INT-131

INT-131, is a novel, non-thiazolidinedione (TZD), selective peroxisome proliferator-activated receptor (PPAR) gamma modulator, which can be used for the treatment of type 2 diabetes mellitus (non-insulin dependent diabetes) (In Vitro) :AMG131 (INT131) binds to PPARγ and displaces Rosiglitazone with a Ki of ~10 nM, demonstrating ~20-fold higher affinity than either Rosiglitazone or Pioglitazone, and with greater than 1000-fold selectivity for PPARγ over PPARα, PPARδ, or a set of other nuclear receptors. AMG131 is highly selective for PPARγ, with no binding to PPARα or δ at 10 μM, 1000 fold over the Ki for PPARγ. (In Vivo) :AMG131 (INT131; 80 mg/kg; 14-day oral treatment) increases in glucose tolerance in Zucker (fa/fa) rats following.