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A DPP-4 inhibitor (IC50 0.01 UM) selective for DPP-4 over DPP-8 DPP-9 and FAP- a (IC50s 277.28 233.72 418.43 UM respectively) inhibits DPP-4 activity in isolated human plasma (IC50 11.5 nM) scavenges methylglyoxal in vitro and inhibits AGE formation between BSA and methylglyoxal and cross-linking of AGE-BSA with rat tail tendon collagen (IC50s 1.15 11.69 and 1.39 mM respectively) reduces the levels of circulating AGE and red blood cell IgG content in db/db diabetic mice at 100 mg/kg decreases blood glucose and HbA1c levels and reduces pancreaticBcell damage in a mouse model of STZ- and high-fat diet-induced diabetes induces cytotoxicity in SW1736 and TPC-1 cells
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