Calcium Flux Assay

HTS131L - ChemiBrite™ IP1 Prostanoid Receptor Stable Cell Line

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HTS131L
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    Prostacyclin (PGI2) is released by vascular endothelial cells and serves as a potent vasodilator, inhibitor of platelet aggregation, and moderator of vascular smooth muscle cell proliferation–migration–differentiation (Narumiya et al. 1999). The function of prostacyclin is mediated via a seven transmembrane GPCR, IP1, which is known to couple to Gs and Gq signaling pathways. Mice lacking the IP1 receptor have shown increased susceptibility to thrombosis (Murata et al. 1997), enhanced injury-induced vascular proliferation and platelet activation (Cheng et al. 2002), as well as reperfusion injury (Xiao et al. 2001). The recent world-wide withdrawal of selective COX-2 inhibitors, rofecoxib (Vioxx™) and valdecoxib (Bextra™) is also due to their discriminating suppression of COX-2-derived prostacyclin and IP1-mediated cardioprotective effects, leading to increased risk of cardiovascular events (Fitzgerald 2004). Eurofins' cloned human IP1 receptor-expressing ChemiBrite cells are made by stable transfection of HEK293 cells with ChemiBrite clytin and IP1 Receptor. These stability tested cells are ready for luminescent analysis of agonists, antagonists and modulators at the IP1 receptor.

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    Item Unit of Measure: PK
    Contents: 2 vials of mycoplasma-free cells, 1 ml per vial.
    Storage: Vials are to be stored in liquid N2.
    Applications: Calcium Flux Assay, cAMP Accumulation
    Entrez Gene Number: NM-000960
    Host Cell: HEK293
    Exogenous Gene Expression: PTGIR cDNA (Accession Number: NM_000960; see CODING SEQUENCE below) and a proprietary mutant clytin photoprotein each expressed in a bicistronic vector
    GMO: This product contains genetically modified organisms.
    Reference 1: 1. Narumiya S, Sugimoto Y and Ushikubi F (1999) Prostanoid receptors: structures, properties, and functions. Physiol. Rev. 79: 1193–1226.
    Reference 2: 2. Murata T, Ushikubi F, Matsuoka T et al. (1997) Altered pain perception and inflammatory response in mice lacking prostacyclin receptor, Nature 388: 678–682.
    Reference 3: 3. Cheng Y, Austin SC, Rocca B et al. (2002) Role of prostacyclin in the cardiovascular response to thromboxane A2. Science 296: 539–541.
    Reference 4: 4. Xiao CH, Hara A, Yuhki KI et al. (2001) Roles of prostaglandin I2 and thromboxane A2 in cardiac ischemiareperfusion injury: a study using mice lacking their respective receptors, Circulation 104: 2210–2215.
    Reference 5: 5. Fitzgerald GA (2004) Coxibs and cardiovascular disease. N. Engl. J. Med. 351: 1709–1711.
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