Glucagon Receptor
Glucagon is a 29-amino acid polypeptide secreted by the alpha or glucagon cell of the islet of Langerhans in response to hypoglycemia, arginine, gastric inhibitory polypeptide (during ambient reduced glucose levels), gastrin, and potassium chloride. Glucagon action is transduced by a G-protein-coupled receptor (GCGR/Gcgr) that is a member of the class II GCGR superfamily of seven transmembrane spanning receptors that are coupled via GTP-binding proteins to adenyl cyclase resulting in an increase in cAMP production. cAMP activates signaling pathways that cause an increase in gluconeogenesis, glycogenolysis, and fatty acid oxidation. In addition, glucagon controls glucose, energy, and lipid metabolism at least in part via AC/cAMP independent signals including p38MAPK, IP3/DAG/Ca, peroxisome proliferator-activated receptor-α (PPARα) and fibroblast growth factor 21 (FGF21)-dependent pathways. Binding sites for glucagon have been identified in liver, kidney, intestinal smooth muscle, brain, adipose tissue, heart, pancreatic islet beta cells and placenta. Gcgr expression is positively regulated by glucose and negatively regulated by glucagon and agents that increase intracellular cAMP.
References
1.Charron MJ,et al. J Endocrinol. 2015;224(3):R123–R130.
References
1.Charron MJ,et al. J Endocrinol. 2015;224(3):R123–R130.
GPCR/G Protein
ACAT(3)
Angiotensin Receptor(27)
Antibacterial(471)
Bombesin Receptor(11)
Bradykinin Receptor(18)
Calcium Channel(137)
cAMP(9)
Cannabinoid Receptor(69)
CaSR(17)
CGRP Receptor(14)
Chemokine Receptor(104)
Cholecystokinin Receptor(17)
CRF Receptor(13)
Dopamine Receptor(145)
Endothelin Receptor(20)
FFAR(5)
Galanin Receptor(1)
GHSR(16)
Glucagon Receptor(36)
GPCR19(7)
GPR119(3)
Hedgehog (Hh)(27)
Histamine Receptor(110)
Imidazoline Receptor(1)
Leukotriene Receptor(9)
LHR(1)
LPA Receptor(12)
Lysophospholipid Receptor(13)
mAChR(25)
MCHR(6)
Melanocortin Receptor(22)
Melatonin Receptor(5)
mGluR(11)
Motilin Receptor(4)
Neurokinin Receptor(34)
Neuropeptide Y Receptor(36)
Neurotensin Receptor(8)
Orexin Receptor(14)
Other Targets(3)
OXTR(2)
P2Y Receptor(8)
PAR(24)
Platelet-activating Factor Receptor(2)
Prostaglandin Receptor(60)
PTH Receptor(1)
S1P Receptor(22)
SGLT(22)
Somatostatin Receptor(11)
Urotensin Receptor(4)
Vasopressin Receptor(16)
Glucagon Receptor
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Bay 55-9837
catalog no : M30737
cas no: 463930-25-8
Selective VPAC2 receptor agonist (EC50 values are 0.4, 100 and >1000 nM for VPAC2, VPAC1 and PAC1, respectively in a cAMP accumulation assay; IC50 values are 60, 8700 and >10000 nM for VPAC2, VPAC1 and PAC1, respectively in a competition binding assay). Stimulates glucose-dependent insulin secretion in isolated human pancreatic islets. Reduces HIV-1 viral replication and shows cooperative effects when given in conjunction with VPAC1 agonists. -
des-His1-[Glu9]-Glucagon (1-29) amide
catalog no : M30688
cas no: 110084-95-2
Glucagon receptor antagonist (pA2 = 7.2 for inhibition of glucagon-induced adenylyl cyclase activation in rat liver membranes); displays no agonist activity. Enhances glucose-stimulated pancreatic insulin release in vitro. Blocks added glucagon-induced hyperglycemia in normal rabbits without affecting glycogenolysis in vivo. Also blocks endogenous glucagon-induced hyperglycemia in streptozocin diabetic rats. -
Oxyntomodulin (porcine, bovine)
catalog no : M30610
cas no: 62340-29-8
GLP-1 receptor agonist. Endogenous preproglucagon-derived neuropeptide that modulates feeding and metabolism. Also secreted by intestinal L-cells. Increases cAMP production and inhibits gastric acid secretion in rat stomach. Also weak glucagon receptor agonist. -
Glucagon (19-29), human
catalog no : M30561
cas no: 64790-15-4
Glucagon is a 29-amino-acid peptide hormone liberated in the alpha cells of the islets of Langerhans. Glucagon-producing alpha cells represent one of the earliest populations of detectable islet cells in the developing endocrine pancreas. -
HAEGTFTSD
catalog no : M30151
cas no: 926018-45-3
HAEGTFTSD is the first N-terminal 1-9 residues of GLP-1 peptide.The GLP-1 (7-36) amide is a product of the preproglucagon gene, which is secreted from intestinal L-cells, in response to the ingestion of food.