Monoacylglycerol Lipase Inhibitor Screening Kit (Fluorometric)

  • Catalog number
    K474-100
  • Price
    Please ask
  • Size
    100 assays
  • Description
    Industry's most sensitive kit to evaluate potential ECE1 inhibitors
  • Summary
    • Detection method - Fluorescence (Ex/Em = 360/460 nm) • Applications- • Screening for inhibitors of human MAGL enzyme
  • Detection Method
    Fluorometric (Ex/Em = 360/460 nm)
  • Species Reactivity
    Mammalian
  • Applications
    • Screening for inhibitors of human MAGL enzyme
  • Sample Type
    Not applicable
  • Features Benefits
    • Simple one-step reaction • Takes only 1-2 hrs • Non-radiometric fluorescent detection • HTP adaptable
  • Storage Conditions
    -20°C
  • Shipping Conditions
    gel pack
  • Shelf life
    12 months
  • Background
    Monoacylglycerol Lipase (MAGL, E.C. 3.1.1.23) is an important enzyme that regulates endocannabinoid signaling in human physiology. MAGL is a serine hydrolase that generates free fatty acid and glycerol from monoacylglycerol stores. One free fatty acid that is frequently generated by MAGL activity, arachidonic acid, is a precursor for eicosanoids, a family of pro-inflammatory signaling molecules. The glycerol moiety can also serve various purposes as a metabolic building block and energy source. Inhibition or inactivation of MAGL leads to 2-arachidonalglycerol (2-AG) buildup, and this has myriad biological consequences. Desensitization of the endocannabinoid receptors and reduced addiction withdrawal symptoms are one outcome of MAGL inhibition. In addition, the downstream eicosanoid signaling pathway is affected; this pathway plays a role in diverse physiological processes including inflammation, immunity, nociception and blood pressure. As a central node in the regulation of both lipid signaling and energy mobilization, MAGL is of considerable interest as a therapeutic target. BioVision’s Monoacylglycerol Lipase Inhibitor Screening Kit provides a straightforward method to identify inhibitors of human MAGL. In the assay, human recombinant MAGL is used to cleave an MAGL substrate, resulting in a fluorescence increase that is abrogated by the presence of an inhibitor for this enzyme. Specific inhibitors for this enzyme are of great clinical interest due to the central role for MAGL in lipid metabolism and energy storage
  • Additional description
    Tissue, pathway, proteinase, peptidase, protease ,acrosin, lipoprotein, activator, caspase, trypsin, papain, esterase inhibitors are proteins or receptor ligands or receptor antagonists that bind to an enzyme receptor and decreases its activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. Not all receptor antagonist that bind to enzymes are inhibitors; enzyme activator ligands or agonists bind to enzymes and increase their enzymatic activity, while enzyme substrates bind and are converted to products in the normal catalytic cycle of the enzyme.
  • Gene target
  • Short name
    Monoacylglycerol Lipase Inhibitor Screening Kit (Fluorometric)
  • Alternative name
    Monoacylglycerol Lipase suppressor detection reagent (fluorescence)
  • Alternative technique
    kits
  • Alternative to gene target
    v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog, C-Kit and CD117 and PBT and SCFR, KIT and IDBG-18980 and ENSG00000157404 and 3815, transferase activity, Extracellular, Kit and IDBG-172083 and ENSMUSG00000005672 and 16590, KIT and IDBG-642326 and ENSBTAG00000002699 and 280832
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