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DPP-4
Evogliptin tartrate significantly inhibits the TNF-α-mediated induction of ICAM-1 and VCAM-1 expression in a concentration-dependent manner (IC
50
= 0.30 and 0.25 μM, respectively).
Evogliptin tartrate inhibits the TNF-α-mediated transcriptional activation of ICAM-1 and VCAM-1.
Evogliptin tartrate inhibits inflammatory responses via suppression of adhesion molecules induced by TNF-α. And TNF-α-mediated activation of NF-κB is ameliorated by evogliptin via the interaction of NF-κB with SIRT1.
Cell Viability Assay
Cell Line: | Endothelial cells |
Concentration: | 0.1 μM, 0.3 μM, 1 μM, 3 μM |
Incubation Time: | 12 hours |
Result: | Inhibits TNF-α-mediated (10 ng/ml) expression of adhesion molecules. |
Evogliptin tartrate (37.5-150 mg/kg; p.o.; daily; for 12 weeks) reduces the high-fat diet-induced atherosclerotic plaque area in the ApoE
?/?
mouse model.
Evogliptin tartrate inhibits the formation of atherosclerotic lesions by reducing vasoinflammation and increases plaque stability.
Animal Model: | ApoE ?/? mice |
Dosage: | 37.5 mg/kg, 75 mg/kg, 150 mg/kg |
Administration: | Oral administration; daily; for 12 weeks |
Result: | Inhibit the development of atherosclerosis. |