References: |
Vildagliptin (LAF-237; NVP-LAF 237) inhibits DPP-4 with IC50 of 2.3 nM.
in vitro: Vildagliptin is an N-substituted glycyl-2-cyanopyrrolidine (figure 2). It is a potent competitive and reversible inhibitor of human and rodent DPP-4 in vitro, with a median inhibitory concentration (IC50) ~2-3 nmol/L. Importantly, vildagliptin inhibits DPP-4 with high specificity relative to other similar peptidases where its IC50 exceeds 200 ?mol/L .
in vivo: Compared to age-, gender-, BMI-matched subjects with normal renal function, the mean AUC of vildagliptin after 14 days in patients with mild, moderate, and severe RI increased by 40%, 71%, and 100%, respectively. The treatment was effective in modulating stress in pancreatic tissue, both by reducing levels of stress markers as well as by increasing activity of SOD and catalase. After analyzing the pancreatic histology, we found that vildagliptin was also able to preserve islets and pancreatic β-cells, especially at the concentration of 5 mg/kg. For the detailed information of Vildagliptin, the solubility of Vildagliptin in water, the solubility of Vildagliptin in DMSO, the solubility of Vildagliptin in PBS buffer, the animal experiment (test) of Vildagliptin, the cell expriment (test) of Vildagliptin, the in vivo, in vitro and clinical trial test of Vildagliptin, the EC50, IC50,and affinity,of Vildagliptin, For the detailed information of Vildagliptin, the solubility of Vildagliptin in water, the solubility of Vildagliptin in DMSO, the solubility of Vildagliptin in PBS buffer, the animal experiment (test) of Vildagliptin, the cell expriment (test) of Vildagliptin, the in vivo, in vitro and clinical trial test of Vildagliptin, the EC50, IC50,and affinity,of Vildagliptin, Please contact DC Chemicals. |