HTS043M - ChemiScreen™ VPAC1 Receptor Membrane Preparation

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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). VPAC1 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 VPAC1 interactions with VIP. The membrane preparations exhibit a Kd of 1.2 nM for [125I]-VIP. With 5 mg/well VPAC1 Membrane Prep and 1.2 nM [125I]-VIP, a greater than 7-fold signal-to-background ratio is obtained.

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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: Radioligand Binding Assay
    Species: Human VIPR1 cDNA, encoding VPAC1 (Accession number L13288).
    Host Cell: Chem-1, an adherent mammalian cell line without any endogenous VPAC1 expression.
    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.