Human EDG1 (S1P1) Lysophospholipid Receptor Cell Line

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  • GTP-g-S response from membranes from cells stably expressing the Edg-1 receptor. Membranes from cells expressing the hEdg-1 receptor were isolated, and stored frozen until used. Membranes were incubated with GTP-g-P35PS and the indicated concentration of sphingosine-1-phosphate then filtered. The amount of GTP-g-P35PS bound to the membranes was measured by liquid scintillation counting. Points are averages of duplicate determinations.
  • S-1-P mediated inhibition of intracellular cAMP accumulation. CHO cells stably expressing the human Edg-1 receptor (green) or untransfected CHO-K1 cells (black) were exposed to the indicated concentrations of S-1-P for 20 min at 37PoPC with 10 µM forskolin and 1 mM IBMX. Intracellular cAMP was assayed using the HitHunter kit (GE Healthcare)
  • Reference Compounds (agonist): Sphingosine-1-phosphate EC50: 56 nM

Human EDG1 (S1P1) Lysophospholipid Receptor Cell Line

  • Cat.#:
  • A623

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Quick Overview

Human Edg-1 (S1P1) Lysophospholipid Receptor-expressing GPCR (G protein-coupled receptor) stable, replicating cell line.

Background

Edg receptors constitute of family of 8 GPCRs (designated as Edg-1 through Edg-8) that can be further sub-classified as sphingosine 1-phosphate receptors (S-1-P) and lysophosphatidic acid (LPA) receptors. The Edg-1 receptor is an S-1-P receptor that is coupled to a variety of intracellular responses via Gi and Go. The Edg-1 receptor was initially cloned as an immediate-early gene induced during differentiation of human endothelial cells, an in vitro model of angiogenesis. It has been shown to play a critical role in regulating cellular proliferation and survival.
General Info
Synonyms S1P1
Product Description Human Edg-1 (S1P1) Lysophospholipid Receptor-expressing GPCR (G protein-coupled receptor) stable, replicating cell line.
Target Type GPCR
Product Type Replicating Cell Line
Receptor Lysophospholipid
Sub-Type EDG1 (S1P1)
Therapeutic Area cancer, vascular
Related Services Membrane Preparation, Large-scale Cryopreservation, GPCR Screening
Genbank Accession Number NM_001400
Validated Assay/Platform binding, cAMP
References Lee, M-J., Brocklyn, J.R., et al. (1998) Sphingosine-1-phosphate as a ligand for the G Protein-Coupled Receptor EDG-1. Science 279: 1552-1555.
Okamoto, H., Takuwa, N. et al., (1998) EDG1 is a Functional Sphingosin-1-phsophate Receptor That is
Host cell CHO-K1
Mycoplasma Status Negative (MycoAlert Kit)
Growth media Ham's F12, 10% FBS, 1% NEAA, 400 µg/mL G418
Storage & Packaging
Packaging Cryopreserved cells, 6 million cells per vial
Storage Recommendation liquid nitrogen
Stability 6 passages
Quantity 6 million cells
Representative Screening Information
Cell Line CHO-K1 stably expressing human S1P1 sphingosine-1-phosphate receptor
Screening Assay cAMP assay
Readout Hit Hunter cAMP kit
Plate Format 384 well
Instrument FlexStation-III
Signal Window 15.70
Z Score 0.75
DMSO Tolerance 0.5% DMSO
Testing Modes agonist, antagonist
Testing Options 16-point minimum, 4-point DRC (n = 4), 8-point DRC (n=3 or 4)
Turnaround Time 2 weeks following receipt of Test Articles
Product Documentation
Specification Sheet  Download PDF Document
Screening Info  Download PDF Document