L-168,049

Catalog # Availability Size / Price Qty
2311/10
2311/50
Glucagon Receptor Antagonists Small Molecule
1 Image
Description: Potent, orally active human glucagon receptor antagonist

Chemical Name: 4-[3-(5-Bromo-2-propoxyphenyl)-5-(4-chlorophenyl)-1H-pyrrol-2-yl]pyridine

Purity: ≥99%

Product Details
Citations (1)
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Biological Activity

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

M.Wt:
467.79
Formula:
C24H20BrClN2O
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
≥99%
Storage:
Store at RT
CAS No:
191034-25-0

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

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Citation for L-168,049

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