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HTS033M | ChemiSCREEN™ GPR14 Membrane Preparation

200 assays  
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      Key Specifications Table

      SpeciesHost CellsProtein Target
      Human Chem-2 UT / UT1 / GPR14
      Catalogue NumberHTS033M
      Brand Family Chemicon®
      Trade Name
      • ChemiScreen
      • Chemicon
      DescriptionChemiSCREEN™ GPR14 Membrane Preparation
      OverviewTRANSFECTION: Full-length human GPR14 cDNA
      Background InformationUrotensin II, a cyclic 11-13 residue peptide expressed in motoneurons of the spinal cord, acts as a potent vasoconstrictor (Coulouarn et al., 1998; Ames et al., 1999). The effects of urotensin II are mediated by binding to a GPCR, GPR14, which is expressed in endothelium, smooth muscle, heart and pancreas (Ames et al., 1999). Genetic deletion of GPR14 in mice renders aortae refractile to the contractile activity of urotensin II without changing baseline hemodynamics (Behm et al., 2003). Pharmacological inhibition of urotensin II/GPR14 interactions prevents renal insufficiency following renal artery ligation (Clozel et al., 2004). Thus, GPR14 is an attractive target for a number of cardiovascular diseases. Chemicon's GPR14 Membrane Preparations are ideal tools for screening for antagonists of urotensin II/GPR14 interactions. The membrane preparations exhibit a Kd of 0.4 nM for [125I]-urotensin II. With 10 mg/well GPR14 Membrane Prep and 0.3 nM [125I]-urotensin II, a greater than 20-fold signal-to-background ratio is obtained.
      Product Information
      PresentationMembranes were adjusted to 0.5 mg protein/ml in 50 mM Tris pH 7.4, 10% glycerol and 1% BSA, rapidly frozen, and stored at -80°C. One vial typically contains 2000 units, where a unit is the amount of membrane that will yield greater than 1000 cpm specific binding of 125I-labeled urotensin II (0.3 nM input concentration).
      ApplicationHuman UT / UT1 / GPR14 GPCR membrane preparation for Radioligand binding Assays.
      Key Applications
      • Radioligand binding assay
      Application NotesRadioligand binding assay.
      Biological Information
      Entrez Gene Number
      Gene Symbol
      • UTS2R
      • GPR14
      • UR-II-R
      • UTR2
      • UTR
      GPCR ClassA
      Host CellsChem-2
      Protein TargetUT / UT1 / GPR14
      Target Sub-FamilyUrotensin II
      UniProt Number
      UniProt SummaryFUNCTION: SwissProt: Q9UKP6 # High affinity receptor for urotensin-2 and urotensin-2B. The activity of this receptor is mediated by a G-protein that activate a phosphatidylinositol-calcium second messenger system.
      SIZE: 389 amino acids; 42130 Da
      SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein.
      TISSUE SPECIFICITY: Most abundant expression in the heart and pancreas.
      SIMILARITY: SwissProt: Q9UKP6 ## Belongs to the G-protein coupled receptor 1 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 50 mM 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.
      Physicochemical Information
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Signal:background and specific binding values obtained in a competition binding assay with GPR14 membrane preparation.
      Product Usage Statements
      10 µg/well
      Signal:Background 28.5
      Specific Binding (cpm) 58253

      1 unit = 10 µg
      Bmax for [125I] urotensin II binding: 2.7 pmol/mg protein
      Kd for [125I] urotensin II binding: ~ 0.37 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

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      Life Science Research > Proteins and Enzymes > GPCR Membrane Preparations