1201913-82-7

• 常用中文名：托格列净
• 常用英文名：Tofogliflozin (hydrate)
• CAS号：1201913-82-7
• 分子式：C₂₂H₂₈O₇
• 分子量：404.45400
• 相关类别： 原料药 激素及调节内分泌功能类药 胰腺激素及其它调节血糖药
• 发布时间：2017-10-09 23:55:48
• 更新时间：2024-01-01 23:06:51
• Tofogliflozin(CSG-452)是SGLT2高效选择性抑制剂，对人源、大鼠和小鼠SGLT2的Ki值分别为2.9、14.9和6.4nM。

名称

• 中文名: 托格列净
• 英文名: (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
• 英文别名: CSG452; Tofogliflozin hydrate (JAN); (1S,3'R,4'S,5'S,6'R)-6-((4-Ethylphenyl)methyl)-3',4',5',6'-tetrahydro-6'-(hydroxymethyl)-spiro(isobenzofuran-1(3H),2'-(2H)pyran)-3',4',5'-triol monohydrate; (1S,3'R,4'S,5'S,6'R)-6-((4-Ethylphenyl)methyl)-6'-(hydroxymethyl)-3',4',5',6'-tetrahydro-3H-spiro(2-benzofuran-1,2'-pyran)-3',4',5'-triol monohydrate; Tofogliflozin (USAN); Tofogliflozin [USAN:INN]; UNII-P8DD8KX4O4; Tofogliflozin (hydrate)

物化性质

• 分子式: C₂₂H₂₈O₇
• 分子量: 404.45400
• 精确质量: 404.18400
• PSA: 108.61000
• LogP: 0.93230
• 外观性状: 粉末
• 储存条件: -20℃

生物活性

• 描述: Tofogliflozin(CSG-452)是SGLT2高效选择性抑制剂,对人源、大鼠和小鼠SGLT2的Ki值分别为2.9、14.9和6.4nM。
• 相关类别:
  信号通路 >> 跨膜转运 >> SGLT
  研究领域 >> 代谢疾病
• 参考文献:

  [1]. 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.

  [2]. Nagata T, et al. Tofogliflozin, a novel sodium-glucose co-transporter 2 inhibitor, improves renal and pancreatic function in db/db mice. Br J Pharmacol. 2013 Oct;170(3):519-31.

  [3]. Yamane M, et al. In vitro profiling of the metabolism and drug-drug interaction of tofogliflozin, a potent and highly specific sodium-glucose co-transporter 2 inhibitor, using human liver microsomes, human hepatocytes, and recombinant human CYP. Xenobioti

  [4]. Nagata T, et al. Selective SGLT2 inhibition by tofogliflozin reduces renal glucose reabsorption under hyperglycemic but not under hypo- or euglycemic conditions in rats. Am J Physiol Endocrinol Metab. 2013 Feb 15;304(4):E414-23.