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

Cytochrome P450 2C9 (CYP2C9) Inhibitor Screening Kit (Fluorometric)is available at Gentaur for Next week Delivery.

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

Description:

Cytochrome P450 2C9 (CYP2C9, 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. 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.

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.

Sample Typ:e Samples containing drugs, inhibitors or ligands (compounds that can interact and affect CYP2C9 activity)

Alternate Name: CYP2C9 Inhibitor screening kit, CYP1A2 Ligand screening kit

Features and Benefits:

• Simple, highly sensitive, high-throughput compatible • Rapid screening of CYP2C9 inhibitors or ligands • Kit includes the CYP2C9 inhibitor Sulfaphenazole and a stable, recombinant human CYP2C9 co-expressed with NADPH Reductase