Glucagon Receptor Antagonist I Chemical Properties

Boiling point:

517.8±50.0 °C(Predicted)

Density 

1.07±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO: soluble

form 

White crystalline solid.

pka

13.46±0.40(Predicted)

Glucagon Receptor Antagonist I Usage And Synthesis

Description

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.

Uses

Glucagon receptor antagonist-7 (Compound 1) is an antagonist for hGCGR, that inhibits the binding of 125I-labeled glucagon to the human glucagon receptor (hGCGR) with IC50 of 181 nM. Glucagon receptor antagonist-7 activates glucagon-stimulated adenylyl cyclase with a KDB of 81 nM in CHO cell. Glucagon receptor antagonist-7 inhibits glucagon-mediated glycogenolysis in human hepatocytes, and lowers blood glucose levels[1].

References

[1] Qureshi SA, et al., A novel glucagon receptor antagonist inhibits glucagon-mediated biological effects. Diabetes. 2004 Dec;53(12):3267-73. DOI:10.2337/diabetes.53.12.3267

Glucagon Receptor Antagonist I(438618-32-7)Related Product Information

• Pazopanib
• KU-55933
• Selumetinib
• BML-275
• PLX-4720
• CX-4945
• Fluoxetine hydrochloride
• Alpelisib (BYL719)
• Tubastatin A hydrochloride
• N-[5-[[[5-(1,1-Dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4-piperidinecarboxamide hydrochloride
• BI 2536
• Neratinib
• D-ERYTHRO-SPHINGOSINE