Glucagon

Category: peptide

Aliases: GlucaGen, Baqsimi (intranasal)

Pharmacological Mechanism

29-residue counter-regulatory hormone from pancreatic α-cells. Activates GcgR (Gs-coupled → cAMP) primarily on hepatocytes → glycogenolysis + gluconeogenesis → rapid glucose rise. Also has minor effects on lipolysis. Rescue agent for severe insulin-induced hypoglycemia when glucose cannot be given orally.

Half-Life (t½)

IV: 0.07h

Dosing Guidelines

• IV: Typical 1 mg (Range: 1–1 mg)
• IM: Typical 1 mg (Range: 1–1 mg)
• SC: Typical 1 mg (Range: 1–1 mg)
• IN: Typical 1 mg (Range: 1–1 mg)

Target Organ Systems

• endocrine
• digestive

Pathways It Modulates

• cAMP / PKA second-messenger signaling (activator) — glucagon receptor (Gs)
• GI endocrine peptides (activator) — glucagon receptor (GCGR)

Chemical Identifiers

• PubChem CID: 16132283
• Formula: C153H225N43O49S
• Molecular weight: 3482.7 g/mol
• InChIKey: MASNOZXLGMXCHN-ZLPAWPGGSA-N
• SMILES: C[C@H]([C@@H](C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC2=CC=C(C=C2)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC3=CC=C(C=C3)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC4=CC=CC=C4)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC5=CNC6=CC=CC=C65)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H]([C@@H](C)O)C(=O)O)NC(=O)CNC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC7=CN=CN7)N)O

References

• PMID 773949