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HTS031M ChemiSCREEN™ CRTH2 Membrane Preparation

Human CRTH2 / DP2 / GPR44 GPCR membrane preparation for Radioligand binding Assays & GTPgammaS binding.

ChemiSCREEN™ CRTH2 Membrane Preparation: SDB (Sicherheitsdatenblätter), Analysenzertifikate und Qualitätszertifikate, Dossiers, Broschüren und andere verfügbare Dokumente.
Host Cell: Chem-1 Uni Prot Number: Q9Y5Y4 Entrez Gene Number: NM_004778.2
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HTS031M
200 units  1 mL
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      Übersicht

      Replacement Information

      Key Spec Table

      SpeciesHost CellsProtein Target
      Human Chem-1CRTH2 / DP2 / GPR44
      Description
      Catalogue NumberHTS031M
      Brand Family Chemicon®
      Trade Name
      • ChemiScreen
      • Chemicon
      DescriptionChemiSCREEN™ CRTH2 Membrane Preparation
      OverviewHuman CRTH2
      Background InformationChemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) is a GPCR related to FPR-like chemoattractant receptors that is highly expressed on Th2 cells, eosinophils, basophils, and type 2 cytotoxic T cells (Nagata et al., 1999). The most potent ligand for CRTH2 is the prostaglandin PGD2, a major mast cell-derived allergic mediator (Hirai et al., 2001). Another GPCR, DP, is activated by PGD2, and the relative contributions of DP and CRTH2 to PGD2-mediated allergic disease are being elucidated. A small molecule antagonist of CRTH2, ramatroban, attenuates PGD2-mediated bronchial hyperresponsiveness and antigen-induced inflammation (Sugimoto et al., 2003; Shichijo et al., 2003).Chemicon's CRTH2 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 PGD2/CRTH2 interactions. The membrane preparations exhibit a Kd of 10 nM for [3H]-Prostaglandin D2. With 2.5 μg/well CRTH2 Membrane Prep and 10 nM [3H]-Prostaglandin D2, a greater than 5-fold signal-to-background ratio is obtained.
      References
      Product Information
      FormatMembranes
      PresentationLiquid in packaging buffer: 50 mM Tris pH 7.4, 10% glycerol and 1% BSA no preservatives.Packaging method: Membranes protein were adjusted to 0.5 mg/ml in 1 ml packaging buffer, rapidly frozen, and stored at -80°C.
      Quality LevelMQ100
      Applications
      ApplicationHuman CRTH2 / DP2 / GPR44 GPCR membrane preparation for Radioligand binding Assays & GTPgammaS binding.
      Key Applications
      • Radioligand binding assay
      • GTPγS binding
      Application NotesRadioligand binding assay, and GTPgammaS binding.
      Biological Information
      Entrez Gene Number
      Entrez Gene SummaryG protein-coupled receptors (GPCRs), such as GPR44, are integral membrane proteins containing 7 putative transmembrane domains (TMs). These proteins mediate signals to the interior of the cell via activation of heterotrimeric G proteins that in turn activate various effector proteins, ultimately resulting in a physiologic response.[supplied by OMIM]
      Gene Symbol
      • GPR44
      • DL1R
      • CRTH2
      • CD294
      GPCR ClassA
      Host CellsChem-1
      Protein TargetCRTH2 / DP2 / GPR44
      Target Sub-FamilyProstanoid
      UniProt Number
      UniProt SummaryFUNCTION: SwissProt: Q9Y5Y4 # Orphan receptor.
      SIZE: 395 amino acids; 43240 Da
      SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein.
      SIMILARITY: SwissProt: Q9Y5Y4 ## 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, 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: 50mM HEPES, 10mM MnCl2, 1mM EDTA, 0.2% BSA, pH to 7.0 and filter.
      Wash buffer: 50mM HEPES, 0.5M NaCl, pH to 7.4 and filter.
      Radioligand: [3H] Prostaglandin D2 (Amersham#: TRK734)
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Table 1. Signal:background and specific binding values obtained in a competition binding assay with CRTH2 membrane preparation with unlabeled Prostaglandin D2.
      Product Usage Statements
      10 µg/well
      Signal:Background 12.2
      Specific Binding (cpm) 4307

      Table 2. IC50 values for ligands obtained in a competition binding assay with CRTH2 membrane preparation.
      IC50 (nM)
      Prostaglanding D2 4.5
      13,14-dihydro-15-keto prostaglandin D2 14.7
      BW A868C 7429


      SPECIFICATIONS: 1 unit = 10 µg
      Bmax: 13.93 pmol/mg
      Kd: 10 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
      Material Package1 mL
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Bestellnummer GTIN
      HTS031M 04053252581724

      Documentation

      Protocols

      Title
      Assembly of a Competition Binding Curve

      ChemiSCREEN™ CRTH2 Membrane Preparation SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

      ÜbersichtPub Med ID
      An orally bioavailable small molecule antagonist of CRTH2, ramatroban (BAY u3405), inhibits prostaglandin D2-induced eosinophil migration in vitro
      Sugimoto, Hiromi, et al
      J Pharmacol Exp Ther, 305:347-52 (2003)  2003

      		12649388 12649388
      Chemoattractant receptor-homologous molecule expressed on Th2 cells activation in vivo increases blood leukocyte counts and its blockade abrogates 13,14-dihydro-15-keto-prostaglandin D2-induced eosinophilia in rats
      Shichijo, Michitaka, et al
      J Pharmacol Exp Ther, 307:518-25 (2003)  2003

      		12975488 12975488
      Prostaglandin D2 selectively induces chemotaxis in T helper type 2 cells, eosinophils, and basophils via seven-transmembrane receptor CRTH2
      Hirai, H, et al
      J Exp Med, 193:255-61 (2001)  2001

      		11208866 11208866
      Prostaglandin D2 as a mediator of allergic asthma
      Matsuoka, T, et al
      Science, 287:2013-7 (2000)  1999

      		10720327 10720327
      Selective expression of a novel surface molecule by human Th2 cells in vivo
      Nagata, K, et al
      J Immunol, 162:1278-86 (1999)  1998

      		9973380 9973380

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      Kategorien

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