Evogliptin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效、长效、可逆、竞争性 DPP-4 抑制剂，IC50 为 0.9 nM。

A potent, long acting, reversible and competitive DPP-4 inhibitor with IC50 of 0.9 nM; displays >600-fold selectivity over DPP8 and DPP9; increases levels of plasma GLP-1 and insulin, and lowers blood glucose levels in mice (0.1-3 mg/kg).Diabetes Approved

Evogliptin (2.49 mM; 12 h) efficiently inhibits mDPP4 (membrane DPP4) enzymatic activity in PWM-induced H9 Th1 cells.Evogliptin prevents inflammatory and fibrotic signaling through autophagy induction in primary hepatocytes of ATG7f/f-Cre+ mice. Cell Viability Assay 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.

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. Animal Model:Male ICR mice (four-week-old; HFD/STZ mice model).Dosage:100, 300 mg/kg Administration:In animal feedings; single daily for 10 weeksResult: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.

DA-1229 | DA1229

Metabolic Enzyme/Protease

DPP

DPP

Metabolic Disease

Diabetes

1222102-29-5

401.43

C19H26F3N3O3

>98% (HPLC)

——

CC(C)(C)OCC1C(=O)NCCN1C(=O)CC(CC2=CC(=C(C=C2F)F)F)N

(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-[(2-methylpropan-2-yl)oxymethyl]piperazin-2-one

(-20℃)

With Ice Pack

≥ 2 years