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.
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.
Complete Your Research
Complete Your Experiment
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
No product specific FAQs exist for this product, however you mayView all Small Molecule FAQs
VersaClone cDNA Plasmids
Reviews for L-168,049
There are currently no reviews for this product. Be the first to review L-168,049 and earn rewards!
Have you used L-168,049?
Submit a review and receive an Amazon gift card.
$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image