HUMAN RECOMBINANT ETA RECEPTOR
MULTISCREEN™ STABLE CELL LINES
1 vial (2 x 106) frozen cells
Sigma Freezing Medium (C-6164)
Full-length Human EDNRA cDNA (GenBank Accession Number NM_001957.1) with FLAG-tag sequence at the N-terminus
Liquid nitrogen upon receiving
Propagation Medium: DME/F12, 10% FBS, 10 µg/mL puromycin
Stable in culture for minimum of two months
Background: Endothelin is a hormone produced predominantly by endothelial cells that have been recognized to play a significant role in the development of several cardiovascular disease states. Its receptor ETA has been reported in a variety of tissues including placenta, uterus, testis, heart, adrenal gland, lung, kidney, ovary, skin, liver, bladder, large blood vessels, cerebellum, neurons, and meningioma tumor cells. In the vasculature, ETA receptors residing on smooth muscle cells mediate prolonged vasoconstriction. Furthermore, activation of the ETA mediates events that regulate mitogenesis, apoptosis, angiogenesis and metastasis in tumors.
The Multispan ETA receptor cell line expresses EDNRA cDNA that is identical to GenBank NM_001957.1 except for 1 mutation that results in a change in amino acid Leu → Val at position 322, which has been reported as a natural variant.
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 stimulation of intracellular cAMP accumulation upon treatment with ligand, measured with MultiscreenTM TR-FRET cAMP 1.0 No Wash Assay Kit (Multispan MSCM01). Figure 3. Receptor expression on cell surface measured by flow cytometry (FACS) using an anti-FLAG antibody. Thin line: parental cells; thick line: receptor-expressing cells.
Dupuis (2000) Endothelin receptor antagonists and their developing role in cardiovascular therapeutics. Can J Cardiol 16:903-910.
Wu-Wong (2002) Endothelin receptor antagonists as therapeutic agents for cancer. Curr Opin Investig Drugs 3:1234-1239.