HTS043C - ChemiScreen™ Human VPAC1 Receptor Calcium-Optimized Stable Cell Line

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    Vasoactive intestinal peptide (VIP), a 28 amino acid peptide originally isolated by its vasodilation activity, binds to two class B GPCRs, VPAC1 and VPAC2, to exert its functions in the CNS, vasculature, immune system and adrenal medulla (Harmar et al., 1998).  In the immune system, VIP is synthesized by mast cells and lymphocytes, and appears to inhibit inflammation and to shift the immune response toward a Th2 pathway (Delgado et al., 2004).  In the heart, VIP is expressed by nerve fibers, where it modulates heart rate, and coronary blood flow (Henning and Sawmiller, 2001).  The cloned human VPAC1-expressing cell line is made in the Chem-1 host, which supports high levels of recombinant VPAC1 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 VPAC1 and its ligands.

    Additional Resource :  HTS043C060815 Datasheet

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    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
    Host Cell: Chem-1, an adherent cell line expressing the promiscuous G-protein, Gα15.
    Exongenous Gene Expression: Human VPAC1 cDNA (Accession Number: NM_004624- see CODING SEQUENCE below) and promiscuous G protein are expressed in a bicistronic vector
    GMO: This product contains genetically modified organisms.
    Reference 1: 1. Delgado M et al. (2004) The significance of vasoactive intestinal peptide in immunomodulation. Pharmacol. Rev. 56: 249-290.
    Reference 2: 2. Harmar AJ et al. (1998) International Union of Pharmacology. XVIII. Nomenclature of receptors for vasoactive intestinal peptide and pituitary adenylate cyclase-activating polypeptide. Pharmacol. Rev. 50: 265-270.
    Reference 3: 3. Henning RJ and Sawmiller DR (2001) Vasoactive intestinal peptide: cardiovascular effects. Cardiovasc. Res. 49: 27-37.