| Identification | Back 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 Properties | Back 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 Information | Back 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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