CYP2B6 Induction Reporter Assay Kit

Territorial Availability: Available through Bertin Technologies only in France

• Correlated keywords
  • kits cells CBAs cell-based assays measuring measurement cytochromes P450s CYP450s CYP-450 heme-thiolates monoxygenases metabolizes endogenous compounds xenobiotics pollutants environmental drugs enzymes metabolisms medications pharmacokinetics multiple doses dosing CYP 2B6 CYP-2B6 biotransformations clinically isozymes inducible genes transcriptional nuclear receptors constitutive androstane hCAR3-mediated hCAR 3 hCAR3 hCAR-3 human activation translocations splice splicing variants activators CITCO 6-(4-clorophenyl)imidazo[2,1-b]thiazole-5-carbaldehydeO-(3,4-dichlorobenzyl)oxime phenobarbital inhibits inhibitors inhibition toxicity low efficacy efficacies developments primary hepatocytes hepatocyte-like regulatory pathways cultured lines transfected construct promoter/enhancer sequences high-throughput hepatic inducers Surface Transfection and Expression Protocol solid phases transient transfection technology technologies Originus Inc Incorproated University of Michigan UofM U of M USPT US patents 6897067 6902933 7056741 native recombinant proteins adherent coatings receptor-mediated endocytosis DNA deoxyribonucleic acids complexes solution-phases co-transfection Secreted Alkaline Phosphatase SEAP promoters Hepatocyte Nuclear Factor-4a HNF-4a Factor-4.alpha. HNF-4.alpha. Factor-4alpha HNF-4alpha Factor-4? HNF-4? inducers inducer-activated factors signals signaling mediums luminescence-based alkaline phosphotase substrates screening screens reverse reporter assay
• Product Overview:
  Early screening of a drug candidate’s potential to induce or inhibit CYP2B6 is a critical step in the drug development process. Cayman’s CYP2B6 Induction Reporter Assay Kit is a novel method to evaluate human Constitutive Androstane Receptor 3 (hCAR3)-mediated CYP2B6 induction for the discovery of hepatic CYP inducers. Our Reverse Transfection Reporter Assays have overcome many of the disadvantages of other transfection approaches. Cayman’s CYP2B6 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 CYP2B6 gene promoter. The complex also contains two nuclear receptor expression constructs, human Constitutive Androstane Receptor 3 (hCAR3) and human Hepatocyte Nuclear Factor 4? (HNF4?). Cells grown on the CYP2B6 Reverse Transfection Strip Plate will introduce the reporter gene and express CAR3 and HNF4?. Binding of inducer-activated receptor and transcription factors to the CYP2B6 promoter initiates a signal resulting in expression of SEAP, which is secreted into the cell culture medium. Aliquots of medium are removed at time intervals beginning at about 24 hours and SEAP activity is measured simply by adding a luminescence-based alkaline phosphatase substrate provided in the kit. The kit is simple to use and can be easily adapted to high-throughput screening for potential CAR-mediated CYP2B6 inducers. A known CYP2B6 inducer, CITCO, is included in the kit for use as a positive control.