Tofogliflozin(CSG 452)

Information Tofogliflozin (CSG 452) is a novelsodium-glucose co-transporter 2(SGLT2)inhibitor with IC50 values of 2.9 nM and 8444 nM for hSGLT2 and hSGLT1, respectively. Targets hSGLT2 (Cell-free assay) 2.9 nM In vitro Tofogliflozin is the potent and most selective inhibitor of SGLT2; the selectivity of tofogliflozin toward SGLT2 is 2900 times that toward SGLT1. Tofogliflozin dose-dependently inhibited glucose entry into tubular cells, tofogliflozin suppressed high glucose-induced ROS generation, MCP-1 gene induction and apoptosis in tubular cells and an antioxidant NAC mimicked the effects of tofogliflozin on high glucoseexposed tubular cells. In vivo A single oral administration of this compound lowers blood glucose levels in Zucker diabetic rats with increased renal glucose clearance and treatment for 4 weeks with this compound improves glucose tolerance in db/db mice. Tofogliflozin treatment lowers urine volume compared with the untreated control group at 8 weeks of treatment. Tofogliflozin treatment increases renal glucose clearance levels compared with untreated db/db mice, whereas losartan treatment has no effect on this parameter. Tofogliflozin treatment reduces the threshold of glucose reabsorption in db/db mice and increases the UGE, and then reduces the PG. Tofogliflozin treatment significantly and dose-dependently elevates the total beta-cell mass, suggesting that beta-cell loss is prevented. Tofogliflozin suppresses plasma glucose and glycated Hb and preserves pancreatic beta-cell mass and plasma insulin levels. Cell Research(from reference) Cell lines：Tubular cells Concentrations：3 nM or 30 nM Incubation Time：24 h

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