HTS068M - ChemiSCREEN™ APJ Apelin Receptor Membrane Preparation

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    Apelin peptides have been discovered to be a family of peptides of different sizes that is derived from the N-terminus of a 77 amino acid precursor peptide (preproapelin) (Hosoya et al., 2000). Apelin receptor (APJ) is a G protein-coupled receptor that is activated by several apelin fragments. APJ activation leads to the inhibition of cAMP production. APJ and apelin peptides have been found to be involved in the regulation of cardiovascular function (Katugampola et al., 2001) and fluid homeostasis (Reaux et al., 2001). Broad roles of apelin system has been established in lowering blood pressure, as a potent cardiac inotrope, in modulating pituitary hormone release and food and water intake, in stress activation, and as a novel adipokine that is excreted from fat cells and regulates insulin (Lee et al., 2006) . APJ 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 agonists and antagonists of APJ. The membrane preparations exhibit a Kd of 0.4 nM for [125I]-Apelin. With 0.25 nM [125I]-Apelin, 5 mg/well APJ Membrane Prep typically yields greater than 20-fold signal-to-background ratio.

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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, GTPγS Binding
    Host Cell: Chem-1, an adherent mammalian cell line without any endogenous apelin expression.
    Reference 1: 1. Hosoya M et al. (2000) Molecular and functional characteristics of APJ: Tissue distribution of mRNA and interaction with the endogenous ligand apelin. J. Biol. Chem. 275: 21061–21067.
    Reference 2: 2. Katugampola SD et al. (2001) [(125)I]-(Pyr(1))Apelin-13 is a novel radioligand for localizing the APJ orphan receptor in human and rat tissues with evidence for a vasoconstrictor role in man. Br. J. Pharmacol. 132: 1255-1260.
    Reference 3: 3. Reaux A et al. (2001) Physiological role of a novel neuropeptide, apelin, and its receptor in the rat brain. J. Neurochem. 77: 1085-1096.
    Reference 4: 4. Lee DK et al. (2006) Unravelling the roles of the apelin system: prospective therapeutic applications in heart failure and obesity. Trends Pharmacol. Sci. 27: 190-194.