Human GPR40 Free Fatty Acid Receptor Cell Line

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  • Intracellular calcium response from CHO-K1 cells stably expressing human GPR40 receptors. Cells were loaded with Fluo-4NW then stimulated with the indicated concentrations of Eicosatrynoic acid. Calcium responses were recorded on a FlexStation plate reader. Data represent the average +/- standard deviation of triplicate determinations.
  • Reference Compounds (agonist): 5,8,11-Eicosatriynoic EC50:  2.7 μM , CAY10587 EC50:  0.05 μM , GW9508 EC50:  0.08 μM

Human GPR40 Free Fatty Acid Receptor Cell Line

  • Cat.#:
  • A651

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Quick Overview

Human GPR40 Free Fatty Acid Receptor-expressing GPCR (G protein-coupled receptor) stable, replicating cell line.

Background

GPR40 is a member of the free fatty acid G protein coupled receptor family and is activated by saturated and unsaturated carboxylic acids with carbon chain lengths greater than six. Expression analysis shows that GPR40 is specifically expressed in brain and in insulin-producing beta cells in the pancreas. Activation of GPR40 by long-chain fatty acids has been shown to amplify glucose-stimulated insulin secretion, suggesting that GPR40 may represent an important target for drugs that regulate diabetes. GPR40 has also been shown to be overexpressed in breast cancer cells, where it may regulate cell growth.
General Info
Synonyms FFAR1
Product Description Human GPR40 Free Fatty Acid Receptor-expressing GPCR (G protein-coupled receptor) stable, replicating cell line.
Target Type GPCR
Product Type Replicating Cell Line
Receptor Free Fatty Acid
Sub-Type GPR40
Therapeutic Area cancer, metabolic & gastrointestinal
Related Services Membrane Preparation, Large-scale Cryopreservation, GPCR Screening
Genbank Accession Number BC120944.1; no expressed tags
Validated Assay/Platform calcium
References Briscoe, C.P., Tadayyon et al. (2003) The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids. J. Biol. Chem. 278: 11303-11.
Steneberg, P.N., Rubins et al. (2005) The FFA receptor GPR40 links hyperinsulinemia
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 12 passages (6 weeks of continuous culture)
Quantity 6 million cells
Representative Screening Information
Cell Line CHO-K1 stably expressing human FFAR1 Free Fatty Acid Receptor
Screening Assay calcium mobilization assay
Readout calcium sensitive fluorescent dye
Plate Format 384 well
Instrument FlexStation-III
Signal Window 20.23
Z Score 0.81
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