| 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 | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : 0.33 mg/mL (0.82 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (8.16 mM), Sonication is recommended.
DMSO : 142.8 mg/mL (353.07 mM), Sonication is recommended.
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| Keywords | Tofogliflozin Hydrate | Tofogliflozin (hydrate) | Tofogliflozin | Sodium-dependent glucose cotransporters | SGLT2 | SGLT | ROS | ReactiveOxygenSpecies | Reactive Oxygen Species | Inhibitor | inhibit | CSG-452 Hydrate | CSG452 Hydrate | CSG-452 | CSG452 | CSG 452 Hydrate | CSG 452 |
| Inhibitors Related | Ethoxyquin | Kaolin | Allopurinol | Cysteamine hydrochloride | Ethyl linoleate | Magnesium acetate tetrahydrate | Inosine | L-Cystine | Copper Sulfate Pentahydrate | Dimethyl itaconate | L-Ascorbic acid sodium salt | Dimethyl phthalate |
| Related Compound Libraries | Highly Selective Inhibitor Library | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | GPCR Compound Library |
United States
