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HTS037M ChemiSCREEN™ Membrane Preparation Recombinant Human PAR2 Protease-Activated Receptor

Human PAR2 GPCR membrane preparation for GTPγS Binding Assays.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
Host Cell: Chem-1 Uni Prot Number: P55085 Entrez Gene Number: AY336105
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HTS037M
200 units  
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      Overview

      Replacement Information

      Key Spec Table

      SpeciesHost CellsProtein Target
      Human Chem-1PAR2
      Description
      Catalogue NumberHTS037M
      Brand Family Chemicon®
      Trade Name
      • ChemiScreen
      • Chemicon
      DescriptionChemiSCREEN™ Membrane Preparation Recombinant Human PAR2 Protease-Activated Receptor
      Overview Human PAR2
      Background InformationThe protease-activated receptor family of GPCRs has a unique mechanism of activation, in which protease cleaves a prodomain to reveal a peptide sequence that functions as a tethered ligand to activate the receptor (Macfarlane et al., 2001). PAR2 is specifically activated by trypsin and mast cell tryptase, and can also be activated by free peptide analogs of the tethered ligand, such as SLIGRL and furoyl-LIGRLO (Coelho et al., 2003; Kawabata et al., 2004). PAR2 is expressed in endothelium, gastrointestinal epithelium, macrophages, eosinophils and nociceptive afferent neurons. Activation of PAR2 in these cells and tissues promotes vasodilation, inflammation, allergy, hyperalgesia and intestinal permeability. Therefore, PAR2 is regarded as an attractive therapeutic target for colitis, asthma, myocardial ischemia/reperfusion injury, and pain (Cocks et al., 1999; Hansen et al., 2005; Lindner et al., 2000; McLean et al., 2002; Vergnolle et al., 2001). Chemicon's PAR2 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 PAR2 interactions with its ligands. The membrane preparations exhibit an EC50 of 1.9 μM for furoyl-LIGRLO in a GTPγS binding assay.
      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 -80oC.
      Quality LevelMQ100
      Applications
      ApplicationHuman PAR2 GPCR membrane preparation for GTPγS Binding Assays.
      Key Applications
      • GTPγS binding
      Application NotesGTPγS Binding Assay.
      Biological Information
      Entrez Gene Number
      Entrez Gene SummaryCoagulation factor II (thrombin) receptor-like 1 (F2RL1) is a member of the large family of 7-transmembrane-region receptors that couple to guanosine-nucleotide-binding proteins. F2RL1 is also a member of the protease-activated receptor family. It is activated by trypsin, but not by thrombin. It is activated by proteolytic cleavage of its extracellular amino terminus. The new amino terminus functions as a tethered ligand and activates the receptor. The F2RL1 gene contains two exons and is widely expressed in human tissues. The predicted protein sequence is 83% identical to the mouse receptor sequence.
      Gene Symbol
      • F2RL1
      • PAR2
      • GPR11
      • PAR-2
      GPCR ClassA
      Host CellsChem-1
      Protein TargetPAR2
      Target Sub-FamilyProtease-activated
      UniProt Number
      UniProt SummaryFUNCTION: SwissProt: P55085 # Receptor for trypsin and trypsin-like enzymes coupled to G proteins that stimulate phosphoinositide hydrolysis. May have a role in the regulation of vascular tone.
      SIZE: 397 amino acids; 44126 Da
      SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein.
      TISSUE SPECIFICITY: Widely expressed in tissues with especially high levels in pancreas, liver, kidney, small intestine, and colon. Moderate expression is detected in many organs, but none in brain or skeletal muscle.
      PTM: A proteolytic cleavage generates a new N-terminus that functions as a tethered ligand.
      SIMILARITY: SwissProt: P55085 ## Belongs to the G-protein coupled receptor 1 family.
      Incubation ConditionsGTPγS ASSAY CONDITIONS: Membranes are permeabilized by addition of saponin to an equal concentration by mass, then mixed with [35S]-GTPγS (final concentration of 0.1 nM) in 20 mM HEPES, pH 7.4/100 mM NaCl/10 mM MgCl2/0.5 μM GDP in a nonbinding 96-well plate. Unlabeled furoyl-LIGRLO is added to the final concentration indicated in Figure 1 (final volume 100 μL), and incubated for 30 min at 30°C. The binding reaction is transferred to an FB filter plate (Millipore MAHF B1H) prewetted with water, and washed 3 times (1 mL per well per wash) with cold 10 mM sodium phosphate, pH 7.4. The plate is dried and counted.
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Quality Assurance1 unit = 5 μg
      EC50 for furoyl-LIGRLO: ~1.9 μM in a GTPγS binding assay
      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 ConditionsStore at –70°C. Product is stable for at least 6 months from the date of receipt when stored as directed. Do not freeze and thaw.
      Packaging Information
      Material Size200 units
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      HTS037M 04053252401442

      Documentation

      ChemiSCREEN™ Membrane Preparation Recombinant Human PAR2 Protease-Activated Receptor SDS

      Title

      Safety Data Sheet (SDS) 

      ChemiSCREEN™ Membrane Preparation Recombinant Human PAR2 Protease-Activated Receptor Certificates of Analysis

      TitleLot Number
      CHEMISCREENTM MEMBRANE PREPARATION SC751424
      CHEMISCREENTM MEMBRANE PREPARATION RECOMBINANT HUMAN PAR2 PROTEASE-ACTIVATED RECEPTOR - 2349733 2349733
      CHEMISCREENTM MEMBRANE PREPARATION RECOMBINANT HUMAN PAR2 PROTEASE-ACTIVATED RECEPTOR - 2060378 2060378

      Data Sheet

      Title
      CHEMISCREEN MEMBRANE PREPARATION RECOMBINANT HUMAN PAR2 PROTEASE-ACTIVATED RECEPTOR - Data Sheet

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