Evogliptintartrate是一种高效、口服有效、选择性的DPP-4抑制剂，具有抗糖尿病活性。Evogliptintartrate可用于靶向动脉炎症和动脉粥样硬化的研究。
Evogliptin tartrate is a potent, orally bioavailable and selective dipeptidyl peptidase-4 (DPP-4) inhibitor, with antidiabetic activity. Evogliptin tartrate has potential for anti-atherosclerosis therapy that targets arterial inflammation[1].
Evogliptin tartrate significantly inhibits the TNF-α-mediated induction of ICAM-1 and VCAM-1 expression in a concentration-dependent manner (IC50 = 0.30 and 0.25 μM, respectively)[1].Evogliptin tartrate inhibits the TNF-α-mediated transcriptional activation of ICAM-1 and VCAM-1[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[1]. Cell Viability Assay[1] Cell Line: Endothelial cells
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[1].Evogliptin tartrate inhibits the formation of atherosclerotic lesions by reducing vasoinflammation and increases plaque stability[1]. Animal Model: ApoE-/- mice[1]
[1]. Modulation of Sirt1/NF-κB interaction of evogliptin is attributed to inhibition of vascular inflammatory response leading to attenuation of atherosclerotic plaque formation. Biochem Pharmacol. 2019 Oct;168:452-464.
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