Cat. No. 2311
Chemical Name: 4-[3-(5-Bromo-2-propoxyphenyl)-5-(4
Biological ActivityVery potent and selective, non-competitive antagonist of the human glucagon receptor (hGR). Binds with high affinity to human GR (IC50 = 3.7 nM), and moderate affinity to murine and canine GRs (IC50 values are 63 and 60 nM respectively). In contrast, displays poor affinity for rat, guinea pig, and rabbit glucagon receptors (IC50 > 1 μM). In functional studies, inhibits glucagon-stimulated cAMP synthesis in CHO cells expressing hGR (IC50 = 41 nM), and in murine liver membranes. Orally active in vivo.
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All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Dallas-Yang et al (2001) Detection of glucagon-dependent GTPgS binding in high-throughput format. Anal.Biochem. 301 156.
Cascieri et al (1999) Characterization of a novel, non-peptidyl antagonist of the human glucagon receptor. J.Biol.Chem. 274 8694. PMID: 10085108.
de Laszlo et al (1999) Potent, orally absorbed glucagon receptor antagonists. Bioorg.Med.Chem.Lett. 9 641. PMID: 10201821.
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