L-168,049, Tocris Bioscience™

Description

Potent, orally active human glucagon receptor antagonist

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.

Specifications

Chemical Identifiers

• CAS: 191034-25-0
• Molecular Formula: C24H20BrClN2O
• Molecular Weight (g/mol): 467.791
• InChI Key: HHBOWXZOLYQFNY-UHFFFAOYSA-N
• Synonym: glucagon receptor antagonist ii, 4-3-5-bromo-2-propoxyphenyl-5-4-chlorophenyl-1h-pyrrol-2-yl pyridine, 2-4-pyridyl-5-4-chlorophenyl-3-5-bromo-2-propyloxyphenyl pyrrole, d0m3ar, glucagon antagonists diabetes, glucagon antagonists diabetes , merck & co, 4-3-5-bromo-2-propoxy-phenyl-5-4-chloro-phenyl-1h-pyrrol-2-yl-pyridine
• PubChem CID: 5311276
• IUPAC Name: 4-[3-(5-bromo-2-propoxyphenyl)-5-(4-chlorophenyl)-1H-pyrrol-2-yl]pyridine
• SMILES: CCCOC1=C(C=C(C=C1)Br)C2=C(NC(=C2)C3=CC=C(C=C3)Cl)C4=CC=NC=C4

• Quantity: 50 mg
• Formula Weight: 467.79
• Percent Purity: >99%
• Chemical Name or Material: L-168, 049

Safety and Handling

Recommended Storage

Store at Room Temperature