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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
中文名称
托福格列嗪(CSG 452), 钠/葡萄糖共转运体 2 抑制剂
英文名称
Tofogliflozin(CSG 452)
中文别名
-
英文别名
(3S,3'R,4'S,5'S,6'R)-5-[(4-ethylphenyl)methyl]-6'-(hydroxymethyl)spiro[1H-2-benzofuran-3,2'-oxane]-3',4',5'-triol;hydrate | CSG-452 hydrate | Q9337027 | tofogliflozin hydrate | (1S,3'R,4'S,5'S,6'R)-6-((4-Ethylphenyl)methyl)-3',4',5',6'-tetrahydro-6'-(hydr
CAS号
1201913-82-7
分子式
C22H26O6.H2O
分子量
404.45 g/mol
精确质量
10mM in DMSO
PSA
100.000 Ų
Logp
1.92
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Tofogliflozin(CSG 452) 10mM in DMSO 1ml

Tofogliflozin(CSG 452) 10mM in DMSO 1ml 麦克林 1201913-82-7,规格齐全,生产科研实验检测,科学材料数智化一站式易购平台。

品牌:麦克林
货号:T797416-1ml
级别: -
货期:30天
已售 199 件
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