Date published: 2025-10-15

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Glucagon Receptor Antagonist I (CAS 438618-32-7)

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Alternate Names:
N-(3-Cyano-6-(1,1-dimethylpropyl)-4,5,6,7-tetrahydro-1-benzothien-2-yl)-2-ethylbutanamide; hGCGR Antagonist
Application:
Glucagon Receptor Antagonist I is a potent and selective cell-permeable glucagon receptor antagonist
CAS Number:
438618-32-7
Purity:
>95%
Molecular Weight:
346.5
Molecular Formula:
C20H30N2OS
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Glucagon Receptor Antagonist I is a potent and selective cell-permeable thienyl-amide compound that acts as a competitive antagonist of the glucagon receptor. Exhibits binding to hGCGR with high affinity and prevents its interaction with glucagon (IC50 = 181 nM, KDB = 81 nM, and pA2 = 7.1 in membranes prepared from CHO-hGCGR). Also suppresses glucagon-induced glycogenolysis in human primary hepatocytes and in mice (50 mg/kg, ip).


Glucagon Receptor Antagonist I (CAS 438618-32-7) References

  1. A novel glucagon receptor antagonist inhibits glucagon-mediated biological effects.  |  Qureshi, SA., et al. 2004. Diabetes. 53: 3267-73. PMID: 15561959
  2. Cloning and expression of canine glucagon receptor and its use to evaluate glucagon receptor antagonists in vitro and in vivo.  |  Yang, X., et al. 2007. Eur J Pharmacol. 555: 8-16. PMID: 17140563
  3. Physiology of the pancreatic alpha-cell and glucagon secretion: role in glucose homeostasis and diabetes.  |  Quesada, I., et al. 2008. J Endocrinol. 199: 5-19. PMID: 18669612
  4. YAP/TAZ Inhibition Induces Metabolic and Signaling Rewiring Resulting in Targetable Vulnerabilities in NF2-Deficient Tumor Cells.  |  White, SM., et al. 2019. Dev Cell. 49: 425-443.e9. PMID: 31063758

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Glucagon Receptor Antagonist I, 1 mg

sc-203972
1 mg
$169.00

Glucagon Receptor Antagonist I, 5 mg

sc-203972A
5 mg
$455.00