盐酸茚罗西生

更新时间:2024-01-09 00:15:03

盐酸茚罗西生结构式
盐酸茚罗西生结构式
品牌特惠专场
常用名 盐酸茚罗西生 英文名 R-1479
CAS号 478182-28-4 分子量 284.229
密度 N/A 沸点 N/A
分子式 C9H12N6O5 熔点 N/A
MSDS N/A 闪点 N/A

 盐酸茚罗西生用途


R-1479 是一种特异性的HCV复制 (HCV replication) 抑制剂,在HCV亚基因组复制体系中,IC50 为 1.28 μM。

 盐酸茚罗西生名称

中文名 盐酸茚罗西生
英文名 4-amino-1-[(2R,3R,4S,5R)-5-azido-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one
英文别名 更多

 盐酸茚罗西生生物活性

描述 R-1479 是一种特异性的HCV复制 (HCV replication) 抑制剂,在HCV亚基因组复制体系中,IC50 为 1.28 μM。
相关类别
靶点

IC50: 1.28 μM (HCV replication)[1]

体外研究 当在增殖的复制子细胞孵育72小时后作为剂量依赖性的Renillaluciferase活性降低测量时,R-1479(R1479)抑制HCV RNA复制,平均IC 50值为1.28μM。 R-1479对浓度高达2mM的HCV复制子或Huh-7细胞的细胞存活率或增殖没有影响[1]。最有效和非细胞毒性的衍生物是R-1479,在HCV复制子系统中IC50为1.28μM。制备R-1479的三磷酸盐,并显示其是由NS5B介导的RNA合成的抑制剂(IC50 = 320nM),由HCV编码的RNA聚合酶。 R-1479在复制子测定中显示出良好的活性,没有可测量的细胞毒性或细胞抑制作用[2]。
激酶实验 膜结合的天然HCV复制酶复合物从2209-23 HCV复制子细胞和携带HCV复制子RNA的衍生细胞系中分离,所述HCV复制子RNA在NS5B编码序列中具有S282T突变。体外复制酶测定包含10μL细胞质膜级分,50 mM HEPES(pH 7.5),10 mM KCl,10 mM二硫苏糖醇,5 mM MgCl2,20μg/ mL放线菌素D,1 mM ATP,1 mM GTP,1 mM UTP,30μCi[α-33P] CTP(3000 Ci / mmol,10 mCi / mL),1单位/μLSUPERase•In,10 mM肌酸磷酸盐和200μg/ mL肌酸磷酸激酶,终体积25μL 。确定核苷酸类似物的抑制[1]。
细胞实验 使用[3H]胸苷掺入闪烁亲近测定系统测量R-1479对氚标记的胸苷掺入细胞DNA的影响。 MTT和WST-1测定系统用于测量细胞活力。 ATP生物发光检测试剂盒HSII用于测量细胞内ATP水平[1]。
参考文献

[1]. Klumpp K, et al. The novel nucleoside analog R1479 (4'-azidocytidine) is a potent inhibitor of NS5B-dependent RNA synthesis and hepatitis C virus replication in cell culture. J Biol Chem. 2006 Feb 17;281(7):3793-9.

[2]. Smith DB, et al. Design, synthesis, and antiviral properties of 4'-substituted ribonucleosides as inhibitors of hepatitis C virus replication: the discovery of R1479. Bioorg Med Chem Lett. 2007 May 1;17(9):2570-6.

 盐酸茚罗西生物理化学性质

分子式 C9H12N6O5
分子量 284.229
精确质量 284.086914
PSA 181.57000
LogP -0.20
储存条件 -20°C

 盐酸茚罗西生合成线路

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盐酸茚罗西生结构式

盐酸茚罗西生

478182-28-4

文献:Smith, David B.; Martin, Joseph A.; Klumpp, Klaus; Baker, Stewart J.; Blomgren, Peter A.; Devos, Rene; Granycome, Caroline; Hang, Julie; Hobbs, Christopher J.; Jiang, Wen-Rong; Laxton, Carl; Pogam, Sophie Le; Leveque, Vincent; Ma, Han; Maile, Graham; Merrett, John H.; Pichota, Arkadius; Sarma, Keshab; Smith, Mark; Swallow, Steven; Symons, Julian; Vesey, David; Najera, Isabel; Cammack, Nick Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 9 p. 2570 - 2576

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盐酸茚罗西生结构式

盐酸茚罗西生

478182-28-4

文献:Smith, David B.; Martin, Joseph A.; Klumpp, Klaus; Baker, Stewart J.; Blomgren, Peter A.; Devos, Rene; Granycome, Caroline; Hang, Julie; Hobbs, Christopher J.; Jiang, Wen-Rong; Laxton, Carl; Pogam, Sophie Le; Leveque, Vincent; Ma, Han; Maile, Graham; Merrett, John H.; Pichota, Arkadius; Sarma, Keshab; Smith, Mark; Swallow, Steven; Symons, Julian; Vesey, David; Najera, Isabel; Cammack, Nick Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 9 p. 2570 - 2576

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盐酸茚罗西生结构式

盐酸茚罗西生

478182-28-4

文献:Smith, David B.; Martin, Joseph A.; Klumpp, Klaus; Baker, Stewart J.; Blomgren, Peter A.; Devos, Rene; Granycome, Caroline; Hang, Julie; Hobbs, Christopher J.; Jiang, Wen-Rong; Laxton, Carl; Pogam, Sophie Le; Leveque, Vincent; Ma, Han; Maile, Graham; Merrett, John H.; Pichota, Arkadius; Sarma, Keshab; Smith, Mark; Swallow, Steven; Symons, Julian; Vesey, David; Najera, Isabel; Cammack, Nick Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 9 p. 2570 - 2576

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盐酸茚罗西生结构式

盐酸茚罗西生

478182-28-4

文献:Smith, David B.; Martin, Joseph A.; Klumpp, Klaus; Baker, Stewart J.; Blomgren, Peter A.; Devos, Rene; Granycome, Caroline; Hang, Julie; Hobbs, Christopher J.; Jiang, Wen-Rong; Laxton, Carl; Pogam, Sophie Le; Leveque, Vincent; Ma, Han; Maile, Graham; Merrett, John H.; Pichota, Arkadius; Sarma, Keshab; Smith, Mark; Swallow, Steven; Symons, Julian; Vesey, David; Najera, Isabel; Cammack, Nick Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 9 p. 2570 - 2576

~%

盐酸茚罗西生结构式

盐酸茚罗西生

478182-28-4

文献:Smith, David B.; Martin, Joseph A.; Klumpp, Klaus; Baker, Stewart J.; Blomgren, Peter A.; Devos, Rene; Granycome, Caroline; Hang, Julie; Hobbs, Christopher J.; Jiang, Wen-Rong; Laxton, Carl; Pogam, Sophie Le; Leveque, Vincent; Ma, Han; Maile, Graham; Merrett, John H.; Pichota, Arkadius; Sarma, Keshab; Smith, Mark; Swallow, Steven; Symons, Julian; Vesey, David; Najera, Isabel; Cammack, Nick Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 9 p. 2570 - 2576

~%

盐酸茚罗西生结构式

盐酸茚罗西生

478182-28-4

文献:Smith, David B.; Martin, Joseph A.; Klumpp, Klaus; Baker, Stewart J.; Blomgren, Peter A.; Devos, Rene; Granycome, Caroline; Hang, Julie; Hobbs, Christopher J.; Jiang, Wen-Rong; Laxton, Carl; Pogam, Sophie Le; Leveque, Vincent; Ma, Han; Maile, Graham; Merrett, John H.; Pichota, Arkadius; Sarma, Keshab; Smith, Mark; Swallow, Steven; Symons, Julian; Vesey, David; Najera, Isabel; Cammack, Nick Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 9 p. 2570 - 2576

~%

盐酸茚罗西生结构式

盐酸茚罗西生

478182-28-4

文献:Smith, David B.; Martin, Joseph A.; Klumpp, Klaus; Baker, Stewart J.; Blomgren, Peter A.; Devos, Rene; Granycome, Caroline; Hang, Julie; Hobbs, Christopher J.; Jiang, Wen-Rong; Laxton, Carl; Pogam, Sophie Le; Leveque, Vincent; Ma, Han; Maile, Graham; Merrett, John H.; Pichota, Arkadius; Sarma, Keshab; Smith, Mark; Swallow, Steven; Symons, Julian; Vesey, David; Najera, Isabel; Cammack, Nick Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 9 p. 2570 - 2576

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 盐酸茚罗西生英文别名

4-amino-1-[(2R,3R,4S,5R)-5-azido-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]pyrimidin-2(1H)-one (non-preferred name)
R-1479||4'-Azidocytidine|R1479
CS-0362
4'-azidocytidine
4'azidocytidine
R1479
4-Amino-1-[(2R,3R,4S,5R)-5-azido-3,4-dihydroxy-5-(hydroxymethyl)tetrahydro-2-furanyl]-2(1H)-pyrimidinone
R-1479
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