Human GPR103 Receptor Cell Line

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  • CHO-K1 cells that stably express the GPR103 receptor were loaded with Fluo4NW, then stimulated with the indicated concentrations of QRFP-26. The resulting increase in intracellular calcium was measured on a FlexStation fluorescent plate reader. Data points represent the average of triplicate determinations; error bars represent +/- standard deviation.
  • Reference Compounds (agonist): QRFP-26  EC50:  99.5 pM

Human GPR103 Receptor Cell Line

  • Cat.#:
  • A646

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Quick Overview

Human GPR103 Receptor-expressing GPCR (G protein-coupled receptor) stable, replicating cell line.

Background

GPR103 is a G-protein coupled receptor that has been shown to be expressed primarily in brain, heart, kidney, adrenal gland, retina and testis. Its ligand has been identified as a 43-residue RF-amide peptide known as QRFP. When administered centrally in mice, QRFP was shown to increase feeding, behavioral arousal and blood pressure. When administered iv, this peptide caused release of aldosterone. Knockout mice (GPR103 -/-) have suggested a role of GPR103 in regulating bone formation. These diverse but important physiological functions of this receptor and ligand make them important possible targets for drug discovery in several fields.
General Info
Synonyms SP9155, AQ27
Product Description Human GPR103 Receptor-expressing GPCR (G protein-coupled receptor) stable, replicating cell line.
Target Type GPCR
Product Type Replicating Cell Line
Receptor RFamide peptide
Sub-Type GPR103
Therapeutic Area metabolic & gastrointestinal
Related Services Membrane Preparation, Large-scale Cryopreservation, GPCR Screening
Genbank Accession Number AF411117
Validated Assay/Platform calcium
References Jiang, Y., Luo, L., et al., (2003) Identification and Charcterization of a Novel RF-amide Peptide Ligand for Orphan G-protein-coupled Receptor SP9155. J. Biol. Chem. 278: 27652-27657.
Takayasu, S., Sakurai, T., et al., (2006) A neuropeptide ligand
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 At least 6 passages
Quantity 6 million cells
Representative Screening Information
Cell Line CHO-K1 stably expressing human GPR103 QRFP receptor
Screening Assay calcium mobilization assay
Readout calcium sensitive fluorescent dye
Plate Format 384 well
Instrument FlexStation-III
Signal Window 22.00
Z Score 0.85
DMSO Tolerance 1.0% 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