Summary: CYP1A2 Activity Assay Kit enables rapid measurement of native or recombinant CYP1A2 activity in biological samples such as liver microsomes. The assay utilizes a non-fluorescent CYP1A2 substrate that is converted into a highly fluorescent metabolite detected in the visible range (Ex/Em = 406/468 nm), ensuring a high signal-to-background ratio with little interference by autofluorescence. A selective CYP1A2 inhibitor is provided for determination of CYP1A2 activity in heterogeneous biological samples, where other CYP isozymes may contribute to substrate metabolism. The inhibitor displays greater than 20-fold selectivity for CYP1A2 over other CYPs, ensuring targeted inhibition. CYP1A2 specific activity is calculated by running parallel reactions in the presence and absence of the selective inhibitor and subtracting any residual activity detected with the inhibitor present. The kit contains a complete set of reagents sufficient for performing 50 sets of paired reactions (in the presence a