INT131

INT131 is a potent, orally administered non-thiazolidinedione (non-TZD) selective peroxisome proliferator-activated receptor gamma (PPARγ) modulator (SPPARM). It was developed as a second-generation SPPARM to treat type 2 diabetes mellitus by improving insulin sensitivity and lowering blood glucose. Unlike traditional TZD PPARγ full agonists such as rosiglitazone and pioglitazone, INT131 is structurally distinct and designed to retain antidiabetic efficacy while minimizing side effects like weight gain and fluid retention. Mechanistically, INT131 binds with high affinity to the PPARγ ligand-binding domain but occupies a unique area in the pocket compared to TZDs. This results in selective modulation of gene expression related to glucose metabolism and adipocyte function. Preclinical studies and phase II clinical trials have shown that INT131 improves glycemic control with less risk of edema or weight gain than standard TZDs[1][5][7].

Other names

INT131 besylateINT-131 besylateINT 131 besylate