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HTS073M ChemiScreen™ Recombinant Human β2 Adrenoceptor

HTS073M
200 units  
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      Tabella delle specifiche principali

      SpeciesHost CellsProtein Target
      Human Chem-2beta 2
      Description
      Catalogue NumberHTS073M
      Brand Family Chemicon®
      Trade Name
      • ChemiScreen
      • Chemicon
      DescriptionChemiScreen™ Recombinant Human β2 Adrenoceptor
      OverviewHuman β2 adrenoceptor
      Background InformationThe endogenous catecholamines epinephrine and norepinephrine have profound effects on smooth muscle activity, cardiac function, carbohydrate and fat metabolism, hormone secretion, neurotransmitter release, and central nervous system actions. These activities are mediated by GPCRs belonging to two subfamilies, the α- and β -adrenergic receptors (Bylund et al., 1994). The β -adrenergic receptors, primarily the β2 subtype, mediate relaxation of smooth muscle in many tissues, and β 2-selective agonists are the preferred drugs for stimulating bronchodilation in the treatment of asthma and chronic obstructive pulmonary disease (Sears and Lotvall, 2005). Activation of the β-adrenergic receptors, primarily the β1 subtype and to a lesser extent the β2 subtype, acutely increases heart rate, cardiac output, and cardiac automaticity, and chronically increases cardiac myocyte apoptosis. As a result, β -adrenergic receptor antagonists (β blockers) are effective in the treatment of congestive heart failure and arrhythmia (Feldman et al., 2005). Chemicon's β2 adrenoceptor 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 β2 adrenoceptor interactions with (-)Iodocyanopindolol (ICYP). The membrane preparations exhibit a Kd of 0.51 nM for [125I]-(-)ICYP. With 5 µg/well β2 Adrenoceptor Membrane Prep and 0.5 nM [125I]-(-)ICYP, a greater than 40-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 40-fold signal:background with 125I-labeled (-)Iodocyanopindolol 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 -80oC.
      Quality LevelMQ100
      Applications
      ApplicationHuman beta 2 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 SummaryThe beta-adrenergic receptor kinase specifically phosphorylates the agonist-occupied form of the beta-adrenergic and related G protein-coupled receptors. Overall, the beta adrenergic receptor kinase 2 has 85% amino acid similarity with beta adrenergic receptor kinase 1, with the protein kinase catalytic domain having 95% similarity. These data suggest the existence of a family of receptor kinases which may serve broadly to regulate receptor function.
      Gene Symbol
      • ADRBK2
      • BARK2
      • GRK3
      • Beta-ARK-2
      • EC 2.7.11.15
      GPCR ClassA
      Host CellsChem-2
      Protein Targetbeta 2
      Target Sub-FamilyAdrenergic
      UniProt Number
      UniProt SummaryFUNCTION: SwissProt: P35626 # Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors.
      SIZE: 688 amino acids; 79710 Da
      SIMILARITY: SwissProt: P35626 ## Belongs to the protein kinase superfamily. AGC Ser/Thr protein kinase family. GPRK subfamily. & Contains 1 AGC-kinase C-terminal domain. & Contains 1 PH domain. & Contains 1 protein kinase domain. & Contains 1 RGS domain.
      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. 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, filtered and stored at 4°C
      Radioligand: [125I]-(-) Iodocyanopindolol (Perkin Elmer # NEX189)
      Wash Buffer: 50 mM Hepes, pH 7.4, 500 mM NaCl, filtered and stored at 4°C.
      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 varying amounts of β2 adrenoceptor membrane prep.
      Product Usage Statements
      10 µg/well 5 µg/well
      Signal:Background 95 103
      Specific Binding (cpm) 51393 58517


      SPECIFICATIONS: 1 unit = 5 µg membrane preparation
      Bmax: 8.5 pmol/mg
      Kd: 0.51 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
      Global Trade Item Number
      Numero di catalogo GTIN
      HTS073M 04053252369414

      Documentation

      ChemiScreen™ Recombinant Human β2 Adrenoceptor MSDS

      Titolo

      Scheda di sicurezza (MSDS) 

      ChemiScreen™ Recombinant Human β2 Adrenoceptor Certificati d'Analisi

      TitoloNumero di lotto
      CHEMISCREENTM MEMBRANE PREPARATION RECOMBINANT HUMAN #946;2 ADRENORECEPTOR RECEPTOR - 2089079 2089079

      Riferimenti bibliografici

      Panoramica dei riferimenti bibliograficiCodice d'identificazione nel Pub Med
      Mechanisms of disease: beta-adrenergic receptors--alterations in signal transduction and pharmacogenomics in heart failure.
      Feldman, David S, et al.
      Nature clinical practice. Cardiovascular medicine, 2: 475-83 (2005)  2004

      Mostra il sommario
      16265588 16265588
      Past, present and future--beta2-adrenoceptor agonists in asthma management.
      Sears, Malcolm R and Lötvall, Jan
      Respiratory medicine, 99: 152-70 (2005)  2004

      Mostra il sommario
      15715182 15715182
      International Union of Pharmacology nomenclature of adrenoceptors
      Bylund, D. B. et al.
      Pharmacol. Rev. , 46(2):121-136 (1994)  1993

      7938162 7938162

      Scheda tecnica

      Titolo
      CHEMISCREENTM MEMBRANE PREPARATION RECOMBINANT HUMAN 2 ADRENORECEPTOR RECEPTOR

      Prodotti e applicazioni correlate

      Linee di prodotti

      Prodotti correlati per: Brand Facete

      Categorie

      Life Science Research > Drug Discovery and Development > GPCR Cell Lines & Assays > GPCR Membrane Preparations
      Life Science Research > Proteins and Enzymes > GPCR Membrane Preparations