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HTS086M ChemiSCREEN™ Human H2 Histamine Receptor Membrane Preparation

Human H2 GPCR membrane preparation for Radioligand binding Assays & GTPγS binding.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
Host Cell: Chem-2 Uni Prot Number: P25021 Entrez Gene Number: NM_022304.1
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HTS086M
200 units  
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      Overview

      Key Spec Table

      SpeciesHost CellsProtein Target
      Human Chem-2H2
      Description
      Catalogue NumberHTS086M
      Brand Family Chemicon®
      Trade Name
      • ChemiScreen
      • Chemicon
      DescriptionChemiSCREEN™ Human H2 Histamine Receptor Membrane Preparation
      OverviewFull-length human HRH2 cDNA encoding H2
      Background InformationThe histamine H2 receptor is a widely distributed G-protein coupled receptor, which is important in regulating a host of physiologic actions extending from gastric acid secretion to gastrointestinal motility (Del Valle and Gantz, 1997). Histamine mediated activation of its receptor leads to signaling through both adenylate cyclase and phosphoinositide /protein kinase C second messenger systems (Hill, 1990). Antagonists for this receptor have proven to be effective therapy for acid peptic disorders of the GI tract. Certain antagonists are used in the treatment of neuropsychiatric and neurological diseases e.g. schizophrenia, Alzheimer's disease and Parkinson's disease. Chemicon's H2 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 agonists and antagonists at H2. The membrane preparations exhibit a Kd of 0.8 nM for [125I]-Iodoaminopotentidine. With 0.65 nM [125I]-Iodoaminopotentidine, 10 µg/well H2 Membrane Prep typically yields greater than 7-fold signal-to-background ratio.
      Product Information
      FormatMembranes
      PresentationOne package contains enough membranes for at least 200 assays (units), where a unit is the amount of membrane that will yield greater than 7-fold signal:background with 125I-labeled Iodoaminopotentidine at 0.65 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 1 mg/mL in packaging buffer, and dispensed at 1 mL/vial. Vials were rapidly frozen, and stored at -80oC.
      Quality LevelMQ100
      Applications
      ApplicationHuman H2 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 SummaryHistamine is a ubiquitous messenger molecule released from mast cells, enterochromaffin-like cells, and neurons. Its various actions are mediated by histamine receptors H1, H2, H3 and H4. Histamine receptor H2 belongs to the family 1 of G protein-coupled receptors. It is an integral membrane protein and stimulates gastric acid secretion. It also regulates gastrointestinal motility and intestinal secretion and is thought to be involved in regulating cell growth and differentiation.
      Gene Symbol
      • HRH2
      • DDX15
      • DBP1
      • H2R
      GPCR ClassA
      Host CellsChem-2
      Protein TargetH2
      Target Sub-FamilyHistamine
      UniProt Number
      UniProt SummaryFUNCTION: SwissProt: P25021 # The H2 subclass of histamine receptors mediates gastric acid secretion. Also appears to regulate gastrointestinal motility and intestinal secretion. Possible role in regulating cell growth and differentiation. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase and, through a separate G protein-dependent mechanism, the phosphoinositide/protein kinase (PKC) signaling pathway (By similarity).
      SIZE: 359 amino acids; 40098 Da
      SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein.
      SIMILARITY: SwissProt: P25021 ## Belongs to the G-protein coupled receptor 1 family.
      MISCELLANEOUS: Antagonists for this receptor have proven to be effective therapy for acid peptic disorders of the gastrointestinal tract. Certain antagonists are used in the treatment of neuropsychiatric and neurological diseases such as schizophrenia, Alzheimer disease and Parkinson disease.
      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, an FC 96-well harvest plate (Millipore cat. # MAHF C1H) 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] Iodoaminopotentidine (Amersham#: IM264)
      Wash Buffer: 50 mM Hepes, pH 7.4, 500mM NaCl , 0.1% BSA, filtered and stored at 4°C.
      Table 1. Signal:background and specific binding values obtained in a competition binding assay with H2 membrane prep and unlabeled tiotidine.
      Product Usage Statements
      10 µg/well
      Signal:Background 11.68
      Specific Binding (cpm) 4152


      SPECIFICATIONS: 1 unit = 10 µg
      Bmax for [125I] Iodoaminopotentidine binding: 0.46 pmol/mg protein
      Kd for [125I] Iodoaminopotentidine binding: ~0.8 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
      HTS086M 04053252470981