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HTS144M ChemiSCREEN™ Membrane Preparation Recombinant Human NK2 Tachykinin Receptor

HTS144M
200 units  
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      Overview

      Key Spec Table

      SpeciesHost CellsProtein Target
      Human Chem-1NK2
      Description
      Catalogue NumberHTS144M
      Trade Name
      • ChemiScreen
      • Chemicon
      DescriptionChemiSCREEN™ Membrane Preparation Recombinant Human NK2 Tachykinin Receptor
      OverviewFull-length human TACR2 cDNA encoding NK2
      Background InformationThe tachykinin peptide family in mammals comprises three peptides, substance P, neurokinin A and neurokinin B, which bind to the tachykinin receptor family of GPCRs, NK1, NK2 and NK3 (Severini et al., 2002). Tachykinins have prominent activity in the GI system, in which they stimulate intestinal contraction and salivation; these effects are mediated by NK1 and NK2. Experiments with selective antagonists of NK2, SR 48,968 and MEN 10,376 indicate that NK2 mediates neurokinin- induced constriction of pulmonary artery and bronchus (Maggi et al., 1993). NK2 antagonists display efficacy in treatment of irritable bowel disorder (Lecci et al., 2004). Millipore's NK2 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 NK2 receptor interactions with its ligand. The membrane preparations exhibit a Kd of 0.76nM for [125I]-NKA. With 10.0 ug/well NK2 Membrane Prep and 0.5nM [125I]-NKA, a greater than 10-fold signal-to-background ratio was obtained.
      Product Information
      FormatMembranes
      PresentationLiquid in packaging buffer: 50 mM Tris pH 7.4, 10% glycerol and 1% BSA with no preservatives.
      Packaging method: Membranes protein was adjusted to the indicated concentration in packaging buffer, rapidly frozen, and stored at -80oC.
      Quality LevelMQ100
      Applications
      ApplicationHuman NK2 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
      Entrez Gene SummaryThis gene belongs to a family of genes that function as receptors for tachykinins. Receptor affinities are specified by variations in the 5'-end of the sequence. The receptors belonging to this family are characterized by interactions with G proteins and 7 hydrophobic transmembrane regions. This gene encodes the receptor for the tachykinin neuropeptide substance K, also referred to as neurokinin A.
      Gene Symbol
      • TACR2
      • SKR
      • NKNAR
      • NK-2R
      • NK2R
      • TAC2R
      GPCR ClassA
      Host CellsChem-1
      Protein TargetNK2
      Target Sub-FamilyTackykinin /neurokinin
      UniProt Number
      UniProt SummaryFUNCTION: SwissProt: P21452 # This is a receptor for the tachykinin neuropeptide substance K (neurokinin A). It is associated with G proteins that activate a phosphatidylinositol-calcium second messenger system.
      SIZE: 398 amino acids; 44439 Da
      SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein.
      SIMILARITY: SwissProt: P21452 ## Belongs to the G-protein coupled receptor 1 family.
      MISCELLANEOUS: The rank order of affinity of this receptor to tachykinins is: substance K > neuromedin-K > substance P.
      Incubation ConditionsRECOMMENDED ASSAY CONDITIONS: Membranes 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, an FC 96-well harvest plate (Millipore cat. # MAHF C1H) is coated with 0.33% polyethyleneimine for 30 min, then washed with 50mM Tris, pH 7.4. 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: 50mM Tris, pH 7.4, 150mM NaCl, 3mM MnCl2, 0.1% BSA, containing one Protease Inhibitor Cocktail Tablet (Roche Cat. No. 11 873 580 001) for each 50ml binding buffer.
      Radioligand: [125I]-NKA (NEX 252)
      Wash Buffer: 50mM Tris, pH 7.4, 150mM NaCl, 3mM MnCl2, 0.1% BSA

      One package contains enough membranes for at least 200 assays (units), where an unit is the amount of membrane that will yield greater than 10-fold signal:background with 125I-labeled NKA at 0.5nM.
      Table 1. Signal:background and specific binding values obtained in a competition binding assay with 10ug/well of NK2 Receptor membrane prep.
      Product Usage Statements
      10 µg/well
      Signal:Background 16.5
      Specific Binding (cpm) 19906
      SPECIFICATIONS: 1 unit = 10.0 µg membrane preparation
      Bmax: 2.21 pmol/mg
      Kd: 0.76 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
      Global Trade Item Number
      Catalogue Number GTIN
      HTS144M 04053252586958