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1222102-51-3

中文名称 Evogliptin Tartrate
英文名称 Evogliptin Tartrate
CAS 1222102-51-3
分子式 C23H32F3N3O9
分子量 551.52
MOL 文件 1222102-51-3.mol
1222102-51-3 结构式 1222102-51-3 结构式

基本信息

中文别名
化合物 T11248
英文别名
DA-1229 tartrate
Evogliptin Tartrate

物理化学性质

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

常见问题列表

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.
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