Calcium Flux Assay

HTS142L - ChemiBrite™ EP4 Prostanoid Receptor Stable Cell Line

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HTS142L
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  • Product Description

    Prostanoids are a series of arachidonic acid metabolites produced by the action of cyclooxygenase and further modified by isomerases and synthases. Cells rapidly secrete prostanoids after synthesis, whereupon the prostanoids bind to a family of 8 GPCRs to exert their biological effects (Narumiya and FitzGerald, 2001). The prostaglandin PGE2 causes pain, vasodilation, immunosuppression of T cells, bone remodeling and promotion of carcinogenesis. Four related GPCRs: EP1, EP2, EP3 and EP4, each bind to PGE2, but the different G protein coupling status of each receptor leads to distinct biological effects. EP4 couples primarily to Gs to increase intracellular cAMP levels. During neonatal development, EP4 participates in closure of the ductus arteriosus, a process required for switching circulation from the placenta to the lungs (Nguyen et al., 1997). In addition, EP4 mediates PGE2-induced bone formation by promoting osteoblastogenesis, and selective EP4 agonists are being evaluated as potential treatments for osteoporosis (Yoshida et al., 2002). Eurofins' cloned EP4 receptor-expressing ChemiBrite cells are made by stable transfection of HEK293 cells with ChemiBrite clytin, EP4 receptor and a promiscuous G protein to couple the receptor to the calcium signaling pathway. These stability tested cells are ready for luminescent analysis of agonists, antagonists and modulators at the EP4 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_000958
    Host Cell: HEK293
    Exogenous Gene Expression: Human PTGER4 cDNA (Accession Number: NM000958; see CODING SEQUENCE below) and a proprietary mutant clytin photoprotein, and promiscuous G protein, each expressed in a bicistronic vector
    GMO: This product contains genetically modified organisms.
    Reference 1: 1. Narumiya S and FitzGerald GA (2001) Genetic and pharmacological analysis of prostanoid receptor function. J. Clin. Invest. 108: 25-30.
    Reference 2: 2. Nguyen M et al. (1997) The prostaglandin receptor EP4 triggers remodelling of the cardiovascular system at birth. Nature 390: 78-81.
    Reference 3: 3. Yoshida K et al. (2002) Stimulation of bone formation and prevention of bone loss by prostaglandin E EP4 receptor activation. Proc. Natl. Acad. Sci. USA 99: 4580-5.
    Reference 4: 4. Wilson R et al (2004) Functional Pharmacology of human prostanoid EP2 and EP4 Receptors, Eur J Pharmacology 501: 49-58
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