Key features and details
- Assay type: Quantitative
- Detection method: Fluorescent
- Platform: Microplate reader
- Sample type: Inhibitor compounds
Product nameCYP2C19 Inhibitor Assay Kit (Fluorometric)
See all CYP2C19 kits
Sample typeInhibitor compounds
CYP2C19 Inhibitor Screening Kit (Fluorometric) (ab211073) allows rapid screening of drugs and other new chemical entities (NCEs) for CYP2C19-compound interaction in a reliable, high-throughput fluorescence-based assay. The assay is based on the conversion of a non-fluorescent CYP2C19 substrate into a highly fluorescent metabolite, which can be detected in the visible range (Ex/Em = 406/468 nm), ensuring a high signal-to-background ratio with little interference by autofluorescence.
This assay can be used in the development of structure-activity relationship (SAR) models to predict CYP2C19 inhibition liability of novel compounds and analogues, as well as in the prediction of adverse drug-drug interaction potential and bioavailability for compounds metabolized by CYP2C19.
The kit contains a yeast microsomal preparation of human CYP2C19 and cytochrome P450 reductase (CPR) enzymes.
Cytochrome P4502C19 (CYP2C19, EC 184.108.40.206) is a member of the cytochrome 450 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 for 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. Polymorphisms in the human CYP2C19 gene have been implicated in clinical drug/drug interactions involving wide-prescribed drugs such as anticonvulsants or antiplatelet agents.
Storage instructionsStore at -20°C. Please refer to protocols.
Components 100 tests β-NADP+ Stock 100X (2 mg) 1 vial 3-CHC Standard (2 mg) 1 vial CYP2C19 Assay Buffer 1 x 100ml CYP2C19 Inhibitor (Ticlopidine) (2 mg) 1 vial CYP2C19 Substrate (2 mg) 1 vial NADPH Generating System 100X (5 mg) 1 vial Recombinant Human CYP2C19 (2 x 5 mg) 2 vials
RelevanceResponsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Cellular localizationEndoplasmic reticulum membrane; Peripheral membrane protein. Microsome membrane; Peripheral membrane protein.
- (R)-limonene 6-monooxygenase
- (S)-limonene 6-monooxygenase
- (S)-limonene 7-monooxygenase
Typical 3-CHC standard calibration curve. One mol of 3-CHC corresponds to the metabolism of one mol of CYP2C19 substrate.
Reaction kinetics of recombinant human CYP2C19 enzyme at 37C in the presence and absence of the indicated inhibitor (solvent control reaction includes final concentration of 0.5% acetonitrile).
Dose-response curves for various CYP2C19 ligands of differing structural and mechanistic classes. For dose-response curves, percent activity was calculated for each concentration of inhibitor by comparison to activity of reactions containing no inhibitor. For each CYP2C19 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.
ab211073 has not yet been referenced specifically in any publications.