Evogliptin

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Evogliptin

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1222102-29-5

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品名称

DA-1229

产品介绍

Evogliptin (DA-1229) 是一种口服有效的DPP4抑制剂，在小鼠模型中具有显著而持久的降糖效果。Evogliptin 还可通过诱导自噬来抑制肝细胞的炎症和纤维化信号的产生。Evogliptin 可用于 2 型糖尿病、骨质疏松症，肾功能损害以及慢性肝脏炎症的研究。

生物活性

Evogliptin (DA-1229) is an orally activeDPP4inhibitor with significant and sustained hypoglycaemic effects in mouse models. Evogliptin also inhibits the production of inflammatory and fibrotic signals in hepatocytes by inducingautophagy. Evogliptin can be used in studies of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammation^[1]^[2]^[3]^[4].

IC₅₀& Target

DPP4^[1]^[2]^[3]^[4].

体外研究
(In Vitro)

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.

体内研究
(In Vivo)

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.

Clinical Trial

分子量

401.42

Formula

C₁₉H₂₆F₃N₃O₃

CAS 号

1222102-29-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.