化合物 Evogliptin T61949

Product Introduction
Bioactivity


英文名: Evogliptin

描述: Evogliptin (DA-1229) 是具有口服活性的DPP4抑制剂。Evogliptin 在小鼠模型中具有显著而持久的降糖效果。Evogliptin 通过诱导自噬抑制肝细胞的纤维化和炎症信号的产生。Evogliptin 可用于 2 型糖尿病、慢性肝脏炎症，骨质疏松症及肾功能损害的研究。

体外活性: Evogliptin (2.49 mM; 12 h) efficiently inhibits mDPP4 (membrane DPP4) enzymatic activity in PWM-induced H9 Th1 cells [1]. Evogliptin prevents inflammatory and fibrotic signaling through autophagy induction in primary hepatocytes of ATG7 f/f -Cre + mice [2]. Cell Viability Assay [1] Cell Line: H9 Th1 cells (pokeweed mitogen (PWM)-induced) Concentration: 2.49 mM (1 μg/mL) Incubation Time: 12 h Result: Potently inhibited mDPP4 (membrane DPP4) activity in a dose-dependent manner but did not affect either the cytokine profile or cell viability in PWM-activated CD4 + CD26 + H9 Th1 cells.

体内活性: Evogliptin (100, 300 mg/kg; in animal feedings; single daily for 10 weeks) exhibits antidiabetic effects on HFD/STZ mice and improves glucose intolerance and insulin resistance [3]. Animal Model: Male ICR mice (four-week-old; HFD/STZ mice model) [3]. Dosage: 100, 300 mg/kg Administration: In animal feedings; single daily for 10 weeks Result: Decreased the blood glucose level from the second weekand persisted through the 10-week treatment, when at 300 mg/kg. Significantly reduced HbA1c level when dosage at 300 mg/kg. Significantly decreased 6 h-fasted blood glucose levels in a dose-dependent manner.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途