L-168,049

L-168,049 is a glucagon receptor (GCGR) antagonist (IC50s = 3.7 and 179 nM in the absence and presence of MgCl2, respectively). It prevents glucagon-induced increases in IL-1beta and IL-6 levels in, and levels secreted from, HepG2 cells when used at a concentration of 3.7 nM. 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-kappaB, and phosphorylated Stat3 in mice.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: (Request formulation change), A solid. Solubility: DMSO: Soluble: >10 mg/ml, Ethanol: 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.