HTS037M - ChemiSCREEN™ PAR2 Protease-Activated Receptor Membrane Preparation

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HTS037M
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    The 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). 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 mM for furoyl-LIGRLO in a GTPgS binding assay.  

    Additional Resource :  HTS037M090414 Datasheet

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    Item Unit of Measure: EA
    Quantity: 200 units
    Storage: On receipt of material store at -70°C. Unopened reagent is stable for a minimum of 1 year from date of shipment when stored at recommended storage temperature. Avoid repeat freeze/thaw cycles. For maximum recovery of product, centrifuge original vial
    Applications: GTPγS Binding
    Species: Human PAR2 (Accession number AY336105)
    Host Cell: Chem-1, an adherent mammalian cell line without any endogenous PAR2 expression.
    Reference 1: 1. Cocks TM et al. (1999) A protective role for protease-activated receptors in the airways. Nature 398: 156-60.
    Reference 2: 2. Coelho AM et al. (2003) Proteinase-activated receptor-2: physiological and pathophysiological roles. Curr. Med. Chem. Cardiovasc. Hematol. Agents. 1: 61-72.
    Reference 3: 3. Hansen KK et al. (2005) A major role for proteolytic activity and proteinase-activated receptor-2 in the pathogenesis of infectious colitis. Proc. Natl. Acad. Sci. USA. 102: 8363-8.
    Reference 4: 4. Kawabata et al. (2004) Potent and metabolically stable agonists for protease-activated receptor-2: evaluation of activity in multiple assay systems in vitro and in vivo. J. Pharmacol. Exp. Ther. 309: 1098-1107.
    Reference 5: 5. Lindner JR et al. (2000) Delayed onset of inflammation in protease-activated receptor-2-deficient mice. J. Immunol. 165: 6504-10.
    Reference 6: 6. Macfarlane SR et al. (2001) Proteinase-activated receptors. Pharma. Rev. 53: 245-82.
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