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BLX-1117 is an amino acid-conjugated small molecule (molecular weight < 500 Da) developed as an oral anti-diabetic agent. Unlike traditional thiazolidinediones (TZDs) such as rosiglitazone, BLX-1117 does not exhibit affinity for peroxisome proliferator-activated receptor gamma (PPARγ) and does not stimulate adipogenesis in 3T3-L1 fibroblasts. In vitro studies have demonstrated that BLX-1117 is non-toxic to human liver (HepG2) cells and effectively stimulates glucose uptake in 3T3-L1 adipocytes, suggesting a novel PPARγ-independent mechanism of action for the treatment of type 2 diabetes.
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