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Cytochrome P450 2C9 (CYP2C9) Inhibitor Screening Kit (CAT#: CB-P241-K) Datasheet

Product Type
Cytochrome P450 2C9 (CYP2C9, 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. CYP2C9 is mainly expressed in the liver and catalyzes the oxidation of weakly acidic or hydrophobic small molecules containing aromatic moieties and at least one hydrogen bond donor. The isoforms of the CYP2C subfamily are responsible for nearly 20% of the metabolism of all small molecule drugs commonly used in humans. The human CYP2C9 gene is highly polymorphic, and CYP2C9 single nucleotide polymorphism (SNP) has been associated with clinical drug/drug interactions, involving prescription drugs with a wide range of interactions, these drugs have a narrow therapeutic index, such as warfarin, Phenytoin and indomethacin. In addition, for drugs whose pharmacological activity needs to be metabolized from the form of prodrugs (such as the antihypertensive drug Losartan), CYP2C9 inhibition or allele deficiency can reduce the efficacy of the drug. Creative Biolabs' CYP2C9 inhibitor screening kit can quickly screen drugs and other new chemical entities (NCE) compound-CYP2C9 interactions in a reliable, high-throughput Fluorometric-based assay. This kit provides yeast microsomal preparations of human CYP2C9 and human cytochrome P450 reductase (CPR) enzymes. The assay utilizes a non-fluorescent CYP2C9 substrate, which is converted into a highly fluorescent metabolite detected in the visible light range (Ex / Em = 415/502 nm), thus ensuring a high signal-to-noise ratio. It is rarely interfered by autoFluorometric. The kit contains a complete set of reagents, enough to perform 100 reactions in a 96-well plate format.
100 assays

Figure 1 7-hydroxy-4-(trifluoromethyl)coumarin (7-HFC) standard curve.

Figure 2 Reaction kinetics of recombinant human CYP2C9 enzyme at 37°C in the presence and absence of the indicated CYP2C9 inhibitors.

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