Cytochrome P450 2C19 (CYP2C19) Inhibitor Screening Kit (Fluorometric)
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Catalog numberK849-100
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PricePlease ask
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Size100 assays
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DescriptionHigh-throughput compatible, quick and easy screening for CYP2C19 inhibitors or ligands; Includes human CYP2C19 - NADPH Reductase.
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Summary• 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.
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Detection MethodFluorescence (Ex/Em 406/468 nm)
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Species ReactivityEukaryotes
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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.
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Sample TypeSamples containing drugs, inhibitors or ligands (compounds that can interact and affect CYP2C19 activity)
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Features Benefits• 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
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Storage Conditions-20°C
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Shipping Conditionsgel pack
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Shelf life12 months
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BackgroundCytochrome 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.
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Additional descriptionTissue, 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.
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Gene target
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Gene symbolCYP2C19, CYP3A7, CYP24A1, CYP1A1, CYP51A1, CYP2D6
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Short nameCytochrome P450 2C19 (CYP2C19) Inhibitor Screening Kit (Fluorometric)
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Alternative nameCytochrome P450 2C19 (CYP2C19) suppressor detection reagent (fluorescence)
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Alternative techniquekits
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Alternative to gene targetv-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog, C-Kit and CD117 and PBT and SCFR, KIT and IDBG-18980 and ENSG00000157404 and 3815, transferase activity, Extracellular, Kit and IDBG-172083 and ENSMUSG00000005672 and 16590, KIT and IDBG-642326 and ENSBTAG00000002699 and 280832
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Gene info
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Identity
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Gene
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Long gene namecytochrome P450 family 2 subfamily C member 19
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Synonyms gene
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Synonyms gene name
- cytochrome P450, subfamily IIC (mephenytoin 4-hydroxylase), polypeptide 19
- cytochrome P450, family 2, subfamily C, polypeptide 19
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Synonyms
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GenBank acession
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Locus
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Discovery year1992-04-06
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Entrez gene record
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Pubmed identfication
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RefSeq identity
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Classification
- Cytochrome P450 family 2
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VEGA ID
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Locus Specific Databases
Gene info
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Identity
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Gene
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Long gene namecytochrome P450 family 3 subfamily A member 7
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Synonyms gene name
- cytochrome P450, subfamily IIIA, polypeptide 7
- cytochrome P450, family 3, subfamily A, polypeptide 7
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Synonyms
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GenBank acession
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Locus
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Discovery year1992-09-14
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Entrez gene record
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Pubmed identfication
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Classification
- Cytochrome P450 family 3
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VEGA ID
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Locus Specific Databases
Gene info
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Identity
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Gene
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Long gene namecytochrome P450 family 24 subfamily A member 1
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Synonyms gene
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Synonyms gene name
- cytochrome P450, subfamily XXIV (vitamin D 24-hydroxylase)
- cytochrome P450, family 24, subfamily A, polypeptide 1
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Synonyms
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GenBank acession
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Locus
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Discovery year1992-09-09
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Entrez gene record
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Classification
- Cytochrome P450 family 24
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VEGA ID
Gene info
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Identity
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Gene
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Long gene namecytochrome P450 family 1 subfamily A member 1
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Synonyms gene
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Synonyms gene name
- cytochrome P450, subfamily I (aromatic compound-inducible), polypeptide 1
- cytochrome P450, family 1, subfamily A, polypeptide 1
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Synonyms
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GenBank acession
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Locus
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Discovery year1986-01-01
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Entrez gene record
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Pubmed identfication
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RefSeq identity
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Classification
- Cytochrome P450 family 1
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VEGA ID
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Locus Specific Databases
Gene info
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Identity
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Gene
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Long gene namecytochrome P450 family 51 subfamily A member 1
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Synonyms gene
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Synonyms gene name
- cytochrome P450, 51 (lanosterol 14-alpha-demethylase)
- cytochrome P450, family 51, subfamily A, polypeptide 1
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Synonyms
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GenBank acession
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Locus
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Discovery year1996-10-26
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Entrez gene record
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Pubmed identfication
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Classification
- Cytochrome P450 family 51
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VEGA ID
Gene info
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Identity
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Gene
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Long gene namecytochrome P450 family 2 subfamily D member 6
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Synonyms gene
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Synonyms gene name
- cytochrome P450, subfamily IID (debrisoquine, sparteine, etc., -metabolizing), polypeptide 6
- cytochrome P450, family 2, subfamily D, polypeptide 7 pseudogene 2
- cytochrome P450, subfamily II (debrisoquine, sparteine, etc., -metabolising), polypeptide 7 pseudogene 2
- cytochrome P450, family 2, subfamily D, polypeptide 8 pseudogene 2
- cytochrome P450, subfamily IID (debrisoquine, sparteine, etc., -metabolising), polypeptide 8 pseudogene 2
- cytochrome P450, family 2, subfamily D, polypeptide 6
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Synonyms
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GenBank acession
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Locus
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Discovery year1992-04-07
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Entrez gene record
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Pubmed identfication
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Classification
- Cytochrome P450 family 2
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VEGA ID
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Locus Specific Databases
