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CYP3A4 Inhibitor Screening Kit (Fluorometric) 

  • Catalog # : KA6487
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  • Specification
  • Product Description:
  • CYP3A4 Inhibitor Screening Kit (Fluorometric)
  • Storage Instruction:
  • Store the kit at -20°C.
    Avoid repeated freezing and thawing.
  • Detection Method:
  • Fluorescence (Ex/Em 535/587 nm)
  • Applications
  • Inhibition Assay
  • Dose-response curves for various CYP3A4 inhibitors of differing structural and mechanistic classes: the canonical competitive CYP3A4 inhibitor Ketoconazole, the selective mechanism-based CYP3A4 inhibitors Azamulin and cyp3cide, and bromocriptine, a CYP3A4 substrate that acts as a weak enzyme inhibitor. For dose-response curves, percent activity was calculated for each concentration of inhibitor by comparison to activity of reactions containing no inhibitor. For each CYP3A4 inhibitor, IC50 values were derived by 4-parameter logistic curve fitting and represent the mean ± SEM of at least three replicate experiments.
  • Application Image
  • Inhibition Assay
  • Gene Information
  • Entrez GeneID:
  • 1576
  • Gene Name:
  • CYP3A4
  • Gene Alias:
  • CP33,CP34,CYP3A,CYP3A3,HLP,MGC126680,NF-25,P450C3,P450PCN1
  • Gene Description:
  • cytochrome P450, family 3, subfamily A, polypeptide 4
  • Gene Summary:
  • This gene, CYP3A4, encodes a member of the cytochrome P450 superfamily of enzymes. The cytochrome P450 proteins are monooxygenases which catalyze many reactions involved in drug metabolism and synthesis of cholesterol, steroids and other lipids. This protein localizes to the endoplasmic reticulum and its expression is induced by glucocorticoids and some pharmacological agents. This enzyme is involved in the metabolism of approximately half the drugs which are are used today, including acetaminophen, codeine, cyclosporin A, diazepam and erythromycin. The enzyme also metabolizes some steroids and carcinogens. This gene is part of a cluster of cytochrome P450 genes on chromosome 7q21.1. Previously another CYP3A gene, CYP3A3, was thought to exist; however, it is now thought that this sequence represents a transcript variant of CYP3A4. [provided by RefSeq
  • Other Designations:
  • P450-III, steroid inducible,cytochrome P450, subfamily IIIA (niphedipine oxidase), polypeptide 3,cytochrome P450, subfamily IIIA (niphedipine oxidase), polypeptide 4,cytochrome P450, subfamily IIIA, polypeptide 4,glucocorticoid-inducible P450,nifedipine o
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