Glucagon hydrochloride

SKU: orb1219518

Description

Glucagon hydrochloride is a peptide hormone, produced by pancreatic α-cells. It activates HNF4α and increases HNF4α phosphorylation. Glucagon hydrochloride stimulates gluconeogenesis.Glucagon stimulates both hepatic kisspeptin1 production and gluconeogenesis. Upon binding to its receptor Gcgr, Glucagon activates cAMP-PKA signaling to stimulate hepatic glucose production (HGP) and cause hyperglycemia. Glucagon (100 nM) increases the phosphorylation of HNF4α. Glucagon (100 nM) represses CYP7A1 mRNA expression in human primary hepatocytes.Glucagon (20 μg/kg) increases glycemia and does not stimulate insulin secretion in ambient-fed mice. High-dose (1 mg/kg) Glucagon lowers glycemia compared with PBS control and stimulates insulin secretion in ambient-fed mice.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 28270-04-4
• MW: 3519.21
• Purity: >98% (HPLC)
• Formula: C₁₅₃H₂₂₅N₄₃O₄₉S.ClH
• SMILES: Cl.CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(O)=O
• Target: glucocorticoid receptor

Bioactivity

• In Vivo:
  Low-dose (20 μg/kg) Glucagon increases glycemia and does not stimulate insulin secretion in ambient-fed mice. High-dose (1 mg/kg) Glucagon lowers glycemia compared with PBS control and stimulates insulin secretion in ambient-fed mice. Animal model: C57BL/6J mice (12-to 24-week-old). Dosage: 20 μg/kg and 1 mg/kg. Administration: Administered by i.p. injection; 45 minutes. Result: Low-dose (20 μg/kg) increased glycemia and did not stimulate insulin secretion. High-dose (1 mg/kg) lowered glycemia and stimulated insulin secretion.
• In Vitro:
  Upon binding to its receptor Gcgr, Glucagon activates cAMP-PKA signaling to stimulate hepatic glucose production (HGP) and cause hyperglycemia. Glucagon stimulates both hepatic kisspeptin1 production and gluconeogenesis. Glucagon (100 nM) represses CYP7A1 mRNA expression in human primary hepatocytes. Glucagon (100 nM) increases phosphorylayion of HNF4α. Western blot analysis. Cell line: Human primary hepatocytes (H1211, HH1215). Concentration: 100 nM. Incubation time: Result: Resulted in a marked increase in the amount of phosphorylated HNF4α.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Porcine glucagon hydrochloride

Quick Database Links

Gene Symbol

glucocorticoid receptor