Cytochrome P450 1A2 (CYP1A2) Inhibitor Screening Kit (Fluorometric)

Cytochrome P450 1A2 (CYP1A2) Inhibitor Screening Kit (Fluorometric)is available at Gentaur for Next week Delivery.

High-throughput compatible, quick and easy screening for CYP1A2 inhibitors or ligands; Includes human CYP1A2 - NADPH Reductase..

Description:

Cytochrome P450 1A2 (CYP1A2, 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. CYP1A2 is primarily expressed in liver, intestinal and olfactory mucosal tissue and catalyzes oxidation of planar polyaromatic and heterocyclic molecules such as aromatic amines. CYP1A2 is responsible for metabolism of approximately 10% of all small molecule drugs commonly used by humans. Polymorphisms in the human CYP1A2 gene have been implicated in clinical drug/drug interactions involving widely-used drugs, including methylxanthines (caffeine and theophylline), ciprofloxacin and a number of antidepressants and antipsychotics. Isoforms of the CYP1A subfamily are also involved in metabolic activation of environmental pro-carcinogens in cigarette smoke and combustion exhaust fumes. BioVision’s CYP1A2 Inhibitor Screening Kit enables rapid screening of drugs and other new chemical entities (NCEs) for compound-CYP1A2 interaction in a reliable, high-throughput fluorescence-based assay. The kit provides a yeast microsomal preparation of human CYP1A2 and human cytochrome P450 reductase (CPR) enzymes. The assay utilizes a non-fluorescent CYP1A2 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.

Applications: • Rapid, high-throughput screening of drugs and novel ligands. • Development of structure-activity relationship (SAR) models to predict CYP1A2 inhibition liability of novel compounds. • Prediction of adverse drug-drug interaction potential and bioavailability for compounds metabolized by CYP1A2.

Sample Typ:e Samples containing drugs, inhibitors or ligands (compounds that can interact and affect CYP1A2 activity)

Alternate Name: CYP1A2 Inhibitor screening kit, CYP1A2 Ligand screening kit

Features and Benefits:

• Simple, highly sensitive, high-throughput compatible • Rapid screening of CYP1A2 inhibitors or ligands • Kit includes the CYP1A2 inhibitor α-naphthoflavone and a stable, recombinant human CYP1A2 co-expressed with NADPH Reductase