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早期筛选候选药物诱导或抑制CYP2C9的潜力是药物开发过程中的关键步骤。CYP2C9诱导报告基因检测试剂盒是一种评估候选药物诱导CYP2C9的新方法。Cayman的CYP2C9诱导报告基因检测试剂盒由96孔板组成,该板涂有转染复合物,其中包含受人类CYP2C9基因启动子调控的分泌性碱性磷酸酶(SEAP)报告基因。在CYP2C9报告基因反向转染条板上生长的细胞将引入报告基因并表达GRα以及HNF4α。促进核受体与CYP2C9启动子结合的测试化合物会启动SEAP表达。随后使用发光读数测量SEAP活性。该试剂盒使用简单,可轻松适应高通量筛选潜在的核受体介导的CYP2C9诱导剂。Early screening of drug candidate's potential to induce or inhibit CYP2C9 is a critical step in the drug development process. The CYP2C9 Induction Reporter Assay Kit is a novel method to evaluate CYP2C9 induction by drug candidates. Cayman's CYP2C9 Induction Reporter Assay Kit consists of a 96-well plate coated with a transfection complex containing a Secreted Alkaline Phosphatase (SEAP) reporter regulated by the human CYP2C9 gene promoter. Cells grown on the CYP2C9 Reporter Reverse Transfection Strip Plate will introduce the reporter gene and express GRα as well as HNF4α. Test compounds that promote binding of the nuclear receptors to the CYP2C9 promoter initiates SEAP expression. SEAP activity is subsequently measured using a luminescence readout. The kit is simple to use and can be easily adapted to high-throughput screening for potential nuclear receptor-mediated CYP2C9 inducers.分子式分子量
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CYP2C9 Induction Reporter Assay Kit
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