Product IntroductionBioactivity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