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.
IC50&Target
DPP-4
体外研究
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).
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.
体内研究
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.
分子式
C23H32F3N3O9
分子量
551.51
CAS号
1222102-51-3
运输条件
Room temperature in continental US; may vary elsewhere.