1. Anti-infection
  2. HCV
  3. TMC647055

TMC647055 是一种有效的 HCV 复制的非核苷 NS5B 聚合酶抑制剂。TMC647055 具有较强的 HCV 结合活性,其 IC50 值为 82 nM。TMC647055 可用于丙型肝炎病毒 (HCV) 的研究。

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TMC647055 Chemical Structure

TMC647055 Chemical Structure

CAS No. : 1204416-97-6

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TMC647055 is a potent nonnucleoside NS5B polymerase inhibitor of HCV replication. TMC647055 has potent HCV combine activity with an IC50 value of 82 nM. TMC647055 can be used for the research of Hepatitis C virus (HCV)[1][2].

IC50 & Target

EC90: 0.3 μM (Huh7-Luc cell)[1].
EC50: 82 nM (HCV)[2]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK-293T CC50
> 50 μM
Compound: 10a, TMC647055
Cytotoxicity against HEK293T cells after 3 days by resazurin-based fluorescence analysis
Cytotoxicity against HEK293T cells after 3 days by resazurin-based fluorescence analysis
[PMID: 24144360]
HepG2 CC50
> 50 μM
Compound: 10a, TMC647055
Cytotoxicity against human HepG2 cells after 3 days by resazurin-based fluorescence analysis
Cytotoxicity against human HepG2 cells after 3 days by resazurin-based fluorescence analysis
[PMID: 24144360]
Huh-7 EC50
> 28 μM
Compound: 10a, TMC647055
Antiviral activity against Hepatitis C virus genotype 2b infected in human HuH7 by transient replicon assay
Antiviral activity against Hepatitis C virus genotype 2b infected in human HuH7 by transient replicon assay
[PMID: 24144360]
Huh-7 EC50
0.027 μM
Compound: 10a, TMC647055
Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7 by transient replicon assay
Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7 by transient replicon assay
[PMID: 24144360]
Huh-7 EC50
0.048 μM
Compound: 10a, TMC647055
Antiviral activity against Hepatitis C virus genotype 1a infected in human HuH7 by transient replicon assay
Antiviral activity against Hepatitis C virus genotype 1a infected in human HuH7 by transient replicon assay
[PMID: 24144360]
Huh-7 EC50
0.051 μM
Compound: 10a, TMC647055
Antiviral activity against wild-type Hepatitis C virus Con 1b infected in human HuH7 by transient replicon assay
Antiviral activity against wild-type Hepatitis C virus Con 1b infected in human HuH7 by transient replicon assay
[PMID: 24144360]
Huh-7 EC50
0.088 μM
Compound: 10a, TMC647055
Antiviral activity against Hepatitis C virus genotype 3a infected in human HuH7 by transient replicon assay
Antiviral activity against Hepatitis C virus genotype 3a infected in human HuH7 by transient replicon assay
[PMID: 24144360]
Huh-7 EC50
0.097 μM
Compound: 10a, TMC647055
Antiviral activity against Hepatitis C virus genotype 4a infected in human HuH7 by transient replicon assay
Antiviral activity against Hepatitis C virus genotype 4a infected in human HuH7 by transient replicon assay
[PMID: 24144360]
Huh-7 EC50
0.113 μM
Compound: 10a, TMC647055
Antiviral activity against Hepatitis C virus genotype 6a infected in human HuH7 by transient replicon assay
Antiviral activity against Hepatitis C virus genotype 6a infected in human HuH7 by transient replicon assay
[PMID: 24144360]
Huh-7 EC50
12.53 μM
Compound: 10a, TMC647055
Antiviral activity against Hepatitis C virus genotype 2a infected in human HuH7 by transient replicon assay
Antiviral activity against Hepatitis C virus genotype 2a infected in human HuH7 by transient replicon assay
[PMID: 24144360]
Huh-7 EC50
166 nM
Compound: 10a, TMC647055
Antiviral activity against Hepatitis C virus genotype 1a infected in human HuH7-SG cells after 3 days by RT-PCR analysis
Antiviral activity against Hepatitis C virus genotype 1a infected in human HuH7-SG cells after 3 days by RT-PCR analysis
[PMID: 24144360]
Huh-7 EC50
77 nM
Compound: 10a, TMC647055
Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7 cells after 72 hrs by luciferase reporter gene assay
Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7 cells after 72 hrs by luciferase reporter gene assay
[PMID: 24144360]
Huh-7 EC50
82 nM
Compound: 18a, TMC647055
Antiviral activity against Hepatitic C virus genotype 1b clone ET infected in human Huh7 replicon cells after 72 hrs by luciferase reporter gene assay
Antiviral activity against Hepatitic C virus genotype 1b clone ET infected in human Huh7 replicon cells after 72 hrs by luciferase reporter gene assay
[PMID: 22633687]
MRC5 CC50
> 50 μM
Compound: 10a, TMC647055
Cytotoxicity against human MRC5 cells after 3 days by resazurin-based fluorescence analysis
Cytotoxicity against human MRC5 cells after 3 days by resazurin-based fluorescence analysis
[PMID: 24144360]
Vero CC50
> 50 μM
Compound: 10a, TMC647055
Cytotoxicity against African green monkey Vero E6 cells after 3 days by resazurin-based fluorescence analysis
Cytotoxicity against African green monkey Vero E6 cells after 3 days by resazurin-based fluorescence analysis
[PMID: 24144360]
体外研究
(In Vitro)

TMC647055 has antiviral activity with an EC90 value of 0.3 μM in Huh7-Luc cells[1].
TMC647055 has potent combine activity with an EC50 value of 82 nM in cellular HCV assays[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

TMC647055 (compound 18a) (2 mg/kg, iv.; 10mg/kg, po.) shows an acceptable PK profile, characterized by high oral bioavailability and high systemic exposure after single oral dosing of 10 mg/kg, combined with a moderate plasma clearanceand low volume of distribution[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rats[2]
Dosage: 2 mg/kg; 10mg/kg
Administration: 2 mg/kg, iv.; 10mg/kg, po.; singel
Result:
No. Cl (L/h/kg) Cmax(ng/mL) [Liver] (ng/mL) L/P F (%)
TMC647055 (compound 18a) 3.2 440 7800 46 >66
分子量

606.73

Formula

C32H38N4O6S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

TMC647055 相关分类

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  • 稀释计算器

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× = ×
C1   V1   C2   V2

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