Cytochrome P450 2C19 (CYP2C19) Activity Assay Kit (Fluorometric) (CAT#: CB-P238-K) Datasheet

Kit

Cytochrome P450 2C19 (CYP2C19, EC 1.14.14.1) is a member of the cytochrome P450 monooxidase (CYP) family of microsomal xenobiotic metabolizing 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. CYP2C19 is mainly expressed in liver and intestinal tissues, and catalyzes the oxidation of neutral or weakly alkaline lipophilic molecules with 2-3 hydrogen bond donor/acceptor sites. The isoforms of the CYP2C subfamily are responsible for nearly 20% of the metabolism of all small molecule drugs commonly used in humans. The polymorphism of the human CYP2C19 gene is related to clinical drug/drug interactions involving a wide range of prescription drugs, including proton pump inhibitors, antiplatelet drugs, and anticonvulsants. In addition, for drugs whose pharmacological activity needs to be metabolized from the prodrug form, CYP2C19 inhibition or allele deficiency will lead to reduced drug efficacy. Creative Biolabs' CYP2C19 activity assay kit can quickly measure the activity of natural or recombinant CYP2C19 in biological samples (such as liver microsomes). The assay uses a non-fluorescent CYP2C19 substrate, which is converted to a highly fluorescent metabolite detected in the visible light range (Ex / Em = 406/468 nm), thus ensuring a high signal-to-noise ratio, while autofluorescent The interference is minimal. Provides a highly selective CYP2C19 inhibitor for the assay of CYP2C19 activity in heterogeneous biological samples, where other CYP isoenzymes may contribute to substrate metabolism. Compared with other CYPs, this inhibitor has a selectivity of CYP2C19 more than 100 times higher, thus ensuring targeted inhibition. The specific activity of CYP2C19 is calculated by performing parallel reactions in the presence and absence of a selective inhibitor and subtracting any residual activity found in the presence of the inhibitor. The kit contains a complete set of reagents, enough to perform 50 paired reactions (in the presence and absence of inhibitors).