HTS163M ChemiSCREEN™ Membrane Preparation Recombinant Human GLP-1

HTS163M
200 units  
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      Overview

      Replacement Information

      Key Specifications Table

      SpeciesHost CellsProtein Target
      Human Chem-9 GLP-1
      Description
      Catalogue NumberHTS163M
      Brand Family Chemicon®
      Trade Name
      • ChemiScreen
      • Chemicon
      DescriptionChemiSCREEN™ Membrane Preparation Recombinant Human GLP-1
      OverviewHuman GLP-1
      Background InformationGlucagon-like peptide-I (GLP-1), a member of the glucagon-secretin peptide family, is secreted from L-cells of the small intestine and binds to a class B (class 2) G protein-coupled receptor (Mayo et al. 2003). The GLP-1 receptor is expressed in pancreatic beta cells and upon binding to GLP-1, it couples to Gs to increase cAMP levels and insulin secretion (Drucker et al. 1987). In addition, GLP-1 has been shown to delay gastric emptying and regulate appetite. Therefore, the GLP-1 receptor represents an important therapeutic target for type II diabetes, and a degradation-resistant analog of GLP-1, exanatide, is used clinically in combination with other glucose-lowering drugs to control type II diabetes (D’Alessio et al. 2004). Millipore's GLP-1 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 for agonists and antagonists at the GLP-1 receptor. The membrane preparations exhibit a Kd of 0.27 nM for [125I]-GLP-1. With 10 μg/well GLP-1 Receptor Membrane Prep and 0.5 nM [125I]-GLP-1, a greater than 9-fold signal-to-background ratio was obtained.
      References
      Product Information
      FormatMembranes
      PresentationOne package contains enough membranes for at least 200 assays (units), where an unit is the amount of membrane that will yield greater than 9-fold signal:background with 125I-labeled GLP-1 at 0.5 nM.

      Liquid in packaging buffer: 50 mM Tris pH 7.4, 10% glycerol and 1% BSA with no preservatives.
      Packaging method: Membranes protein were adjusted to the indicated concentration in packaging buffer, rapidly frozen, and stored at -80°C.
      Applications
      ApplicationHuman GLP-1 GPCR membrane preparation for Radioligand binding Assays & GTPγS binding.
      Key Applications
      • Radioligand binding assay
      • GTPγS binding
      Application NotesRadioligand binding assay, and GTPγS binding.
      Biological Information
      Entrez Gene Number
      Gene Symbol
      • GLP1R
      • MGC138331
      • GLP-1R
      • GLP-1-R
      GPCR ClassB
      Host CellsChem-9
      Protein TargetGLP-1
      Target Sub-FamilyGlucagon
      UniProt Number
      UniProt SummaryFUNCTION: SwissProt: P43220 # This is a receptor for glucagon-like peptide 1. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
      SIZE: 463 amino acids; 53060 Da
      SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein.
      SIMILARITY: SwissProt: P43220 ## Belongs to the G-protein coupled receptor 2 family.
      Incubation ConditionsMembranes are mixed with radioactive ligand and unlabeled competitor (see Figures 1 and 2 for concentrations tested) in binding buffer in a nonbinding 96-well plate, and incubated for 1-2 h. Prior to filtration, a GF/C 96-well filter plate is coated with 0.33% polyethyleneimine for 30 min, then washed with 50mM HEPES, pH 7.4, 0.5% BSA. Binding reaction is transferred to the filter plate, and washed 3 times (1 mL per well per wash) with Wash Buffer. The plate is dried and counted.

      Binding buffer: 50 mM Hepes, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.2% BSA, filtered and stored at 4°C
      Radioligand: [125I] GLP-1(7-36) (Perkin Elmer # NEX308)
      Wash Buffer: 50 mM Hepes, pH 7.4, 500mM NaCl , 0.1% BSA, filtered and stored at 4°C.
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      SPECIFICATIONS:
      Signal:background and specific binding values obtained in a competition binding assay with varying amounts of GLP-1 membrane prep:
      Product Usage Statements
      20 µg/well 10 µg/well
      Signal:Background 12.0 14.9
      Specific Binding (cpm) 31366 27411


      1 unit = 10 µg membrane preparation


      Bmax: 3.96 pmol/mg


      Kd: 0.27 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

      Documentation

      ChemiSCREEN™ Membrane Preparation Recombinant Human GLP-1 SDS

      Title

      Safety Data Sheet (SDS) 

      ChemiSCREEN™ Membrane Preparation Recombinant Human GLP-1 Certificates of Analysis

      TitleLot Number
      CHEMISCREEN MEMBRANE PREPARATION RECOMBINANT HUMAN GLP-1 GLUCAGON FAMILY RECEPTOR -
      CHEMISCREENTM MEMBRANE PREPARATION RECOMBINANT HUMAN GLP-1 GLUCAGON FAMILY RECEPTOR - 21440922144092
      CHEMISCREENTM MEMBRANE PREPARATION RECOMBINANT HUMAN GLP-1 GLUCAGON FAMILY RECEPTOR - 20379002037900
      CHEMISCREEN™ MEMBRANE PREPARATION RECOMBINANT HUMAN GLP-1 GLUCAGON FAMILY RECEPTOR - SC031698SC031698

      References

      Reference overviewPub Med ID
      International Union of Pharmacology. XXXV. The glucagon receptor family.
      Mayo KE et al.
      Pharmacol. Rev., 55:167-194 (2003)  2003

      12615957 12615957

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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