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HTS034M ChemiSCREEN™ NTR1 Membrane Preparation

Human NTR1 / NTS1 GPCR membrane preparation for Radioligand binding Assays & GTPgammaS binding.

ChemiSCREEN™ NTR1 Membrane Preparation MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
Host Cell: Chem-2 Uni Prot Number: P30989 Entrez Gene Number: NM_002531.2
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HTS034M
200 assays  
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      Overview

      Replacement Information

      Key Spec Table

      SpeciesHost CellsProtein Target
      Human Chem-2NTR1 / NTS1
      Description
      Catalogue NumberHTS034M
      Brand Family Chemicon®
      Trade Name
      • ChemiScreen
      • Chemicon
      DescriptionChemiSCREEN™ NTR1 Membrane Preparation
      OverviewHuman NTR1
      Background InformationNeurotensin is a 13 amino acid peptide that induces hypothermia and mediates analgesia when administered centrally, and also mediates the behavioral effects of antipsychotic drugs in rodents (Kinkead and Nemeroff, 2004). In addition, several intestinal functions, such as contractility and inflammation, are mediated by neurotensin (Castagliuolo et al., 1999). The actions of neurotensin are mediated by two GPCRs, NTR1 (or NTS1) and NTR2 (or NTS2). NTR1 knockout mice are resistant to the hypothermic, analgesic and contractile effects of neurotensin, indicating that NTR1 is the primary mediator of these effects (Pettibone et al., 2002). Small molecule antagonists, including SR48692 and SR142948A, that are partially selective for NTR1 also interfere with the biological effects of neurotensin (Labbé-Jullié et al., 1998).

      Chemicon's NTR1 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 antagonists of neurotensin/NTR1 interactions. The membrane preparations exhibit a Kd of 1.5 nM for [125I]-neurotensin. With 2.5 μg/well NTR1 Membrane Prep and 0.5 nM [125I]-neurotensin, a greater than 7-fold signal-to-background ratio is obtained.
      References
      Product Information
      FormatMembranes
      PresentationPACKAGING: Packaging buffer: 50 mM Tris pH 7.4, 10% glycerol and 1% BSAPackaging method: Membranes protein were adjusted to 0.5 mg/ml in 1 ml packaging buffer, rapidly frozen, and stored at -80oC.
      Quality LevelMQ100
      Applications
      ApplicationHuman NTR1 / NTS1 GPCR membrane preparation for Radioligand binding Assays & GTPgammaS binding.
      Key Applications
      • Radioligand binding assay
      • GTPγS binding
      Application NotesRadioligand binding assay, and GTPgammaS binding.
      Biological Information
      Concentration0.5 mg/mL
      Entrez Gene Number
      Entrez Gene SummaryNeurotensin receptor 1 belongs to the large superfamily of G-protein coupled receptors. NTSR1 mediates the multiple functions of neurotensin, such as hypotension, hyperglycemia, hypothermia, antinociception, and regulation of intestinal motility and secretion.
      Gene Symbol
      • NTSR1
      • NTRR
      • NT-R-1
      • NTRH
      • NTR
      GPCR ClassA
      Host CellsChem-2
      Protein TargetNTR1 / NTS1
      Target Sub-FamilyNeurotensin
      UniProt Number
      UniProt SummaryFUNCTION: SwissProt: P30989 # Receptor for the tridecapeptide neurotensin. It is associated with G proteins that activate a phosphatidylinositol- calcium second messenger system.
      SIZE: 418 amino acids; 46259 Da
      SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein.
      SIMILARITY: SwissProt: P30989 ## Belongs to the G-protein coupled receptor 1 family.
      Incubation ConditionsBinding buffer: 50mM HEPES, 5mM MgCl2, 1mM CaCl2, 0.2% BSA, pH to 7.4 and filter.
      Radioligand: [125I] Neurotensin (PerkinElmer#: NEX198)
      One vial contains enough membranes for at least 200 assays (units), where an unit is the amount of membrane that will yield greater than 5-fold signal:background with 125I-labeled neurotensin at 0.5 nM.
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Signal:background and specific binding values obtained in a competition binding assay with NTR1 membrane prep:
      Product Usage Statements
      5 µg/well
      Signal:Background 47
      Specific Binding (cpm) 17556


      SPECIFICATIONS: 1 unit = 5 µg
      Bmax: 12.9 pmol/mg
      Kd: 1.5 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 assays
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      HTS034M 04053252287916

      Documentation

      Protocols

      Title
      Assembly of a Competition Binding Curve

      ChemiSCREEN™ NTR1 Membrane Preparation SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overviewPub Med ID
      Neurotensin, schizophrenia, and antipsychotic drug action
      Kinkead, Becky and Nemeroff, Charles B
      Int Rev Neurobiol, 59:327-49 (2004)  2004

      		15006494 15006494
      The effects of deleting the mouse neurotensin receptor NTR1 on central and peripheral responses to neurotensin
      Pettibone, Douglas J, et al
      J Pharmacol Exp Ther, 300:305-13 (2002)  2002

      		11752130 11752130
      Neurotensin is a proinflammatory neuropeptide in colonic inflammation
      Castagliuolo, I, et al
      J Clin Invest, 103:843-9 (1999)  1999

      		10079105 10079105
      Mutagenesis and modeling of the neurotensin receptor NTR1. Identification of residues that are critical for binding SR 48692, a nonpeptide neurotensin antagonist
      Labbé-Jullié, C, et al
      J Biol Chem, 273:16351-7 (1998)  1998

      		9632698 9632698

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