Glucagon
Glucagon
Overview
Glucagon is a 29-amino-acid peptide hormone produced by alpha cells of the pancreatic islets of Langerhans that acts as the primary counter-regulatory hormone to insulin. It is FDA-approved for emergency treatment of severe hypoglycemia and as a diagnostic agent in GI imaging. Glucagon is fundamental to understanding glucose homeostasis and serves as a key mechanistic reference for the dual GIP/GLP-1 and glucagon receptor agonist class of metabolic peptides under development. New generation multi-agonist compounds targeting both GLP-1 and glucagon receptors show enhanced fat loss beyond single GLP-1 agonism.
Mechanism of Action
Glucagon acts through the glucagon receptor (GCGR) — a G-protein-coupled receptor coupled to adenylyl cyclase — primarily expressed in the liver. Receptor activation rapidly stimulates glycogenolysis (glycogen breakdown) and gluconeogenesis (new glucose synthesis) in hepatocytes raising blood glucose. Glucagon also stimulates hepatic fatty acid oxidation and ketone body production. In the cardiovascular system glucagon has positive inotropic and chronotropic effects through cardiac GCGR expression. In adipose tissue glucagon stimulates lipolysis contributing to fat mobilization. The opposing actions of insulin and glucagon create the hormonal balance that maintains glucose homeostasis. In obesity and type 2 diabetes glucagon secretion is inappropriately elevated worsening hyperglycemia — suppression of glucagon is one mechanism by which GLP-1 receptor agonists improve glycemic control.
Where does Glucagon sit?
See how this peptide compares across all 85 peptides in our database.
Dosage Information
Typical Dose
1 mg for hypoglycemia emergency
Frequency
As needed for hypoglycemia
Administration
Intramuscular, subcutaneous, or intranasal (Baqsimi)
Notes
Primarily used as emergency treatment for severe hypoglycemia. Intranasal formulation (Baqsimi) available without injection for emergency use. Not used for metabolic optimization — serves as mechanistic reference for multi-agonist peptide therapeutics.
Compound Data
Molecular Formula
C153H225N43O49S
Molecular Weight
3482.70 g/mol
IUPAC Name
(3S)-3-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-5-oxopentanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxypropanoyl]amino]hexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-3-carboxypropanoyl]amino]-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-oxopentanoyl]amino]-4-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(1S,2R)-1-carboxy-2-hydroxypropyl]amino]-1,4-dioxobutan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-oxobutanoic acid
PubChem CID
16132283Potential Side Effects
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Quick Facts
- Administration
- Intramuscular, subcutaneous, or intranasal (Baqsimi)
- Typical Dose
- 1 mg for hypoglycemia emergency
- Frequency
- As needed for hypoglycemia
- References
- 0 curated + 3 from PubMed
- Clinical Trials
- 37 registered
- Evidence Score
- 48.3 / 100