Product nameCYP2D6 Inhibitor Assay Kit (Fluorometric)
See all CYP2D6 kits
Sample typeInhibitor compounds
CYP2D6 Inhibitor Screening Kit (Fluorometric) (ab211079) allows rapid screening of drugs and other new chemical entities (NCEs) for CYP2D6-compound interaction in a reliable, high-throughput fluorescence-based assay. The kit provides a yeast microsomal preparation of human CYP2D6 and cytochrome P450 reductase (CPR) enzymes. The assay utilizes a non-fluorescent CYP2D6-selective substrate that is converted into a highly fluorescent metabolite detected in the visible range (Ex/Em = 390/468 nm), ensuring a high signal-to-background ratio with little interference by autofluorescence.
The kit contains a complete set of reagents sufficient for performing 200 reactions in a 96 well plate format.
Cytochrome P450 2D6 (CYP2D6, EC 126.96.36.199) 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. CYP2D6 catalyzes oxidation of lipophilic bases with an aromatic ring and a nitrogen atom and is highly expressed in liver and brain tissue. The enzyme is responsible for metabolism of nearly 25% of all small molecule drugs commonly used by humans, particularly psychiatric drugs such as antidepressants, antipsychotics and stimulants. The CYP2D6 gene is highly polymorphic in the human population, with resulting CYP2D6 activity ranging from complete metabolic deficiency to ultra-rapid metabolism depending upon allelic variation and gene copy number. Due to this wide phenotypic variability, CYP2D6 is frequently implicated in drug toxicity and clinical drug/drug interactions.
Storage instructionsStore at -20°C. Please refer to protocols.
Components 200 tests β-NADP+ Stock 100X (2 mg) 1 vial AHMC Standard (in DMSO) 1 x 25µl CYP2D6 Assay Buffer 1 x 100ml CYP2D6 Inhibitor (Quinidine) (150 µg) 1 vial CYP2D6 Substrate (200 µg) 1 vial NADPH Generating System 100X (25 mg) 1 vial Recombinant Human CYP2D6 (2 x 15 mg) 2 vials
- Pathways and Processes
- Metabolic signaling pathways
- Lipid and lipoprotein metabolism
FunctionResponsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Sequence similaritiesBelongs to the cytochrome P450 family.
Cellular localizationEndoplasmic reticulum membrane. Microsome membrane.
- Information by UniProt
- Cholesterol 25-hydroxylase
Typical AHMC standard calibration curve. One mol of AHMC corresponds to the metabolism of one mol of CYP2D6 substrate.
Reaction kinetics of recombinant human CYP2D6 enzyme at 37°C in the presence and absence of the indicated inhibitor (solvent control reaction includes final concentration of 0.5% acetonitrile).
Dose-response curves for various CYP2D6 ligands of differing structural and mechanistic classes: the canonical competitive CYP2D6 inhibitor quinidine, dextromethorphan, a prototypical CYP2D6 substrate and the antidepressants fluoxetine and paroxetine (a mechanism-based, irreversible CYP2D6 inhibitor). For dose-response curves, percent activity was calculated for each concentration of inhibitor by comparison to activity of reactions containing no inhibitor. For each CYP2D6 inhibitor, IC50 values were derived by 4-parameter logistic curve fitting with points representing the mean ± SEM of at least three replicate experiments. Assays were performed according to the kit protocol.
ab211079 has been referenced in 1 publication.
- Seggio M et al. Preclinical evidence of enhanced analgesic activity of duloxetine complexed with succinyl-ß-cyclodextrin: A comparative study with cyclodextrin complexes. Int J Pharm 566:391-399 (2019). PubMed: 31158453