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 | |
| Screening Info | |



