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  • An inhibitor of the protein tyrosine phosphatase 1B (PTP1B) and dual peroxisome proliferator-activated receptor (PPAR) alpha and gamma agonist with hypoglycemic and anti-lipidemic activity. Ertiprotafib inhibits PTP1B preventing the dephosphorylation of the insulin receptor, which improves insulin sensitivity and decreases blood glucose levels. In addition, this agent is able to stimulate both PPAR alpha and gamma thereby further improving glucose homeostasis and reducing triglyceride (TG) and free fatty acid levels. Ertiprotafib was also shown to be a potent inhibitor of IkappaB kinase beta (IKKbeta), which cotributes to its anti-inflammatory properties.
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