glucagon , human

Glucagon significantly impacts protein and amino acid metabolism. It hinders the integration of amino acids into the proteins of the liver, muscle, and pancreas, augmenting nitrogen excretion and stimulating hepatic urea synthesis. Additionally, it elevates hepatic transaminase and urea cycle enzyme levels. Glucagon also enhances hepatic amino acid uptake, facilitating their conversion into liver glycogen, and reduces blood amino acid concentrations [1].

Glucagon (19-29), human acetate a COOH-terminal fragment processed from glucagon, is a potent and efficient inhibitor of insulin secretion.

Human glucagon-like peptide-1-(7-36)-Lys(Biotin) amide, a biotin-labeled variant of glucagon-like peptide-1-(7-36), is a gastrointestinal peptide known for its antidiabetogenic properties, including enhancing insulin secretion [1] [2].

(Asp28)-Glucagon (1-29) (human, rat, porcine) is an analog of glucagon with an aspartic acid (Asp) substitution at position 28, notably enhancing its aqueous solubility at physiological pH levels while retaining glucagon's innate biological activity [1].

Glucagon-like peptide 1 (1-37), human acetate is a highly potent the GLP-1 receptor agonist.

Glucagon-Like Peptide 1 (GLP-1) (7-36)-Lys (Biotin), amide, human, is a human GLP-1 (7-36) amide biotinylated at the C-terminal.

Glucagon-like peptide 2 (GLP-2) is a recently identified intestinal epithelium-specific growth factor that has been shown to reduce the severity of inflammatory disorders of the intestine in rodent models. Currently Glucagon-Like Peptide 2 is used as a po

Glucagon (1-29), bovine, human, porcine hydrochloride (Porcine glucagon hydrochloride) is a peptide hormone produced by pancreatic α-cells that activates HNF4α, increases HNF4α phosphorylation, and stimulates gluconeogenesis.

(Met(O)27)-Glucagon (1-29) (human, rat, porcine) is a modified glucagon exhibiting the same maximum glucose-synthesizing activity in rat hepatocytes as its native form, but with reduced potency, highlighting the importance of methionine in glucagon's attachment to hepatic receptors [1].

Glucagon-like peptide 1 (1-37), human, is a highly potent agonist of the GLP-1 receptor and a pancreatic hormone synthesized by post-translational processing of proglucagon. Unlike truncated forms of GLP-1, it neither affects food intake in rats nor enhances pancreatic insulin secretion.

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.

Glucagon-like peptide 1 (1-37), human (TFA), is a highly potent agonist of the GLP-1 receptor and is a pancreatic hormone synthesized through post-translational processing of proglucagon.

Biotinyl-Glucagon (1-29), encompassing human, bovine, and porcine versions, is a biotinylated form of glucagon. This peptide hormone, synthesized by the pancreas's α-cells, elevates glucose and fatty acid levels in the bloodstream [1] [2].

Glucagon is a peptide hormone, produced by pancreatic α-cells. Glucagon reduces the activity of HNF-4. Glucagon stimulates gluconeogenesis. Glucagon enhances HNF4α phosphorylation.

GLP-1 secretion by human enteroendocrine NCI-H716 cells is augmented in a dose-dependent manner by the addition of CPE.

GLP-1 (1-36) amide (human, rat) TFA, a variant of GLP-1 (7-36) amide, induces [14C]aminopyrine accumulation in enzymatically dispersed enriched rat parietal cells [1].

GLP-1 (1-36) amide (human, rat) is a molecular variant of the GLP-1 (7-36) amide and has the capacity to stimulate [14C]aminopyrine accumulation in enzymatically dispersed, enriched rat parietal cells [1].

GLP-2(1-33) (human) is an enteroendocrine hormone that stimulates intestinal epithelium growth.

Semaglutide is a glucagon-like peptide 1 receptor (GLP-1R) agonist(EC50 of 6.2 pM in a reporter assay using BHK cells expressing the human receptor).

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

Crotedumab (REGN1193), a fully human IgG4 monoclonal antibody, selectively binds to and inhibits the glucagon receptor (GCGR) with a dissociation constant (K D) of 0.1 nM, making it a potent candidate for diabetes research [1] [2].

GLP-1 amide is a peptide hormone cleaved from proglucagon in the pancreas.1,2 Mice lacking the glucagon receptor (Gcgr-/-) have approximately nine-fold higher levels of total GLP-1 amide, including GLP-1 (1-36) amide and truncated GLP-1 (7-36) amide , in pancreatic tissue compared to wild-type mice.2References1. Schjoldager, B.T., Mortensen, P.E., Christiansen, J., et al. GLP-1 (glucagon-like peptide 1) and truncated GLP-1, fragments of human proglucagon, inhibit gastric acid secretion in humans. Dig. Dis. Sci. 34(5), 703-708 (1989).2. Gelling, R.W., Du, X.Q., Dichmann, D.S., et al. Lower blood glucose, hyperglucagonemia, and pancreatic α cell hyperplasia in glucagon receptor knockout mice. Proc. Natl. Acad. Sci. U.S.A. 100(3), 1438-1443 (2003). GLP-1 amide is a peptide hormone cleaved from proglucagon in the pancreas.1,2 Mice lacking the glucagon receptor (Gcgr-/-) have approximately nine-fold higher levels of total GLP-1 amide, including GLP-1 (1-36) amide and truncated GLP-1 (7-36) amide , in pancreatic tissue compared to wild-type mice.2 References1. Schjoldager, B.T., Mortensen, P.E., Christiansen, J., et al. GLP-1 (glucagon-like peptide 1) and truncated GLP-1, fragments of human proglucagon, inhibit gastric acid secretion in humans. Dig. Dis. Sci. 34(5), 703-708 (1989).2. Gelling, R.W., Du, X.Q., Dichmann, D.S., et al. Lower blood glucose, hyperglucagonemia, and pancreatic α cell hyperplasia in glucagon receptor knockout mice. Proc. Natl. Acad. Sci. U.S.A. 100(3), 1438-1443 (2003).

GRPP (human), a 30-amino-acid peptide derived from Gcg, modestly elevates plasma insulin levels while reducing plasma glucagon concentrations. However, GRPP (human) has no impact on insulin secretion within rat islets [1].

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.

Somatostatin, also known as growth hormone-inhibiting hormone, is a naturally-occurring peptide hormone of 14 or 28 amino acid residues that regulates the endocrine system. It is secreted by the D cells of the islets to inhibit the release of insulin and

Gulgafafusp alfa is a human IgG2κ monoclonal antibody that selectively binds to the glucagon-like peptide 1 receptor (GLP1R) [1].

GLP-1(9-36)amide TFA, a predominant metabolite of glucagon-like peptide-1-(7-36)amide synthesized through dipeptidyl peptidase-4 (DPP-4) activity, functions as an antagonist to the human pancreatic GLP-1 receptor [1] [2].

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).

Albiglutide TFA, a glucagon-like peptide (GLP)-1 mimetic, is a long acting GLP-1 receptor agonist. Albiglutide TFA significantly reduces glycosylated hemoglobin (A1C). Albiglutide TFA can be used for type 2 diabetes (T2D) research. Albiglutide TFA is generated by the genetic fusion of a DPP-4-resistant GLP-1 dimer to human albumin [1] [2] [3] .

PACAP-related peptide (PRP) is an endogenous 29-amino acid peptide that belongs to the secretin/glucagon superfamily of peptides, which includes secretin , glucagon , glucagon-like peptide-1 , GLP-2 , and pituitary adenylate cyclase-activating polypeptide . It is expressed in normal human pancreas and adrenal gland tissue and in some tumors that produce vasoactive intestinal peptide (VIP). PRP (1-29) is secreted by CHO-K1 cells that express human recombinant preproPACAP.

GLP-1R Agonist DMB is an agonist of glucagon-like peptide 1 receptor (GLP-1R; KB = 26.3 nM for the recombinant human receptor).

Retatrutide acetate (LY3437943) is a peptide and triple agonist for the glucagon receptor (GCGR), glucose-dependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R), exhibiting potent inhibitory effects on human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643, and 0.775 nM respectively; it is utilized in obesity research [1].

(Ser8)-GLP-1 (7-36) amide, human, is a glucagon-like peptide-1 amide derived from glucagonogen, a cleavage product of the GLP-1 (1-36) amide peptide. This entero-insulinotropic hormone promotes glucose-dependent insulin secretion from pancreatic β-cells and affects gastrointestinal motility and secretion [1].

L-168049 is a selective and non-competitive antagonist of human glucagon receptor with IC50s of 3.7 nM, 63 nM, and 60 nM for human, murine, and canine, respectively.

NVP-DPP728 is a potent, reversible, nitrile-dependent inhibitor of dipeptidyl peptidase IV (DPP-IV) with an inhibition constant (K i) of 11 nM for human DPP-IV amidolytic activity. By inhibiting the degradation of glucagon-like peptide-1 (GLP-1), NVP-DPP728 enhances insulin release following glucose intake, making it useful for diabetes research [1].

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.

Glucagon receptor antagonist I is a competitive antagonist of the glucagon receptor (GCGR; IC50 = 181 nM). It blocks glucagon-induced glycogenolysis in primary human hepatocytes and isolated liver. Glucagon receptor antagonist I, at 50 mg/kg, reduces the increase in glucose levels observed after intraperitoneal administration of glucagon in humanized mice. Glucagon receptor antagonist inactive control does not prevent glucagon-mediated actions.

Tirzepatide acts as an agonist for both the glucagon-like peptide 1 receptor (GLP-1R) and G protein-coupled receptor 119 (GPR119), effectively inducing cAMP production in HEK293 cells that express either human GLP-1R or GPR119, with EC50 values of 6.54 and 1.01 nM, respectively. Additionally, at a concentration of 100 nM, it triggers receptor internalization in these cells. In vivo studies demonstrate that tirzepatide, administered at 10 nmol/kg per day, significantly reduces body weight, food intake, as well as plasma and hepatic triglyceride levels, free fatty acids (FFAs), leptin, and blood glucose in mice with high-fat diet-induced obesity. Furthermore, a dose of 50 nmol/kg every three days prevents an increase in eosinophils and lymphocytes in the bronchoalveolar lavage fluid (BALF) and inhibits bronchoconstriction prompted by methacholine in mice models of both asthma and diabetes, indicating its potential in treating type 2 diabetes mellitus.

NNC-0640 is a negative allosteric modulator of Human Glucagon Receptor with an IC50 of 69.2 nM.

Amylin, amide, human TFA, a 37-amino acid polypeptide, functions as a pancreatic hormone cosecreted with insulin, playing distinct roles in metabolism and glucose homeostasis by regulating blood sugar through inhibiting glucagon secretion, delaying gastric emptying, and promoting satiety [1].

Oxyntomodulin (human, mouse, rat) (Proglucagon [33-69]) is a 37-amino acid derivative of the glucagon progenitor that includes the entire glucagon sequence plus an additional C-terminal octapeptide.

5(S)-HEPE, an active metabolite of eicosapentaenoic acid (EPA), is produced via the action of 5-lipoxygenase (5-LO). This compound functions as an agonist for G protein-coupled receptor 119 (GPR119), promoting cAMP accumulation in CHO-K1 cells expressing human GPR119 at 10 µM concentration. Additionally, 5(S)-HEPE enhances glucose-stimulated insulin secretion from MING6 insulinoma pancreatic islets and glucagon-like peptide 1 (GLP-1) secretion from HuTu 80 adenocarcinoma cells at the same concentration. Notably, serum levels of 5(S)-HEPE are increased in hyperlipidemia patients.