850649-61-5

• 常用中文名：阿格列汀
• 常用英文名：Alogliptin
• CAS号：850649-61-5
• 分子式：C₁₈H₂₁N₅O₂
• 分子量：339.392
• 相关类别： 生物化工 抑制剂 蛋白酶体(Proteases) DPP-4 抑制剂
• 发布时间：2018-07-18 07:06:09
• 更新时间：2024-01-05 06:42:04
• Alogliptin(SYR-322)是高活性DPP4选择性抑制剂,IC50<10 nM,比对DPP8和DPP9的抑制性高10000倍以上。

名称

• 中文名: 阿格列汀
• 英文名: alogliptin
• 中文别名: 阿洛利停
• 英文别名: ALOGLIPTIN(ALOGLIPTINE,ALOGLIPTINA); 2-({6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl}methyl)benzonitrile; Alogliptin; UNII-JHC049LO86; 2-({6-[(3R)-3-Amino-1-piperidinyl]-3-methyl-2,4-dioxo-3,4-dihydro-1(2H)-pyrimidinyl}methyl)benzonitrile; Benzonitrile, 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-; 2-[[6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxopyrimidin-1-yl]methyl]benzonitrile; alogliptina

物化性质

• 密度: 1.3±0.1 g/cm3
• 沸点: 519.2±60.0 °C at 760 mmHg
• 分子式: C₁₈H₂₁N₅O₂
• 分子量: 339.392
• 闪点: 267.8±32.9 °C
• 精确质量: 339.169525
• PSA: 97.05000
• LogP: 1.84
• 蒸汽压: 0.0±1.4 mmHg at 25°C
• 折射率: 1.660
• 储存条件: 室温，干燥，密封

生物活性

• 描述: Alogliptin(SYR-322)是高活性DPP4选择性抑制剂,IC50<10 nM,比对DPP8和DPP9的抑制性高10000倍以上。
• 相关类别:
  信号通路 >> 代谢酶/蛋白酶 >> 二肽基肽酶
  研究领域 >> 代谢疾病
• 参考文献:

  [1]. Feng J, et al. Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV. J Med Chem. 2007 May 17;50(10):2297-300.

  [2]. Ta NN, et al. DPP-4 (CD26) inhibitor alogliptin inhibits TLR4-mediated ERK activation and ERK-dependent MMP-1 expression by U937 histiocytes. Atherosclerosis. 2010 Dec;213(2):429-35.

  [3]. Asakawa T, et al. A novel dipeptidyl peptidase-4 inhibitor, alogliptin (SYR-322), is effective in diabetic rats with sulfonylurea-induced secondary failure. Life Sci. 2009 Jul 17;85(3-4):122-6.

  [4]. Moritoh Y, et al. The dipeptidyl peptidase-4 inhibitor alogliptin in combination with pioglitazone improves glycemic control, lipid profiles, and increases pancreatic insulin content in ob/ob mice. Eur J Pharmacol. 2009 Jan 14;602(2-3):448-54.

  [5]. Kajiwara A, et al. Risk Factors for Adverse Symptoms During Dipeptidyl Peptidase-IV Inhibitor Therapy: A Questionnaire-Based Study Carried Out by the Japan Pharmaceutical Association Drug Event Monitoring Project in Kumamoto Prefecture. Drug Saf. 2013 Oct

安全

• 危害码 (欧洲): Xi
• 安全声明 (欧洲): 24/25
• 危险品运输编码: 3077

合成路线

865758-95-8 ~% 850649-61-5

文献：Journal of Medicinal Chemistry, , vol. 50, # 10 p. 2297 - 2300

22115-41-9 ~% 850649-61-5

文献：Journal of Medicinal Chemistry, , vol. 50, # 10 p. 2297 - 2300