产品描述 | Vaniprevir (MK-7009) is a non-covalent competitive inhibitor of the hepatitis C virus (HCV) NS3/4A protease.IC50 Value: Target: HCV NS3/4A Protease; HCVvaniprevir (MK-7009) is a macrocyclic hepatitis C virus NS3/4a protease inhibitor, is active against both the genotype 1 and genotype 2 NS3/4a protease enzymes. vaniprevir (MK-7009) has good plasma exposure and excellent liver exposure in multiple species. References: [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. |