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HTS101M CHEMISCREEN™ MEMBRANE PREPARATION RECOMBINANT HUMAN µ (Mu) OPIOID RECEPTOR

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HTS101M
200 units  
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      Overview

      Replacement Information

      Key Specifications Table

      SpeciesHost CellsProtein Target
      Human Chem-5Mu / OP3 / MOP / MOR
      Description
      Catalogue NumberHTS101M
      Trade Name
      • ChemiScreen
      • Chemicon
      DescriptionCHEMISCREEN™ MEMBRANE PREPARATION RECOMBINANT HUMAN µ (Mu) OPIOID RECEPTOR
      OverviewFull-length human OPRM1 cDNA encoding Mu
      Background InformationOpiates derived from the opium poppy, Papaver somniferum, have been used in for millenia for their anti-diarrheal, analgesic and euphoric properties. More recently, endogenous peptides, enkephalins, dynorphins, and endorphins, were found to bind to the same sites as opiate alkaloids. The receptors for the classical opioids are three related GPCRs, µ κ and δ that activate Gi/o to reduce intracellular cAMP levels. Most clinically used opioids function by activation of the µ opioid receptor (Dhawan et al., 1996). Chemicon's µ opioid receptor membrane preparations are crude membrane preparations made from our proprietary stable recombinant cell lines to ensure high-level of GPCR surface expression; thus, they are ideal HTS tools for screening of µ opioid receptor interactions with its ligands. The membrane preparations exhibit an EC50 of 1.6nM for DAMGO in a GTPγS binding assay.
      References
      Product Information
      FormatMembranes
      PresentationLiquid in packaging buffer: 50 mM Tris pH 7.4, 10% glycerol and 1% BSA with no preservatives.
      Packaging method: Membrane protein was adjusted to the indicated concentration in packaging buffer, rapidly frozen, and stored at -80°C
      Quality LevelMQ100
      Applications
      ApplicationHuman Mu / OP3 / MOP / MOR GPCR membrane preparation for GTPγS Binding & Radioligand Binding Assays.
      Key Applications
      • GTPγS binding
      • Radioligand binding assay
      Application NotesGTPγS Binding and Radioligand Binding Assay.
      Biological Information
      Entrez Gene Number
      Gene Symbol
      • OPRM1
      • MOR-1
      • MOR1
      • KIAA0403
      • OPRM
      GPCR ClassA
      Host CellsChem-5
      Protein TargetMu / OP3 / MOP / MOR
      Target Sub-FamilyOpioid
      UniProt Number
      UniProt SummaryFUNCTION: SwissProt: P35372 # Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Receptor for beta-endorphin.
      SIZE: 400 amino acids; 44779 Da
      SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein.
      SIMILARITY: SwissProt: P35372 ## Belongs to the G-protein coupled receptor 1 family.
      Incubation ConditionsASSAY CONDITIONS: Membranes are permeabilized by addition of saponin to an equal concentration by mass, then mixed with [35S]-GTPγS (final concentration of 0.3 nM) in 20 mM HEPES, pH 7.4/100 mM NaCl/10 mM MgCl2/0.5 μM GDP in a nonbinding 96-well plate. Unlabeled DAMGO added to the final concentration indicated in Figure 1 (final volume 100 μL), and incubated for 30 min at 30°C. The binding reaction is transferred to an FB filter plate (Millipore MAHF B1H) previously prewetted with water, and washed 3 times (1 mL per well per wash) with cold 10 mM sodium phosphate, pH 7.4. The plate is dried and counted.

      One vial contains enough membranes for at least 200 assays (units), where one unit is the amount of membrane that will yield greater than 1000 cpm specific DAMGO-stimulated [35S]-GTPγS binding.
      The μ opioid receptor membrane preparation is expected to be functional in a radioligand binding assay; however, the end user will need to determine the optimal radiolabeled ligand for use with this product.
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Quality AssuranceEC50 in GTPγS binding assay by DAMGO: ~ 1.6 nM
      Usage Statement
      • Unless otherwise stated in our catalog or other company documentation accompanying the product(s), our products are intended for research use only and are not to be used for any other purpose, which includes but is not limited to, unauthorized commercial uses, in vitro diagnostic uses, ex vivo or in vivo therapeutic uses or any type of consumption or application to humans or animals.
      Storage and Shipping Information
      Storage ConditionsMaintain frozen at -70°C for up to 2 years. Do not freeze and thaw.
      Packaging Information
      Material Size200 units
      Transport Information
      Supplemental Information
      Specifications

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      Categories

      Life Science Research > Drug Discovery and Development > GPCR Cell Lines & Assays > GPCR Membrane Preparations
      Life Science Research > Proteins and Enzymes > GPCR Membrane Preparations