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HTS074M ChemiSCREEN™ Human PK1 Prokineticin Receptor Membrane Preparation

Human PK1 / PKR1 GPCR membrane preparation for Radioligand binding Assays & GTPγS binding.

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.
Host Cell: Chem-1 Uni Prot Number: Q8TCW9 Entrez Gene Number: NM_138964.2
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HTS074M
200 units  
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      Aperçu

      Replacement Information

      Tableau de caractéristiques principal

      SpeciesHost CellsProtein Target
      Human Chem-1PK1 / PKR1
      Description
      Catalogue NumberHTS074M
      Brand Family Chemicon®
      Trade Name
      • ChemiScreen
      • Chemicon
      DescriptionChemiSCREEN™ Human PK1 Prokineticin Receptor Membrane Preparation
      OverviewFull-length human GPR73 cDNA, encoding PK1
      Background InformationProkineticins, also known as endocrine gland vascular endothelial growth factors (EG-VEGF), are two ~10 kD secreted proteins originally described to mediate angiogenesis and gastrointestinal smooth muscle contraction (Li et al., 2001; LeCouter et al., 2003). Subsequently, prokineticins have been found to mediate central nervous system functions including circadian rhythms and olfactory bulb development (Cheng et al., 2002; Ng et al., 2005). Two Gq-coupled receptors, PK1 and PK2 (also known as GPR73a and GPR73b), mediate cellular responses to prokineticins (Lin et al., 2002). Chemicon's PK1 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 PK1 interactions and its ligands. The membrane preparations exhibit a Kd of 0.11 nM for [125I]-Mamba Intestinal Toxin-1 (MIT-1). With 0.2 nM [125I]-MIT-1, 2.5 µg/well and 5 µg/well PK1 Membrane Prep typically yield greater than 5-fold signal-to-background ratio.
      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 PK1 / PKR1 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
      Gene Symbol
      • PROKR1
      • PK-R1
      • PKR1
      • GPR73
      • GPR73a
      • ZAQ
      GPCR ClassA
      Host CellsChem-1
      Protein TargetPK1 / PKR1
      Target Sub-FamilyProkineticin
      UniProt Number
      UniProt SummaryFUNCTION: SwissProt: Q8TCW9 # Receptor for prokineticin 1. Exclusively coupled to the G(q) subclass of heteromeric G proteins. Activation leads to mobilization of calcium, stimulation of phosphoinositide turnover and activation of p44/p42 mitogen-activated protein kinase.
      SIZE: 393 amino acids; 44770 Da
      SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein.
      TISSUE SPECIFICITY: Expressed in the stomach, throughout the small intestine, colon, rectum, thyroid gland, pituitary gland, salivary gland, adrenal gland, testis, ovary, brain, spleen, prostate and pancreas.
      SIMILARITY: SwissProt: Q8TCW9 ## 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 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]-MIT-1 (Perkin Elmer#:NEX-410 )
      Wash Buffer: 50 mM Hepes, pH 7.4, 500mM NaCl , 0.1% BSA, filtered and stored at 4°C.
      One package contains enough membranes for at least 200 assays (units), where a unit is the amount of membrane that will yield greater than 10-fold signal:background with 125I-labeled MIT-1 at 0.2 nM
      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 PK1 membrane prep:
      Product Usage Statements
      5 µg/well 2.5 µg/well
      Signal:Background 6 6.4
      Specific Binding (cpm) 3166 1798


      SPECIFICATIONS: 1 unit = 5 µg
      Bmax for [125I] MIT-1 binding: 0.58 pmol/mg protein;
      Kd for [125I] MIT-1 binding: ~ 0.11 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
      Référence GTIN
      HTS074M 04053252326592

      Documentation

      ChemiSCREEN™ Human PK1 Prokineticin Receptor Membrane Preparation FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographiqueNº PubMed
      Dependence of olfactory bulb neurogenesis on prokineticin 2 signaling
      Ng, Kwan L, et al
      Science, 308:1923-7 (2005)  2004

      		15976302 15976302
      Prokineticin 2 transmits the behavioural circadian rhythm of the suprachiasmatic nucleus.
      Cheng, Michelle Y, et al.
      Nature, 417: 405-10 (2002)  2002

      Afficher le résumé       		12024206 12024206
      Endocrine gland-derived VEGF and the emerging hypothesis of organ-specific regulation of angiogenesis.
      LeCouter, Jennifer, et al.
      Nat. Med., 8: 913-7 (2002)  2002

      Afficher le résumé       		12205443 12205443

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      Catégories

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