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).
Soluble in DMSO (5 mg/ml), and methanol (5 mg/ml).
Store at 4° C
212.68° C (Predicted)
517.78° C at 760 mmHg (Predicted)
1.08 g/cm3 (Predicted)
n20D 1.54 (Predicted)
hGCGR interaction with glucagon: IC50 = 181 nM (membranes prepared from CHO-hGCGR); Glucagon receptor: IC50 = 129 nM (human); human cell lines: IC50 = 129 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
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QureshiQureshi, SA. et al. (PubMed 15561959) reported that Glucagon Receptor Antagonist I is capable of blocking glucagon-induced glycogenolysis in a dosage-dependent manner. -SCBT Publication Review
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