Human LPA1 Lysophosphatidic Acid Receptor Cell Line

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  • LPA-mediated inhibition of intracellular cAMP accumulation. RH7777 cells that stably express the Human EDG2 (LPA1) Receptor (green circles) and untransfected RH7777 cells (black triangles) were exposed to the indicated concentrations of LPA for 20 min at 37oC with 10 µM forskolin and 0.5 mM IBMX. Intracellular cAMP was assayed using the HitHunter kit (DiscoveRx).
  • Reference Compounds (agonist): Lysophosphatidic Acid EC50:  3.6 μM
  • Reference Compounds (antagonist): Ki6425 IC50: 0.12 μM

Human LPA1 Lysophosphatidic Acid Receptor Cell Line

  • Cat.#:
  • A624
  • Lot #:
  • 890

Availability: In stock

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Quick Overview

Human LPA1 Lysophosphatidic Acid Receptor-expressing GPCR (G protein-coupled receptor) stable, replicating cell line.

Background

Lysophosphatidic acid (LPA) is a small, bioactive phospholipid that mediates multiple cellular responses, including proliferation, differentiation, motility, and survival in both normal physiology and disease. The extracellular actions of LPA are mediated primarily through its interaction with five G protein-coupled receptors which include LPA1(EDG2), LPA2(EDG4), LPA3(EDG7), LPA4 (GPR23 or P2Y9) and LPA5 (GPR92). Among them, LPA1 (EDG2) is most widely expressed in normal tissue during growth and development. After LPA stimulation, LPA1 (EDG2) couples to Gi and G12/13 and was reported to play an important role in development of chronic neuroimmune disease and initiation of neuropathic pain.
General Info
Synonyms LPA1, EDG2
Product Description Human LPA1 Lysophosphatidic Acid Receptor-expressing GPCR (G protein-coupled receptor) stable, replicating cell line.
Target Type GPCR
Product Type Replicating Cell Line
Receptor Lysophosphatidic Acid
Sub-Type LPA1
Therapeutic Area cancer, pain & inflammation
Related Services Membrane Preparation, Large-scale Cryopreservation, GPCR Screening
Genbank Accession Number NM_001401
Validated Assay/Platform binding, cAMP
References Inoue, M., et al., (2004) Initiation of neuropathic pain requires lysophosphatidic acid receptor signaling. Nat. Med. 10(7):712-8.
Takuwa, Y., et al (2002) The Edg family G protein-coupled receptors for lysophospholipids: their signaling propert
Host cell RH7777
Mycoplasma Status Negative (MycoAlert Kit)
Growth media DMEM, 10% FBS, 0.5 mg/mL G418
Storage & Packaging
Packaging Cryopreserved cells, 6 million cells per vial
Storage Recommendation liquid nitrogen
Stability 12 passages of continuous culture (6 weeks) at 2 passages/week
Quantity 6 million cells
Representative Screening Information
Cell Line CHO-K1 stably expressing human LPA1 receptor
Screening Assay cAMP assay
Readout cAMP detection kit
Plate Format 384 well
Instrument FlexStation-III
Signal Window 10.93
Z Score 0.64
DMSO Tolerance 0.5% DMSO
Testing Modes agonist, antagonist, PAM
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