HTS037RTA - Ready-to-Assay™ PAR2 Protease-Activated Receptor Frozen Cells

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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). Cloned human PAR2-expressing cell line is made in the Chem-1 host, which supports high levels of recombinant PAR2 expression on the cell surface and contains high levels of the promiscuous G protein Gα15 to couple the receptor to the calcium signaling pathway. Thus, the cell line is an ideal tool for screening for antagonists of interactions between PAR2 and its ligands

    Additional Resource :  HTS037RTA100614 Datasheet

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    Item Unit of Measure: PK
    Contents: Pack contains 2 vials of mycoplasma-free cells, 1 ml per vial. Fifty (50) mL of Media Component.
    Storage: Vials are to be stored in liquid N2. Media Component at 4ºC (-20ºC for prolonged storage).
    Applications: Calcium Flux Assay
    Host Cell: Chem-1, an adherent rat hematopoietic cell line expressing endogenous Gα15 protein
    GMO: This product contains genetically modified organisms.