A GCGR antagonist
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L-168,049

Item No. 41112

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[3-(5-bromo-2-propoxyphenyl)-5-(4-chlorophenyl)-1H-pyrrol-2-yl]-pyridine
CAS Number
191034-25-0
Synonyms
  • GCGR Antagonist II
  • Glucagon Receptor Antagonist II
Molecular Formula
C24H20BrClN2O
Formula Weight
467.8
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Soluble: ≥10 mg/ml
SMILES
BrC1=CC=C(OCCC)C(C2=C(C3=CC=NC=C3)NC(C4=CC=C(Cl)C=C4)=C2)=C1
InChi Code
InChI=1S/C24H20BrClN2O/c1-2-13-29-23-8-5-18(25)14-20(23)21-15-22(16-3-6-19(26)7-4-16)28-24(21)17-9-11-27-12-10-17/h3-12,14-15,28H,2,13H2,1H3
InChi Key
HHBOWXZOLYQFNY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    Cayman Chemical
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    Product Description

    L-168,049 is a glucagon receptor (GCGR) antagonist (IC50s = 3.7 and 179 nM in the absence and presence of MgCl2, respectively).1 It prevents glucagon-induced increases in IL-1β and IL-6 levels in, and levels secreted from, HepG2 cells when used at a concentration of 3.7 nM.2 L-168,049 inhibits glucagon-induced increases in the mRNA encoding complement 3 (C3), C-reactive protein (CRP), and fibrinogen in HepG2 cells. In vivo, L-168,049 (1 µM in drinking water) inhibits glucagon-induced increases in the hepatic levels of NOD-like receptor protein 3 (NLRP3), phosphorylated NF-κB, and phosphorylated Stat3 in mice.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cascieri, M.A., Koch, G.E., Ber, E., et al. Characterization of a novel, non-peptidyl antagonist of the human glucagon receptor. The Journal of Biological Chemisty 274(13), 8694-8697 (1999).

    2. Andreozzi , F., Di Fatta, C., Spiga, R., et al. Glucagon induces the hepatic expression of inflammatory markers in vitro and in vivo. Diabetes Obes. Metab. 25(2), 556-569 (2023).