1535212-07-7

• 常用中文名：伏西瑞韦
• 常用英文名：voxilaprevir
• CAS号：1535212-07-7
• 分子式：C₄₀H₅₂F₄N₆O₉S
• 分子量：868.93400
• 相关类别： 信号通路 代谢酶/蛋白酶 HCV蛋白酶
• 发布时间：2018-02-04 08:00:00
• 更新时间：2026-07-05 17:57:07
• Voxilaprevir (GS-9857) 是一种含氟大环丙型肝炎病毒 (HCV) 非结构蛋白 (NS) 3/4A 蛋白酶抑制剂。对基因型 1-6 HCV 具有很强的体外抗病毒活性,并广泛覆盖 NS3/4A 蛋白酶多态性。GS-9857 提高了对常见的 NS3 抗药性相关突变体 (RAVs) 的覆盖率。

名称

• 中文名: 伏西瑞韦
• 英文名: voxilaprevir
• 中文别名: 维昔普维; 伏西瑞韦,10 MM DMSO 溶液; (33R,34S,35S,91R,92R,5S)-5-(叔丁基)-N-((1R,2R)-2-(二氟甲基)-1-(((1-甲基环丙基)磺酰基)氨基甲酰基)环丙基)-34-乙基-14,14-二氟-17-甲氧基-4,7-二氧代-2,8-二氧杂-6-氮杂-1(2,3)-喹喔啉-3(3,1)-吡咯烷-9(1,2)-环丙烷环十四烷-35-甲酰胺
• 英文别名: (1R,18R,20R,24S,27S,28S)-N-[(1R,2R)-2-(Difluoromethyl)-1-{[(1-methylcyclopropyl)sulfonyl]carbamoyl}cyclopropyl]-28-ethyl-13,13-difluoro-7-methoxy-24-(2-methyl-2-propanyl)-22,25-dioxo-2,21-dioxa-4,11,2 ;3,26-tetraazapentacyclo[24.2.1.0.0.0]nonacosa-3(12),4,6,8,10-pentaene-27-carboxamide; Voxilaprevir, 10 mM in DMSO; voxilaprevirum; (1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-{[(1-methylcyclopropyl)sulfonyl]carbamoyl}cyclopropyl]-9-ethyl-18,18-difluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide; inhibit,antiviral,HCV Protease,Inhibitor,GS9857,pangenotypic,GS-9857,GS 9857,Voxilaprevir,infection,DAA,HCV,direct-acting antiviral; GS-9857; Cyclopropanecboxamide, N-[[[(1R,2R)-2-[5,5-difluoro-5-(3-hydroxy-6-methoxy-2-quinoxalinyl)pentyl]cyclopropyl]oxy]carbonyl]-3-methyl-L-valyl-(3S,4R)-3-ethyl-4-hydroxy-L-prolyl-1-amino-2-(difluoromethyl)-N-[(1-methylcyclopropyl)sulfonyl]-, cyclic (1→2)-ether, (1R,2R); UNII:0570F37359; GS9857; GS-333170; (1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1 R,2R)-2-(difluoromethyl)-1-{[(1-methylcyclopropyl)sulfonyl]carbamoyl}cyclopropyl]-9-ethyl-18,18-difluoro-14- methoxy-3,6-dioxo-1,1a,3,4,5,6,9,1 0,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide; (33R,34S,35S,91R,92R,5S)-5-(tert-Butyl)-N-((1R,2R)-2-(difluoromethyl)-1-(((1-methylcyclopropyl)sulfonyl)cbamoyl)cyclopropyl)-34-ethyl-14,14-difluoro-17-methoxy-4,7-dioxo-2,8-dioxa-6-aza-1(2,3)-quinoxalina-3(3,1)-pyrrolidina-9(1,2)-cyclopropanacyclotetradecaphane-35-cboxamide; Voxilaprevir

物化性质

• 密度: 1.4±0.1 g/cm3
• 分子式: C₄₀H₅₂F₄N₆O₉S
• 分子量: 868.93400
• 精确质量: 868.34500
• PSA: 203.60000
• LogP: 3.83
• 折射率: 1.596
• 储存条件: 2-8°C
• 水溶解性: Insuluble (2.8E-4 g/L) (25 ºC)

生物活性

• 描述: Voxilaprevir (GS-9857) 是一种含氟大环丙型肝炎病毒 (HCV) 非结构蛋白 (NS) 3/4A 蛋白酶抑制剂。对基因型 1-6 HCV 具有很强的体外抗病毒活性,并广泛覆盖 NS3/4A 蛋白酶多态性。GS-9857 提高了对常见的 NS3 抗药性相关突变体 (RAVs) 的覆盖率。
• 相关类别:
  研究领域 >> 感染
  信号通路 >> 代谢酶/蛋白酶 >> HCV蛋白酶
• 靶点:

  Hepatitis C virus (HCV) nonstructural protein (NS) 3/4A protease[1]

• 参考文献:

  [1]. Rodriguez-Torres M, et al. GS-9857 in patients with chronic hepatitis C virus genotype 1-4 infection: a randomized, double-blind, dose-ranging phase 1 study. J Viral Hepat. 2016 Aug;23(8):614-22.

  [2]. Lawitz E, et al. Efficacy of Sofosbuvir, Velpatasvir, and GS-9857 in Patients With Genotype 1 Hepatitis C VirusInfection in an Open-Label, Phase 2 Trial. Gastroenterology. 2016 Nov;151(5):893-901.e1.