Chemical Name: 4-[3-(5-Bromo-2-propoxyphenyl)-5-(4-chlorophenyl)-1H-pyrrol-2-yl]pyridine
Biological ActivityL-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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Characterization of a novel, non-peptidyl antagonist of the human glucagon receptor.
Cascieri et al.
Potent, orally absorbed glucagon receptor antagonists.
de Laszlo et al.
Detection of glucagon-dependent GTPgS binding in high-throughput format.
Dallas-Yang et al.
Citation for L-168,049
The citations listed below are publications that use Tocris products. Selected citations for L-168,049 include:
1 Citation: Showing 1 - 1
Paracrine Interactions within the Pancreatic Islet Determine the Glycemic Set Point.
Authors: Rodriguez-Diaz Et al.
Cell Metab 2018;27:549
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