928672-86-0

• 常用中文名：卡格列净半水合物
• 常用英文名：Canagliflozin hemihydrate
• CAS号：928672-86-0
• 分子式：C₂₄H₂₆FO_5.5S
• 分子量：453.52
• 相关类别： 信号通路 跨膜转运 SGLT
• 发布时间：2018-03-12 08:00:00
• 更新时间：2024-01-01 18:10:56
• Canagliflozin(JNJ 28431754; TA 7284)半水合物是高活性的hSGLT2选择性抑制剂,IC50为2.2 nM,比对hSGLT1的抑制性高400倍。

名称

• 中文名: 卡格列净半水合物
• 英文名: Canagliflozin hemihydrate
• 中文别名: 坎格列嗪半水合物; 坎格列净半水合物
• 英文别名: (1S)-1,5-Anhydro-1-(3-{[5-(4-fluorophenyl)-2-thienyl]methyl}-4-methylphenyl)-D-glucitol hydrate (2:1); (2S,3R,4R,5S,6R)-2-[3-[[5-(4-fluorophenyl)thiophen-2-yl]methyl]-4-methylphenyl]-6-(hydroxymethyl)oxane-3,4,5-triol,hydrate; UNII-0SAC974Z85; canagliflozin hydrate; D-Glucitol, 1,5-anhydro-1-C-[3-[[5-(4-fluorophenyl)-2-thienyl]methyl]-4-methylphenyl]-, (1S)-, hydrate (2:1); Invokana; TA-7284; Canagliflozin (hemihydrate)

物化性质

• 分子式: C₂₄H₂₆FO_5.5S
• 分子量: 453.52
• PSA: 246.01000
• LogP: 5.87230
• 外观性状: 类白色至黄色固体
• 储存条件: -20℃

生物活性

• 描述: Canagliflozin(JNJ 28431754; TA 7284)半水合物是高活性的hSGLT2选择性抑制剂,IC50为2.2 nM,比对hSGLT1的抑制性高400倍。
• 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]. Sumihiro Nomura et al. Discovery of Canagliflozin, a Novel C-Glucoside with Thiophene Ring, as Sodium-Dependent Glucose Cotransporter 2 Inhibitor for the Treatment of Type 2 Diabetes Mellitus J. Med. Chem., 2010, 53 (17), pp 6355-6360

  [2]. Nicolle LE, Capuano G, Ways K, Usiskin K.Effect of canagliflozin, a sodium glucose co-transporter 2 (SGLT2) inhibitor, on bacteriuria and urinary tract infection in subjects with type 2 diabetes enrolled in a 12-week, phase 2 study.Curr Med Res Opin. 2012 Jul;28(7):1167-71.

  [3]. Rosenstock J, et al. Canagliflozin DIA 2001 Study Group.Dose-ranging effects of canagliflozin, a sodium-glucose cotransporter 2 inhibitor, as add-on to metformin in subjects with type 2 diabetes.Diabetes Care. 2012 Jun;35(6):1232-8.

  [4]. Liang Y, et al. Effect of canagliflozin on renal threshold for glucose, glycemia, and body weight in normal and diabetic animal models.PLoS One. 2012;7(2):e30555.

  [5]. Devineni D, et al. Canagliflozin improves glycaemic control over 28 days in subjects with type 2 diabetes not optimally controlled on insulin.Diabetes Obes Metab. 2012 Jun;14(6):539-45. doi: 10.1111/j.1463-1326.2012.01558.x.