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Cytochrome P450 3A4 (CYP3A4) Inhibitor Screening Kit (Fluorometric)

High-throughput compatible, quick and easy screening for CYP3A inhibitors or ligands; Includes human CYP3A4 - NADPH Reductase.
Catalog #: K702
$595.00

Product Details

Cat # +Size K702-200
Size 200 assays
Detection Method Fluorescence (Ex/Em 535/587 nm)
Species Reactivity Eukaryotes
Applications Rapid, high-throughput screening of drugs and novel ligands.
Development of structure-activity relationship (SAR) models to predict CYP3A4 inhibition liability of novel compounds.
Prediction of adverse drug-drug interaction potential and bioavailability for compounds metabolized by CYP3A4.
Features & Benefits • Simple, highly sensitive, high-throughput compatible
• Rapid screening of CYP3A4 inhibitors or ligands
• Kit includes the canonical CYP3A inhibitor ketoconazole and a stable, recombinant human CYP3A4 co-expressed with NADPH Reductase
Kit Components • CYP3A4 Assay Buffer
• Resorufin Standard (5 mM in DMSO)
• CYP3A4 Inhibitor (Ketoconazole)
• NADPH Generating System (100X)
• β-NADP+ Stock (100X)
• CYP3A4 Substrate
• Recombinant Human CYP3A4
Storage Conditions -20°C
Shipping Conditions Gel Pack
USAGE For Research Use Only! Not For Use in Humans.

Details

Cytochrome P450 3A4 (CYP3A4, EC 1.14.13.157) 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 transformed to more hydrophilic products to facilitate excretion from the body. CYP3A4 is expressed in high levels in the liver and intestines, where it catalyzes oxidation of an extraordinarily wide variety of structurally distinct ligands. More than half of all small molecule drugs commonly used by humans are metabolized by CYP3A4 and inhibition of CYP3A4-mediated metabolism is a common cause of adverse drug/drug and drug/food interactions and toxicity. In addition, for drugs whose pharmacological activity requires metabolism from a pro-drug form, CYP3A4 inhibition can lead to decreased drug efficacy. BioVision’s CYP3A4 Inhibitor Screening Kit enables rapid screening of drugs and other new chemical entities (NCEs) for compound-CYP3A4 interaction in a reliable, high-throughput fluorescence-based assay. The kit provides a yeast microsomal preparation of human CYP3A4 and cytochrome P450 reductase (CPR) enzymes. The assay utilizes a non-fluorescent CYP3A4 substrate that is converted into a highly fluorescent metabolite detected in the visible range (Ex/Em = 535/587 nm), ensuring a high signal-to-background ratio with little interference by autofluorescence. The concentration of fluorogenic substrate used for screening is roughly equivalent to its Km for CYP3A4, facilitating detection of weak competitive inhibitors. The kit contains a complete set of reagents sufficient for performing 200 reactions in a 96-well plate format.


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Can we use frozen samples with this assay?
We would recommend using fresh samples. However, frozen samples can be used too provided they have not undergone multiple freeze thaw cycles.
Can the kit work on bacteria or yeast cells?
The kit has been standardized for mammalian cells only.
What is the exact volume of sample required for this assay?
There is no specific volume we can recommend for the amount any sample to be used since it is completely sample concentration and quality based. You have to do a pilot expt with multiple sample volumes to determine the optimal volume which gives a reading within the linear range of the standard curve. Please refer to the citations for this product to see what other clients have used with similar sample types.
Do you have trial sizes of this kit?
Unfortunately, we do not have trial sizes of this kit available. However, if you are based in the US or Canada, we will give you a 10% off list price introductory discount on its purchase price. If you are based out of this area please contact your regional BioVision distributor.
What is the shelf life of this kit?
BioVisions’s assay kits expire 6-12 months from the date of shipment. Some components of the kit may expire sooner as mentioned in the data sheet.
Can we purchase individual components of this kit?
Yes, you can purchase any of the kit's components without the whole kit. Please refer to the component Cat #s mentioned on the datasheet for ordering.
Can we use an alternate buffer for sample preparation (cell lysis, sample dilutions etc)?
Our assay buffers are optimized for the reactions they are designed for. They not only contain some detergents for efficient lysis of your cells/tissue, but also contain some proprietary components required for the further reactions. Therefore, we highly recommend using the buffers provided in the kit for the best results.