Cytochrome P450 3A4 (CYP3A4) Activity Assay Kit (Fluorometric) (CAT#: CB-P244-K) Datasheet

Kit

Cytochrome P450 3A4 (CYP3A4, EC 1.14.13.157) 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 unique 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 adverse drug/drug 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 activity assay kit can quickly measure the activity of natural or recombinant CYP3A4 in biological samples (such as liver microsomes). 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 specific activity of CYP3A4 was calculated by performing parallel reactions in the presence and absence of the effective inhibitor ketoconazole, and subtracting any residual activity found in the presence of the inhibitor. The kit contains a complete set of reagents, enough to perform 100 paired reactions (in the presence and absence of inhibitors).