Gemigliptin 是一种选择性的，可逆的，竞争性的二肽基肽酶 4 (DPP-4) 抑制剂，对人重组 DPP-4 的IC50=10.3 nM。Gemigliptin具有很强的抗糖基化活性，能够用于晚期糖基化终产物相关的糖尿病并发症的研究。

Gemigliptin is a potent dipeptidyl peptidase-4 (DPP-4) inhibitor(KD : 7.25 nM.)

Gemigliptin attenuated vascular calcification and osteogenic trans-differentiation in vascular smooth muscle cells via multiple steps including downregulation of PiT-1 expression and suppression of reactive oxygen species generation, phospho-PI3K/AKT, and the Wnt signaling pathway[1].Gemigliptin treatment attenuated phosphorylated nuclear factor-κB levels, which had been increased in the UUO kidney as well as in TGF-β-treated cultured renal cells[2].

Using immunohistochemical and Western blot analysis, Quantitated components of the NLRP3 inflammasome in kidneys with and without gemigliptin treatment, and in vitro in human kidney tubular epithelial human renal proximal tubule cells (HK-2) cells, further analyzed the effect of gemigliptin on transforming growth factor-β (TGF-β)-stimulated production of profibrotic proteins[2].

911637-19-9

C18H19F8N5O2

489.36

LC15-0444;吉格列汀酒石酸盐

DMSO:122.5 mg/mL (250.33 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years