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Cytochrome P450 2D6 (CYP2D6) Inhibitor Screening Kit (Fluorometric) (CAT#: CB-P243-K) Datasheet

Product Type
Cytochrome P450 2D6 (CYP2D6, EC is a member of the cytochrome P450 monooxidase (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. CYP2D6 catalyzes the oxidation of lipophilic bases with aromatic rings and nitrogen atoms, and is highly expressed in liver and brain tissues. This enzyme is responsible for nearly 25% of the metabolism of all small molecule drugs commonly used by humans (especially psychotropic drugs such as antidepressants, antipsychotics and stimulants). The CYP2D6 gene is highly polymorphic in the population. According to allelic variation and gene copy number, the CYP2D6 activity produced ranges from complete metabolism deficiency to ultra-rapid metabolism. Due to this wide phenotypic variability, CYP2D6 is usually associated with drug toxicity and clinical drug/drug interactions. In addition, for drugs whose pharmacological activity needs to be metabolized from the prodrug form, CYP2D6 inhibition or allele deficiency can lead to reduced drug efficacy. Creative Biolabs' CYP2D6 inhibitor screening kit can quickly screen drugs and other new chemical entities (NCE) compound-CYP2D6 interactions in a reliable, high-throughput Fluorometric-based assay. This kit provides yeast microsomal preparations of human CYP2D6 and cytochrome P450 reductase (CPR) enzymes. The assay utilizes a non-fluorescent CYP2D6 selective substrate, which is converted into a highly fluorescent metabolite detected in the visible light range (Ex / Em = 390/468 nm), thereby ensuring a high signal-to-noise ratio, And is rarely interfered by autoFluorometric. The kit contains a complete set of reagents, enough to perform 200 reactions in a 96-well plate format.
200 assays

Figure 1 AHMC standard curve.

Figure 2 Reaction kinetics of recombinant human CYP2D6 enzyme at 37°C in the presence and absence of the indicated CYP2D6 inhibitors.

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