(1R,2R)-N-[[[6-(2-羧基-2,3-二氢-1H-异吲哚-4-基)-2,2-二甲基己基]氧]羰基]-3-甲基-L-缬氨酰-(4R)-4-羟基-L-脯氨酰-1-氨基-N-(环丙基磺酰基)-2-乙基环丙甲酰胺 (1-2)-内酯

• 常用名: (1R,2R)-N-[[[6-(2-羧基-2,3-二氢-1H-异吲哚-4-基)-2,2-二甲基己基]氧]羰基]-3-甲基-L-缬氨酰-(4R)-4-羟基-L-脯氨酰-1-氨基-N-(环丙基磺酰基)-2-乙基环丙甲酰胺 (1-2)-内酯
• 英文名: Vaniprevir
• CAS号: 923590-37-8
• 分子量: 757.93600
• 密度: 1.33g/cm3
• 沸点: N/A
• 分子式: C₃₈H₅₅N₅O₉S
• 熔点: N/A
• 闪点: N/A

用途

Vaniprevir(MK-7009)是非共价的HCV NS3/4A蛋白酶抑制剂。

名称

• 中文名: (1R,2R)-N-[[[6-(2-羧基-2,3-二氢-1H-异吲哚-4-基)-2,2-二甲基己基]氧]羰基]-3-甲基-L-缬氨酰-(4R)-4-羟基-L-脯氨酰-1-氨基-N-(环丙基磺酰基)-2-乙基环丙甲酰胺 (1-2)-内酯
• 英文名: Vaniprevir

生物活性

• 描述: Vaniprevir(MK-7009)是非共价的HCV NS3/4A蛋白酶抑制剂。
• 相关类别:
  信号通路 >> 代谢酶/蛋白酶 >> HCV蛋白酶
  信号通路 >> 抗感染 >> HCV
  研究领域 >> 感染
• 参考文献:

  [1]. Liverton, Nigel J.; Carroll, Steven S.; Di Muzio, Jillian;.MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease. Antimicrobial Agents and Chemotherapy (2009), Volume Date 2010, 54(1), 305-311.

  [2]. Kong J, Chen CY, Balsells-Padros J, Cao Y, Dunn RF, Dolman SJ, Janey J, Li H, Zacuto MJ.Synthesis of the HCV protease inhibitor Vaniprevir (MK-7009) using ring-closing metathesis strategy.J Org Chem. 2012 Apr 20;77(8):3820-8. Epub 2012 Apr 10.

  [3]. Manns MP, Gane E, Rodriguez-Torres M, Stoehr A, Yeh CT, Marcellin P, Wiedmann RT, Hwang PM, Caro L, Barnard RJ, Lee AW; for the MK-7009 Protocol 007 Study Group.Vaniprevir with pegylated interferon alpha-2a and ribavirin in treatment-na?ve patients with chronic hepatitis C: A randomized phase II study.Hepatology. 2012 Sep;56(3):884-893.

  [4]. Song ZJ, Tellers DM, Journet M, Kuethe JT, Lieberman D, Humphrey G, Zhang F, Peng Z, Waters MS, Zewge D, Nolting A, Zhao D, Reamer RA, Dormer PG, Belyk KM, Davies IW, Devine PN, Tschaen DM.Synthesis of vaniprevir (MK-7009): lactamization to prepare a 20-membered [corrected] macrocycle.J Org Chem. 2011 Oct 7;76(19):7804-15. Epub 2011 Aug 31.

  [5]. McCauley JA, McIntyre CJ, Rudd MT, Nguyen KT, Romano JJ, Butcher JW, Gilbert KF, Bush KJ, Holloway MK, Swestock J, Wan BL, Carroll SS, DiMuzio JM, Graham DJ, Ludmerer SW, Mao SS, Stahlhut MW, Fandozzi CM, Trainor N, Olsen DB, Vacca JP, Liverton NJ.Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor.J Med Chem. 2010 Mar 25;53(6):2443-63.

物理化学性质

• 密度: 1.33g/cm3
• 分子式: C₃₈H₅₅N₅O₉S
• 分子量: 757.93600
• 精确质量: 757.37200
• PSA: 197.59000
• LogP: 5.27350
• 储存条件: -20°C，密闭，干燥