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.
Size
200 assays
Concentration
n/a
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.