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HTS114M ChemiSCREEN™ Human PAC1-long Receptor Membrane Preparation

Human PAC1 long isoform / PACAP 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-1 Uni Prot Number: P41586 Entrez Gene Number: NM_001118.3
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HTS114M
200 units  
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      Overview

      Replacement Information

      Key Specifications Table

      SpeciesHost CellsProtein Target
      Human Chem-1PAC1 long isoform / PACAP
      Description
      Catalogue NumberHTS114M
      Brand Family Chemicon®
      Trade Name
      • ChemiScreen
      • Chemicon
      DescriptionChemiSCREEN™ Human PAC1-long Receptor Membrane Preparation
      OverviewHuman ADCYAP1R1 cDNA encoding the long isoform of PAC1
      Background InformationPACAP (pituitary adenylyl cyclase-activating peptide) is a peptide that exists in 2 forms, 27 or 38 amino acids, and is related to vasoactive intestinal peptide (VIP). Three related class B GPCRs, PAC1, VPAC1 and VPAC2, bind to PACAP; however, VPAC1 and VPAC2 have a much higher affinity for VIP than does PAC1 (Vaudry et al., 2000). Several splice variants of PAC1 result in proteins that differ at the N-terminus and third intracellular loop; these variants differ in their affinities for PACAP and abilities to activate Gq and Gs. High expression of PAC1 is observed in the CNS and the adrenal medulla. Studies with PAC1-null mice indicate that PAC1 plays important roles in regulation of circadian rhythms, neutrophil migration, and pulmonary vascular tone (Hannibal et al., 2001; Martinez et al., 2005; Otto et al., 2004). Chemicon's PAC1-long 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 PAC1-long interactions with PACAP27. The membrane preparations exhibit a Kd of 2.7 nM for [125I]-PACAP27. With 5 µg/well PAC1-long Membrane Prep and 0.75 nM [125]-PACAP27, a greater than 20-fold signal-to-background ratio was obtained.
      References
      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 were adjusted to the indicated concentration in packaging buffer, rapidly frozen, and stored at -80°C.
      Quality LevelMQ100
      Applications
      ApplicationHuman PAC1 long isoform / PACAP 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 encodes type I adenylate cyclase activating polypeptide receptor, which is a membrane-associated protein and shares significant homology with members of the glucagon/secretin receptor family. This receptor mediates diverse biological actions of adenylate cyclase activating polypeptide 1 and is positively coupled to adenylate cyclase. Alternative splicing of two exons of this gene generates four major splice variants, but their full-length nature has not been determined.
      Gene Symbol
      • ADCYAP1R1
      • PACAPRI
      • PACAP-R-1
      • PACAPR
      GPCR ClassB
      Host CellsChem-1
      Protein TargetPAC1 long isoform / PACAP
      Target Sub-FamilyVIP/PACAP
      UniProt Number
      UniProt SummaryFUNCTION: SwissProt: P41586 # This is a receptor for PACAP-27 and PACAP-38. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase. May regulate the release of adrenocorticotropin, luteinizing hormone, growth hormone, prolactin, epinephrine, and catecholamine. May play a role in spermatogenesis and sperm motility. Causes smooth muscle relaxation and secretion in the gastrointestinal tract.
      SIZE: 468 amino acids; 53314 Da
      SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein.
      TISSUE SPECIFICITY: Most abundant in the brain, low expression in the lung, liver, thymus, spleen, pancreas and placenta.
      SIMILARITY: SwissProt: P41586 ## Belongs to the G-protein coupled receptor 2 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] PACAP27 (Perkin Elmer # NEX294) 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 an unit is the amount of membrane that will yield greater than 20-fold signal:background with 125I-labeled PACAP27 at 0.75 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 PAC1-long membrane prep:
      Product Usage Statements
      10 µg/well 5 µg/well
      Signal:Background 22.9 29
      Specific Binding (cpm) 63650 62987


      SPECIFICATIONS:
      1 unit = 5 µg membrane preparation
      Bmax: 52.0 pmol/mg
      Kd: 2.7 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
      Catalog Number GTIN
      HTS114M 04053252585548

      Documentation

      ChemiSCREEN™ Human PAC1-long Receptor Membrane Preparation SDS

      Title

      Safety Data Sheet (SDS) 

      ChemiSCREEN™ Human PAC1-long Receptor Membrane Preparation Certificates of Analysis

      TitleLot Number
      CHEMISCREENTM MEMBRANE PREPARATION RECOMBINANT HUMAN PAC1-long RECEPTOR - 2093604 2093604

      References

      Reference overviewPub Med ID
      Analysis of the role of the PAC1 receptor in neutrophil recruitment, acute-phase response, and nitric oxide production in septic shock
      Martínez, Carmen, et al
      J Leukoc Biol, 77:729-38 (2005)  2005

      		15661828 15661828
      Pulmonary hypertension and right heart failure in pituitary adenylate cyclase-activating polypeptide type I receptor-deficient mice
      Otto, Christiane, et al
      Circulation, 110:3245-51 (2004)  2004

      		15520307 15520307
      Dissociation between light-induced phase shift of the circadian rhythm and clock gene expression in mice lacking the pituitary adenylate cyclase activating polypeptide type 1 receptor
      Hannibal, J, et al
      J Neurosci, 21:4883-90 (2001)  2001

      		11425915 11425915
      Pituitary adenylate cyclase-activating polypeptide and its receptors: from structure to functions.
      Vaudry, D, et al.
      Pharmacol. Rev., 52: 269-324 (2000)  2000

      Show Abstract       		10835102 10835102

      Data Sheet

      Title
      CHEMISCREENTM MEMBRANE PREPARATION RECOMBINANT HUMAN PAC1-LONG RECEPTOR

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