Anagliptin is a potent and selective DPP-4 inhibitor(IC50= 3.8 nM) and > 10 fold less potent for DPP-8 and DPP-9.
Anagliptin/利格列汀 细胞实验
Cell Line
Concentration
Treated Time
Description
References
RAW264.7 macrophages
100 µM
10 min
To evaluate the effect of Anagliptin on LPS-stimulated inflammatory responses in macrophages. Results showed Anagliptin significantly reduced the production of TNF-α, MCP-1, and IL-6, and inhibited phosphorylation of p65 and ERK1/2.
J Am Heart Assoc. 2017 Jun 19;6(6):e004777
Anagliptin/利格列汀 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6 J mice
Antigen-induced arthritis (AIA) model
Oral
0.3%
4 and 8 weeks
To evaluate the effect of Anagliptin on RA progression, results showed Anagliptin decreased FABP4 levels in serum and synovial macrophages, alleviating RA symptoms.
Bone Res. 2022 Jun 22;10(1):45.
Sprague Dawley rats
Intracranial aneurysm model
Oral
300 mg/kg
2 to 4 weeks
To evaluate the inhibitory effect of Anagliptin on intracranial aneurysm growth. Results showed Anagliptin significantly reduced aneurysm size, inhibited macrophage infiltration and MCP-1 expression, and decreased phosphorylation of p65.
J Am Heart Assoc. 2017 Jun 19;6(6):e004777
Human
Patients with type 2 diabetic nephropathy
Oral
200 mg/day
Once daily for 24 weeks
To evaluate the effect of Anagliptin on glucose/lipid metabolism and renoprotection. Results showed that Anagliptin significantly reduced urinary albumin to creatinine ratio (UACR) and urinary liver-type fatty acid-binding protein (ULFABP) excretion, but had no significant effect on HbA1c, lipid data, systolic blood pressure, and renal function.
BMJ Open Diabetes Res Care. 2017 Jul 7;5(1):e000391
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