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Following in vitro tests, compound 57 (Figure 7) was shown to be the most potent DPP-4 inhibitor, with an IC 50 of 0.87 nM

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Specifically, GLP-1RAs reduce SREBP-2 expression via activation of the SIRT6-AMPK pathway, resulting in decreased expression of cholesterol and bile acid synthesis genes, and increased expression of genes associated with RCT and LDL-C uptake

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