Evogliptin Tartrate

生物活性靶点体外研究体内研究 Evogliptin Tartrate 试剂级价格

Evogliptin Tartrate

CAS号:1222102-51-3
英文名:Evogliptin Tartrate
中文名:Evogliptin Tartrate
CBNumber:CB15984681
分子式:C19H26F3N3O3 · (C4H6O6)
分子量:551.52
MOL File:1222102-51-3.mol

Evogliptin Tartrate化学性质

储存条件 :Store at -20°C
溶解度 :DMSO: 100 mg/mL (181.32 mM)
形态 :Solid
颜色 :White to off-white

Evogliptin Tartrate性质、用途与生产工艺

生物活性 Evogliptin tartrate 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。Evogliptin tartrate 可用于靶向动脉炎症和动脉粥样硬化的研究。
靶点

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 (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.

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.