibitors or ligands • Kit includes the canonical CYP2D6 inhibitor Quinidine and a stable, recombinant human CYP2D6 co-expressed with NADPH Reductase

Cytochrome P450 2D6, CYP2D6, CYPII2D6, CYP2D, P450 2D, CYP2D6 inhibitor, CYP2D6 ligand

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, high-throughput screening of drugs and novel ligands. • Development of structure-activity relationship (SAR) models to predict CYP2D6 inhibition liability of novel compounds. • Prediction of adverse drug-drug interaction potential and bioavailability for compounds metabolized by CYP2D6.

Samples containing drugs, inhibitors or ligands (compounds that can interact and affect CYP2D activity)

Tissue, pathway, proteinase, peptidase, protease ,acrosin, lipoprotein, activator, caspase, trypsin, papain, esterase inhibitors are proteins or receptor ligands or receptor antagonists that bind to an enzyme receptor and decreases its activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. Not all receptor antagonist that bind to enzymes are inhibitors; enzyme activator ligands or agonists bind to enzymes and increase their enzymatic activity, while enzyme substrates bind and are converted to products in the normal catalytic cycle of the enzyme.