ChemiScreen™ CALCIUM-OPTIMIZED STABLE CELL LINE
HUMAN RECOMBINANT GLUCAGON RECEPTOR

ChemiScreen™ CALCIUM-OPTIMIZED STABLE CELL LINE
HUMAN RECOMBINANT GLUCAGON RECEPTOR

• ChemiScreen
• Chemicon (Millipore)

2 vials

Full-length human GCGR cDNA encoding Glucagon Receptor

Glucagon is a 29-amino acid peptide that stimulates glycogenolysis and gluconeogenesis in the liver to increase blood glucose. The receptor for glucagon is a class 2 (or class B) GPCR that signals through Gs to stimulate cAMP production (Mayo et al., 2003). Mice lacking the glucagon receptor have mild hypoglycemia after fasting, and exhibit hyperplasia of pancreatic alpha-cells (Gelling et al., 2003). Because of its role in promoting hyperglycemia, the glucagon receptor presents a potential target for treatment of diabetes. Chemicon's cloned human Glucagon Receptor-expressing cell line is made in the Chem-1 host, which supports high levels of recombinant Glucagon Receptor expression on the cell surface and contains high levels of the promiscuous G protein Galpha15 to couple the receptor to the calcium signaling pathway. Thus, the cell line is an ideal tool for screening for antagonists of interactions between the Glucagon Receptor and its ligands.

Calcium flux assay, ligand binding assays

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The physiologic effects of glucagon (GCG; MIM 138030) are mediated through the glucagon receptor, a member of the superfamily of receptors characterized by a 7-transmembrane domain structure and by their coupling via GTP-binding proteins (G proteins) to adenyl cyclase.[supplied by OMIM]

FUNCTION: SwissProt: P47871 # This is a receptor for glucagon which plays a central role in regulating the level of blood glucose by controlling the rate of hepatic glucose production and insulin secretion. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase and also a phosphatidylinositol-calcium second messenger system.
SIZE: 477 amino acids; 54009 Da
SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein.
DISEASE:SwissProt: P47871 # It is a candidate for certain defects in non-insulin- dependent diabetes mellitus (NIDDM). The variant in position 40 (Ser) is found in some NIDDM patients, but also in nondiabetic subjects.
SIMILARITY: SwissProt: P47871 ## Belongs to the G-protein coupled receptor 2 family.

Human

EC50 for calcium mobilization by Glucagon: ~ 14.5 nM

Chem-1

GPCR Cell Lines

Chemicon

Chem-1

Cells are frozen at 2 x 10e6 cells/mL in DMEM/20% fetal bovine serum/100 U/ml penicillin and streptomycin/10% DMSO. Cell line tests negative for mycoplasma.

glucagon / GCG

P47871

peptide

Glucagon

Place cells in liquid nitrogen immediately upon receipt. Maintain frozen in liquid nitrogen for up to 5 years. Thaw cells rapidly by removing from liquid nitrogen and immediately immersing in a 37ºC water bath. Immediately after ice has thawed, sterilize the exterior of the vial with 70% ethanol. Transfer contents of the vial to a T75 flask containing 20 mL growth media, and place in a humidified 37°C incubator with 5% CO2.. After 8-24 h, cells will adhere to the plate, at which time the media should be replaced to remove residual DMSO. Cells are passaged by washing with Ca++ and Mg++-free HBSS (10 mL/T75), incubating with 0.05% trypsin/0.2 g/L EDTA (1 mL/T75) for 5-10 minutes at 37°C, and rapping the side of the flask to dislodge the cells. Neutralize the trypsin by addition of 4 volumes growth media. Cells are typically passaged 1:10 with every 3-4 days, and should be passaged at least once after thawing prior to use in calcium flux assays.

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B

1 mL per vial

• GCGR
• MGC138246
• GL-R
• GGR

GPCRs

ChemiScreen™ CALCIUM-OPTIMIZED STABLE CELL LINE
HUMAN RECOMBINANT GLUCAGON RECEPTOR

NM_000160.2

DMEM containing 4.5 g/L glucose/10% heat inactivated fetal bovine serum/1x nonessential amino acids/10 mM HEPES/0.25 mg/ml Geneticin (G418)/100 U/ml each penicillin and streptomycin

2 x 10e6 cells/mL