Cytochrome P450 2C19 (CYP2C19) Inhibitor Screening Kit (Fluorometric)

Cytochrome P450 2C19 (CYP2C19, 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. CYP2C19 is primarily expressed in liver and intestinal tissue and catalyzes oxidation of neutral or weakly basic lipophilic molecules with 2-3 hydrogen bond donor/acceptor sites. Isoforms of the CYP2C subfamily are responsible for metabolism of nearly 20% of all small molecule drugs commonly used by humans. Polymorphisms in the human CYP2C19 gene have been implicated in clinical drug/drug interactions involving widely-prescribed drugs, including proton pump inhibitors, antiplatelet agents and anticonvulsants. In addition, for drugs whose pharmacological activity requires metabolism from a pro-drug form (such as the antithrombotic drug clopidogrel), CYP2C19 inhibition or allelic deficiency can lead to decreased drug efficacy. BioVision’s CYP2C19 Inhibitor Screening Kit enables rapid screening of drugs and other new chemical entities (NCEs) for compound-CYP2C19 interaction in a reliable, high-throughput fluorescence-based assay. The kit provides a yeast microsomal preparation of human CYP2C19 and cytochrome P450 reductase (CPR) enzymes. The assay utilizes a non-fluorescent CYP2C19 substrate that is converted into a highly fluorescent metabolite detected in the visible range (Ex/Em = 406/468 nm), ensuring a high signal-to-background ratio with little interference by autofluorescence. The kit contains a complete set of reagents sufficient for performing 100 reactions in a 96-well plate format.

• Detection method : Fluorescence (Ex/Em 406/468 nm) • Species reactivity : Eukaryotes • Applications : • Rapid, high:throughput screening of drugs and novel ligands. • Development of structure:activity relationship (SAR) models to predict CYP2C19 inhibition liability of novel compounds. • Prediction of adverse drug:drug interaction potential and bioavailability for compounds metabolized by CYP2C19.

• Simple, highly sensitive, high-throughput compatible • Rapid screening of CYP2C19 inhibitors or ligands • Kit includes the CYP2C19 inhibitor Ticlopidine and a stable, recombinant human CYP2C19 co-expressed with NADPH Reductase

Cytochrome P450 2C19, CYP2C19, CYPII2c19, CYP2C, P450 2C, CYP2C19 inhibitor, CYP2C19 ligand, Cyt P450 2C19

CYP2C19 Inhibitor screening kit, CYP2C19 Ligand screening kit

• CYP2C19 Assay Buffer • 3-CHC Standard • CYP2C19 Inhibitor (Ticlopidine) • NADPH Generating System (100X) • β-NADP+ Stock (100X) • CYP2C19 Substrate • Recombinant Human CYP2C19

-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 CYP2C19 inhibition liability of novel compounds. • Prediction of adverse drug-drug interaction potential and bioavailability for compounds metabolized by CYP2C19.

Samples containing drugs, inhibitors or ligands (compounds that can interact and affect CYP2C19 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.