ChemicalBook--->CAS DataBase List--->438618-32-7

438618-32-7

438618-32-7 Structure

438618-32-7 Structure
IdentificationBack Directory
[Name]

Glucagon Receptor Antagonist I
[CAS]

438618-32-7
[Synonyms]

Glucagon Receptor Antagonist I
N-[3-cyano-6-(2-methylbutan-2-yl)-4,5,6,7-tetrahydro-1-benzothiophen-2-yl]-2-ethylbutanamide
[Molecular Formula]

C20H30N2OS
[MDL Number]

MFCD01920208
[MOL File]

438618-32-7.mol
[Molecular Weight]

346.53
Chemical PropertiesBack Directory
[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)
Hazard InformationBack Directory
[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].
[storage]

Store at -20°C
[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
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