HUMAN RECOMBINANT APJ RECEPTOR
MULTISCREEN™ STABLE CELL LINES
1 vial (2 x 106) frozen cells
Sigma Freezing Medium (C-6164)
Expression vector containing full-length human APLNR cDNA (GenBank Accession Number NM_005161) with FLAG tag sequence at N-terminus
Liquid nitrogen upon receiving
Propagation Medium: DMEM-F12, 10% FBS, 10µg/mL puromycin
Stable after minimum of two months continuous growth
Background: APJ (also called AGTRL1, angiotensin II receptor-like 1) is a G- protein-coupled receptor that mediates diverse physiological effects of the neuropeptide apelin. It plays a role in the central and peripheral regulation of the cardiovascular system, in water and food intake, and possibly in immune function. APJ is highly expressed in the cardiovascular system and exerts the hypotensive effect in vivo and plays a counter-regulatory role against the repressor action of angiotensin II. APJ is also found to be a coreceptor for the entry of several HIV-1 and SIV strains, and apelin blocks the entry of HIV-1 and HIV-2.
Application: Functional assays
Figure 1. Dose-dependent stimulation of calcium flux upon treatment with ligand, measured with MultiscreenTM Calcium 1.0 No Wash Assay Kit (Multispan MSCA01). Figure 2. Dose-dependent inhibition of forskolin-stimulated intracellular cAMP level upon treatment with ligand, measured with MultiscreenTM TR-FRET cAMP 1.0 No Wash Assay Kit (Multispan MSCM01).
Cayabyab et al. (2000) Apelin, the natural ligand of the orphan seventransmembrane receptor APJ, inhibits human immunodeficiency virus type 1 entry. J Virol 74:11972- 11976.
Katugampola et al. (2002) Discovery of recently adopted orphan receptors for apelin, urotensin II, and ghrelin identified using novel radioligands and functional role in the human cardiovascular system. Can J Physiol Pharmacol 80:369-374.