951382-34-6

• 常用中文名：依格列净脯氨酸
• 常用英文名：Ipragliflozin L-Proline
• CAS号：951382-34-6
• 分子式：C₂₆H₃₀FNO₇S
• 分子量：519.58200
• 相关类别： 信号通路 跨膜转运 SGLT
• 发布时间：2016-05-20 04:03:58
• 更新时间：2026-07-06 18:50:30
• Ipragliflozin (L-Proline) 是 SGLT2 高活性的,选择性抑制剂,IC50 为 2.8 nM,对 SGLT1/3/4/5/6 几乎无活性。

名称

• 中文名: 依格列净脯氨酸
• 英文名: (2S,3R,4R,5S,6R)-2-[3-(1-benzothiophen-2-ylmethyl)-4-fluorophenyl]-6-(hydroxymethyl)oxane-3,4,5-triol,(2S)-pyrrolidine-2-carboxylic acid
• 中文别名: 伊格列净L-脯氨酸 951-6; 依格列净脯氨酸/L-脯氨酸依格列净; 阿齐沙坦杂质62; 伊格列净标准品2-L; (2S,3R,4R,5S,6R)-2-(3-(苯并[B]噻吩-2-基甲基)-4-氟苯基)-6-(羟甲基)四氢-2H-吡喃-3,4,5-三醇 (S)-吡咯烷-2-羧酸盐; L-脯氨酸伊格列净; 依格列净L-脯氨酸; L-脯氨酸与(1S)-1,5-脱水-1-C-[3-(苯并[B]噻吩-2-基甲基)-4-氟苯基]-D-山梨糖醇的化合物; 伊格列净脯氨酸; 伊格列净L-脯氨酸盐; 伊格列净002; 伊格列净L-脯氨酸; 依格列净L-脯氨酸盐; L-脯氨酸依格列净
• 英文别名: L-proline compound with (3R,4R,5S,6R)-2-(3-(benzo[b]thiophen-2-ylmethyl)-4-fluorophenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol (1:1); L-Proline compd. with (1S)-1,5-anhydro-1-C-[3-(benzo[b]thien-2-ylmethyl)-4-fluorophenyl]-D-glucitol; Ipragliflozin-002-L; (2S,3R,4R,5S,6R)-2-[3-(1-benzothiophen-2-ylmethyl)-4-fluorophenyl]-6-(hydroxymethyl)oxane-3,4,5-triol,(2S)-pyrrolidine-2-cboxylic acid; D1060; Ipragliflozin L-proline; L-Prolinecompd.with(1S)-1,5-anhydro-1-C-[3-(benzo[b]thien-2-ylmethyl)-4-fluorophenyl]-D-glucitol(1:1); Ipragliflozin (L-Proline); Azilstan Impurity 62; lpragliflozin L-Proline; Ipragliflozin L-prolineQ: What is Ipragliflozin L-proline Q: What is the CAS Number of Ipragliflozin L-proline Q: What is the storage condition of Ipragliflozin L-proline Q: What e the applications of Ipragliflozin L-proline; l-prolinecompd.with(1s)-1,5-anhydro-1-c-(3-(benzo(b)thien-2; ASP-1941; L-Proline compd. with (1S)-1,5-anhydro-1-C-[3-(benzo[b]thien-2-ylmethyl)-4-fluorophenyl]-D-glucitol (1:1); UNII-M6N3GK48A4; L-Proline compd. with (1S)-1,5-anhydro-1-C-[3-(benzo[b]thien-2-ylmethyl)-4-fluorophenyl]-D-glucitol (1:1)ChemicalBook; l-prolinecompd; (2S,3R,4R,5S,6R)-2-(3-(Benzo[b]thiophen-2-ylmethyl)-4-fluorophenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol (S)-Pyrrolidine-2-cboxylic acid

物化性质

• 分子式: C₂₆H₃₀FNO₇S
• 分子量: 519.58200
• 精确质量: 519.17300
• PSA: 167.72000
• LogP: 2.29790
• 储存条件: 2-8℃

生物活性

• 描述: Ipragliflozin (L-Proline) 是 SGLT2 高活性的,选择性抑制剂,IC50 为 2.8 nM,对 SGLT1/3/4/5/6 几乎无活性。
• 相关类别:
  信号通路 >> 跨膜转运 >> SGLT
  研究领域 >> 代谢疾病
• 靶点:

  IC50 value: 2.8 nM (SGLT2)[1][2].

• 体外研究: Ipragliflozin(L-Proline)在纳摩尔范围内有效且选择性地抑制人,大鼠和小鼠SGLT2,并显示出对抗肠葡萄糖苷酶的稳定性[3]。
• 体内研究: Ipragliflozin(L-Proline)在口服给药后显示出良好的药代动力学特性,并且剂量依赖性地增加尿糖排泄,其在正常小鼠中持续超过12小时[3]。口服ipragliflozin可以剂量依赖的方式增加尿糖排泄,这种作用在0.3 mg/kg或更高剂量时显着,持续时间超过12 h [4]。单次给予ipragliflozin剂量依赖性地增加尿糖排泄,降低血糖和血浆胰岛素水平,并改善葡萄糖耐受不良[5]。
• 参考文献:

  [1]. Imamura M, et al. Discovery of Ipragliflozin (ASP1941): a novel C-glucoside with benzothiophene structure as a potent and selective sodium glucose co-transporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes mellitus. Bioorg Med Chem. 2012 May 15;20(10):3263-79.

  [2]. 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.

  [3]. Tahara A, et al. Pharmacological profile of ipragliflozin (ASP1941), a novel selective SGLT2 inhibitor, in vitro and in vivo. Naunyn Schmiedebergs Arch Pharmacol. 2012 Apr;385(4):423-36.

  [4]. Tahara A, et al. Antidiabetic effects of SGLT2-selective inhibitor ipragliflozin in streptozotocin-nicotinamide-induced mildly diabetic mice. J Pharmacol Sci. 2012;120(1):36-44.

  [5]. Tahara A, et al. Effects of SGLT2 selective inhibitor ipragliflozin on hyperglycemia, hyperlipidemia, hepatic steatosis, oxidative stress, inflammation, and obesity in type 2 diabetic mice. Eur J Pharmacol. 2013 Sep 5;715(1-3):246-55.