| Name | Tofogliflozin (hydrate) |
| Description | Tofogliflozin hydrate (CSG-452 hydrate) is a potent and highly specific inhibitor of SGLT2, with an 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, respectively. |
| 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]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | H2O : 0.33 mg/mL (0.82 mM), Sonication is recommended.
DMSO : 90 mg/mL (222.52 mM)
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| Keywords | Tofogliflozin Hydrate | inhibit | CSG 452 Hydrate | CSG 452 | CSG452 | Reactive Oxygen Species | Tofogliflozin (hydrate) | CSG-452 | CSG452 Hydrate | Sodium-dependent glucose cotransporters | CSG-452 Hydrate | SGLT | Tofogliflozin | Inhibitor |
| Inhibitors Related | Imeglimin hydrochloride | Acetylcysteine | L-Ascorbic acid |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Membrane Protein-targeted Compound Library | Drug Repurposing Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
