| Description | Gemigliptin (LC15-0444) is a potent dipeptidyl peptidase-4 (DPP-4) inhibitor(KD : 7.25 nM.) |
| In vitro | 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]. |
| Cell experiments | 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]. |
| Target activity | DPP4:7.25 nM(KD) |
| Synonyms | 吉格列汀酒石酸盐, LC15-0444 |
| molecular weight | 489.36 |
| Molecular formula | C18H19F8N5O2 |
| CAS | 911637-19-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 122.5 mg/mL (250.33 mM) |
| References | 1. Choi S Y , Ryu H M , Oh E J , et al. Dipeptidyl peptidase-4 inhibitor gemigliptin protects against vascular calcification in an experimental chronic kidney disease and vascular smooth muscle cells[J]. PLoS ONE, 2017, 12(7):e0180393. 2. Jung, Beom, Seo, et al. Gemigliptin Attenuates Renal Fibrosis Through Down-Regulation of the NLRP3 Inflammasome.[J]. Diabetes & metabolism journal, 2019. |