rat glucagon receptor

GRA Ex-25 (GRA-Ex-25) is an inhibitor of glucagon receptor.

Secretin (33-59), rat (Secretin (rat)) is a classical hormone in the gastrointestinal system and a neuropeptide.

ZP3022 is a dual agonist targeting the glucagon-like peptide 1 receptor (GLP-1R) and cholecystokinin 2 (CCK2) receptor. It selectively enhances cAMP accumulation or ERK phosphorylation in HEK293 cells with GLP-1R or CCK2 receptor expression, compared to ERK phosphorylation in cells with the CCK1 receptor (EC50s: 0.02, 10.3, and >1,000 nM for human receptors, respectively). At 40 nM, ZP3022 promotes proliferation of rat neonatal β-cells in vitro. It also boosts glucose-induced insulin secretion (GSIS) in rat pancreatic islets at 10 and 100 nM concentrations and decreases body weight in rats at 40 nmol/kg doses twice daily. Administered at 100 nmol/kg daily, ZP3022 enhances β-cell and total pancreatic mass and improves glucose tolerance in db/db mice, while reducing food intake but not body weight in these mice.

Skyrin is a natural bis-anthraquinone derivative and receptor-selective glucagon antagonist that inhibits the growth of HeLa, Vero, K562, Raji, Wish, and Calu-1 tumour cell lines.

Pituitary adenylate cyclase-activating peptide (PACAP) (6-27) is a PACAP receptor antagonist with IC50 values of 1,500, 600, and 300 nM, respectively, for rat PAC1, rat VPAC1, and human VPAC2 recombinant receptors expressed in CHO cells. It binds to PACAP receptors on SH-SY5Y and SK-N-MC human neuroblastoma and T47D human breast cancer cells (IC50s = 24.5, 106, and 105 nM, respectively) and inhibits cAMP accumulation induced by PACAP (1-38) (Kis = 457, 102, and 283 nM, respectively, in SH-SY5Y, SK-N-MC, and T47D cells). In vivo, in newborn pigs, PACAP (6-27) (10 μM) inhibits vasodilation of pial arterioles induced by PACAP (1-27) and PACAP (1-38) . It also inhibits PACAP (1-27)-stimulated increases in plasma insulin and glucagon levels and pancreatic venous blood flow in dogs when administered locally to the pancreas at a dose of 500 μg.

GCGR Antagonist 2, a Furan-2-carbohydrazide, serves as an orally active antagonist of the glucagon receptor. It exhibits affinity for the human glucagon receptor (hGluR) with a dissociation constant (Kd) of 2.3 nM and demonstrates inhibitory activity against the rat receptor with a half-maximal inhibitory concentration (IC50) of 0.43 nM. Additionally, this compound effectively prevents glucagon-stimulated glycogenolysis.

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 ag

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 hy

GEP44 is a peptide-biased triple agonist targeting the glucagon-like peptide-1 receptor (GLP-1R), neuropeptide Y1 receptor (Y1-R), and neuropeptide Y2 receptor (Y2-R). It induces GLP-1R-dependent insulin secretion in rat and human islets by offsetting the actions of Y1-R and GLP-1R agonism, controlled by Y1-R antagonists. Additionally, GEP44 enhances glucose uptake in muscle tissue through Y1-R mediation independent of insulin and significantly reduces food intake and body weight in diet-induced obese rat models. GEP44 is utilized in studies related to obesity and type 2 diabetes.