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Cytochrome P450 3A4 (CYP3A4) Inhibitor Screening Kit (Fluorometric) (CAT#: CB-P245-K) Datasheet

Product Type
Cytochrome P450 3A4 (CYP3A4, EC is a member of the cytochrome P450 monooxygenase (CYP) family of microsomal heterologous biological metabolic enzymes. CYP is the membrane-bound hemoglobin responsible for the phase I biotransformation reaction, in which lipophilic drugs and other heterogeneous biological compounds are converted into more hydrophilic products to promote human excretion. CYP3A4 is expressed at high levels in the liver and intestines, where it catalyzes the oxidation of a variety of structurally different ligands. More than half of all small molecule drugs commonly used in humans are metabolized by CYP3A4. Inhibition of CYP3A4-mediated metabolism is a common cause of drug/drug adverse reactions, drug/food interactions and toxicity. In addition, for drugs whose pharmacological activity needs to be metabolized from the prodrug form, CYP3A4 inhibition may lead to reduced drug efficacy. Creative Biolabs' CYP3A4 inhibitor screening kit enables rapid screening of drugs and other new chemical entities (NCE) compound-CYP3A4 interactions in a reliable, high-throughput Fluorometric-based assay. This kit provides yeast microsomal preparations of human CYP3A4 and cytochrome P450 reductase (CPR) enzymes. This assay utilizes a non-fluorescent CYP3A4 substrate, which is converted into a highly fluorescent metabolite detected in the visible light range (Ex / Em = 535/587 nm), thus ensuring a high signal-to-noise ratio. The interference of autoFluorometric is very small. The concentration of the fluorescent substrate used for screening is approximately equal to the Km of its CYP3A4, which helps to detect weakly competitive inhibitors. The kit contains a complete set of reagents, enough to perform 200 reactions in a 96-well plate format.
200 assays

Figure 1 Resorufin standard curve.

Figure 2 Reaction kinetics of recombinant human CYP3A4 enzyme at 25°C in the presence and absence of the indicated CYP3A4 inhibitors.

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