Cytochrome P450 2C9 (CYP2C9) Inhibitor Screening Kit (Fluorometric) (ab284519)
Key features and details
- Assay type: Enzyme activity
- Detection method: Fluorescent
- Platform: Microplate (12 x 8 well strips)
- Sample type: Inhibitor compounds
Overview
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Product name
Cytochrome P450 2C9 (CYP2C9) Inhibitor Screening Kit (Fluorometric)
See all CYP2C9 kits -
Detection method
Fluorescent -
Sample type
Inhibitor compounds -
Assay type
Enzyme activity -
Assay duration
Multiple steps standard assay -
Product overview
The CYP2C9 Inhibitor Screening Kit (ab284519) (K896) 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.
General range = 0-20 pmol/well.
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Notes
This product is manufactured by BioVision, an Abcam company and was previously called K896 Cytochrome P450 2C9 (CYP2C9) Inhibitor Screening Kit (Fluorometric). K896-100 is the same size as the 100 test size of ab284519.
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Platform
Microplate (12 x 8 well strips)
Properties
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Storage instructions
Store at -20°C. Please refer to protocols. -
Components 100 tests 7-HFC Standard 1 vial beta-NADP+ Stock (100X) 1 vial CYP2C9 Assay Buffer 1 x 100ml CYP2C9 Inhibitor (Sulfaphenazole) 1 vial CYP2C9 Substrate 1 vial NADPH Generating System (100X) 1 vial Recombinant Human CYP2C9 2 vials -
Research areas
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Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenytoin, tolbutamide and losartan. -
Sequence similarities
Belongs to the cytochrome P450 family. -
Cellular localization
Endoplasmic reticulum membrane. Microsome membrane. - Information by UniProt
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Alternative names
- (R)-limonene 6-monooxygenase
- (S)-limonene 6-monooxygenase
- (S)-limonene 7-monooxygenase
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Images
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Relative fluorescence units and 7-HFC (7-hydroxy-4-(trifluoromethyl)coumarin) standard curve. One mole of 7-HFC corresponds to the metabolism of one mole of CYP2C9 substrate.
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Recombinant human CYP2C9 enzyme and its reaction kinetics at 37°C in the presence and absence of the indicated CYP2C9 inhibitors. The solvent control reaction contained assay buffer with 0.3% acetonitrile.
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Dose-response curves for various CYP2C9 ligands of differing structural and mechanistic classes. The results from canonical competitive CYP2C9 inhibitor sulfaphenazole, the mechanism-based irreversible inhibitor tienilic acid, the antidepressant fluvoxamine (a competitive inhibitor of several CYP isoforms) and the CYP2C9-selective substrate diclofenac are presented in the graph. For dose-response curves, percent activity was calculated for each concentration of inhibitor by comparison to activity of reactions containing no inhibitor. For each CYP2C9 inhibitor, IC50 values were derived by 4- parameter logistic curve fitting with each point representing the mean ± SEM of at least three replicates. Assays were performed according to the kit protocol.
Datasheets and documents
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SDS download
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Datasheet download
References (0)
ab284519 has not yet been referenced specifically in any publications.