GW1929

GW1929 is a potent, non-thiazolidinedione, tyrosine-based agonist of the peroxisome proliferator-activated receptor gamma (PPARγ). Developed by Glaxo Wellcome (now GSK), it acts as an insulin sensitizer, effectively lowering blood glucose, free fatty acids, and triglycerides in animal models of type 2 diabetes, such as Zucker diabetic fatty rats. Its mechanism involves the regulation of gene expression across multiple insulin-sensitive tissues, including the stimulation of lipogenic genes in adipose tissue and the downregulation of pyruvate dehydrogenase kinase 4 (PDK4) in skeletal muscle, which enhances oxidative glucose metabolism. While it demonstrated significant efficacy in preclinical metabolic studies, it is primarily utilized today as a high-affinity pharmacological tool in research.

Other names

N-(2-benzoylphenyl)-O-[2-(methyl-2-pyridinylamino)ethyl]-L-tyrosine