1415407-45-2

Upstream product

• 100791-00-2 4-chloronicotinoyl chloride 
• 1940-42-7 4-bromo-2,5-dichlorophenol 
• 37831-62-2 ethyl 4-chloronicotinate 
• 10177-29-4 4-chloronicotinic acid 

Downstream Products

• 1315469-60-3 4-(4-bromo-2,5-dichloro-phenoxy)-nicotinic acid 
• 1315468-79-1 [4-(2,5-dichloro-4-bromophenoxy)pyridin-3-yl]-(4-cyclopropyl-3,4-dihydro-2H-quinoxalin-1-yl)methanone 
• 1415407-63-4 C₂₄H₂₁Cl₂N₃O₂ 
• 1415407-64-5 C₂₅H₂₃Cl₂N₃O₂ 

Relevant academic research and scientific papers

Discovery of intestinal targeted TGR5 agonists for the treatment of type 2 diabetes

Activation of TGR5 stimulates intestinal glucagon-like peptide-1 (GLP-1) release, but activation of the receptors in gallbladder and heart has been shown to cause severe on-target side effects. A series of low-absorbed TGR5 agonists was prepared by modify

Design, synthesis, and antidiabetic activity of 4-phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists

4-Phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists are reported. Several 4-phenoxynicotinamide derivatives were found to activate human and mouse TGR5 (hTGR5 and mTGR5) with EC50 values in the low nanomolar range. Compound 23g, with an EC50 value of 0.72 nM on hTGR5 and an EC 50 value of 6.2 nM on mTGR5, was selected for further in vivo efficacy studies. This compound exhibited a significant dose-dependent glucagon-like peptide-1 (GLP-1) secretion effect. A single oral dose of 23g (50 mg/kg) significantly reduced blood glucose levels in db/db mice and caused a 49% reduction in the area under the blood glucose curve (AUC)0-120min following an oral glucose tolerance test (OGTT) in imprinting control region (ICR) mice. However, 23g stimulated gallbladder filling, which might result in side effects to the gallbladder.