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.

Skyrin is a fungal metabolite characterized by a bisanthraquinone structure. It interferes with glucagon signaling through adenylate cyclase without binding to the glucagon receptor. At 10 μM, skyrin reduces both glucagon-stimulated cAMP production and glycogenolysis. It does not interfere with epinephrine or glucagon-like peptide 1 effects on these parameters.[1] Reference:[1]. Parker, J.C., McPherson, R.K., Andrews, K.M., et al. Effects of skyrin, a receptor-selective glucagon antagonist, in rat and human hepatocytes. Diabetes 49, 2079-2086 (2012).

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