L-168,049

Biological Activity

L-168,049 is a very 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.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Characterization of a novel, non-peptidyl antagonist of the human glucagon receptor.
   Cascieri et al.
   J.Biol.Chem., 1999;274:8694
2. Potent, orally absorbed glucagon receptor antagonists.
   de Laszlo et al.
   Bioorg.Med.Chem.Lett., 1999;9:641
3. Detection of glucagon-dependent GTPgS binding in high-throughput format.
   Dallas-Yang et al.
   Anal.Biochem., 2001;301:156

Product Datasheets