| Description | Tofogliflozin hydrate (CSG-452 hydrate) is a potent and highly specific inhibitor of SGLT2(IC50 of 2.9 nM and Ki values of 2.9 nM, 14.9 nM, and 6.4 nM for human, rat, and mouse SGLT2). |
| In vitro | Tofogliflozin, a highly selective inhibitor of SGLT2 on oxidative stress generation, inflammatory and proapoptotic reactions in cultured human proximal tubular cells exposed to high glucose.?Tofogliflozin dose-dependently suppressed glucose entry into tubular cells.?High glucose exposure (30 mM) for 4 and 24 h significantly increased oxidative stress generation in tubular cells, which were suppressed by the treatment of tofogliflozin or an antioxidant N-acetylcysteine (NAC).?Monocyte chemoattractant protein-1 (MCP-1) gene expression and apoptotic cell death were induced by 4 h- and 8 day-exposure to high glucose, respectively, both of which were also blocked by tofogliflozin or NAC.?The present study suggests that SGLT2-mediated glucose entry into tubular cells could stimulate oxidative stress and evoke inflammatory and proapoptotic reactions in this cell type.?Blockade of glucose reabsorption in tubular cells by SGLT2 inhibitor might exert beneficial effects on tubulointerstitial damage in diabetic nephropathy[1]. |
| Target activity | SGLT2 (rat):14.9 nM(Ki) , SGLT2:2.9 nM , SGLT2:6.4 nM(Ki), SGLT2 (human):2.9 nM(Ki) |
| Synonyms | 托格列净, Tofogliflozin hydrate, CSG-452 hydrate |
| molecular weight | 404.45 |
| Molecular formula | C22H28O7 |
| CAS | 1201913-82-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: 0.33 mg/mL (0.82 mM), Sonication is recommended. DMSO: 90 mg/mL (222.52 mM) |
| References | 1. Ishibashi Y, et al. Tofogliflozin, A Highly Selective Inhibitor of SGLT2 Blocks Proinflammatory and Proapoptotic Effects of Glucose Overload on Proximal Tubular Cells Partly by Suppressing Oxidative Stress Generation. Horm Metab Res. 2016 Mar;48(3):191-5. 2. Suzuki M, et al. Tofogliflozin, a potent and highly specific sodium/glucose cotransporter 2 inhibitor, improves glycemic control in diabetic rats and mice. J Pharmacol Exp Ther. 2012 Jun;341(3):692-701. |