TM-N1324

TM-N1324 (also known as Cpd1324 or Compound 1324) is a potent, selective, and orally active small molecule agonist of G-protein coupled receptor 39 (GPR39), a zinc-sensing receptor belonging to the ghrelin receptor family. Developed by researchers at the University of Copenhagen, TM-N1324 activates human GPR39 with high efficacy, exhibiting potencies of 280 nM and 9 nM in the absence and presence of zinc, respectively. It has been widely utilized as a chemical probe to investigate the physiological roles of GPR39. Studies have demonstrated that TM-N1324 stimulates the secretion of glucagon-like peptide-1 (GLP-1) and somatostatin, reduces food intake and body weight in mouse models of obesity, and protects against metabolic dysfunction-associated steatotic liver disease (MASLD) and metabolic dysfunction-associated steatohepatitis (MASH). Additionally, GPR39 activation by TM-N1324 in the kidney has been shown to alter cytoskeleton integrity, impair aquaporin-2 (AQP2) trafficking, and induce diuresis.

Other names

4-(2-chloro-4-fluorophenyl)-1,4,5,7-tetrahydro-3-methyl-1-(9H-purin-6-yl)-6H-pyrazolo[3,4-b]pyridin-6-one