Vaniprevir
Based on 1 publication(s) in Google Scholar
Vaniprevir (MK-7009) is a non-covalent competitive inhibitor of the hepatitis C virus (HCV) NS3/4A protease.
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- CAS 番号: 923590-37-8
- 分子式: C38H55N5O9S
- 分子量:757.94
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Vaniprevir
More
生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | EC50 |
0.27 nM
Compound: MK-7009
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Antiviral activity against HCV1b harboring Q80Q polymorphism in NS3 protease gene infected in human Huh7/Lunet cells assessed as inhibition of viral replication after 3 days by luciferase based transient-transfection assay
Antiviral activity against HCV1b harboring Q80Q polymorphism in NS3 protease gene infected in human Huh7/Lunet cells assessed as inhibition of viral replication after 3 days by luciferase based transient-transfection assay
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[PMID: 20855726] |
| Huh-7 | EC50 |
0.41 nM
Compound: MK-7009
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Antiviral activity against HCV1b harboring Q80K polymorphism in NS3 protease gene infected in human Huh7/Lunet cells assessed as inhibition of viral replication after 3 days by luciferase based transient-transfection assay
Antiviral activity against HCV1b harboring Q80K polymorphism in NS3 protease gene infected in human Huh7/Lunet cells assessed as inhibition of viral replication after 3 days by luciferase based transient-transfection assay
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[PMID: 20855726] |
| Huh-7 | EC50 |
0.7 nM
Compound: MK-7009
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Antiviral activity against HCV1b Con1 harboring NS3 protease gene infected in human Huh7/Lunet cells assessed as inhibition of viral replication after 3 days by luciferase based transient-transfection assay
Antiviral activity against HCV1b Con1 harboring NS3 protease gene infected in human Huh7/Lunet cells assessed as inhibition of viral replication after 3 days by luciferase based transient-transfection assay
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[PMID: 20855726] |
| Huh-7 | EC50 |
5 nM
Compound: MK-7009
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Antiviral activity against HCV 1B infected in human Huh7 cells by firefly luciferase reporter gene assay
Antiviral activity against HCV 1B infected in human Huh7 cells by firefly luciferase reporter gene assay
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[PMID: 20541424] |
| Huh-7 | IC50 |
19 nM
Compound: 1, MK-7009
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Antiviral activity against Hepatitis C virus (isolate Con1) genotype 1b infected in human HuH7 cells assessed as inhibition of viral replication after 24 hrs in presence of 50% NHS
Antiviral activity against Hepatitis C virus (isolate Con1) genotype 1b infected in human HuH7 cells assessed as inhibition of viral replication after 24 hrs in presence of 50% NHS
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[PMID: 24900473] |
| Huh-7 | IC50 |
19 nM
Compound: 35b, vaniprevir, MK-7009
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Antiviral activity against HCV Con1 infected in human HuH7 cells assessed as inhibition of viral replication after 24 hrs by replicon assay in presence of 50% normal human serum
Antiviral activity against HCV Con1 infected in human HuH7 cells assessed as inhibition of viral replication after 24 hrs by replicon assay in presence of 50% normal human serum
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[PMID: 20163176] |
| Huh-7 | IC50 |
3 nM
Compound: 35b, vaniprevir, MK-7009
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Antiviral activity against HCV Con1 infected in human HuH7 cells assessed as inhibition of viral replication after 24 hrs by replicon assay in presence of 10% fetal bovine serum
Antiviral activity against HCV Con1 infected in human HuH7 cells assessed as inhibition of viral replication after 24 hrs by replicon assay in presence of 10% fetal bovine serum
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[PMID: 20163176] |
| Huh-7 | IC50 |
9 nM
Compound: 35b, vaniprevir, MK-7009
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Antiviral activity against HCV JFH-1 infected in human HuH7 cells assessed as inhibition of viral replication after 24 hrs by replicon assay in presence of 10% fetal bovine serum
Antiviral activity against HCV JFH-1 infected in human HuH7 cells assessed as inhibition of viral replication after 24 hrs by replicon assay in presence of 10% fetal bovine serum
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[PMID: 20163176] |
| Species | Dose | Route | CLplasma | Vd | T1/2 | AUC0-24 | Cmax |
|---|---|---|---|---|---|---|---|
| Rat[2] | 2 mg/kg | i.v. | 74 L/min/kg | 1.9 L/kg | 54 min | 0.6 μM·h | / |
| Rat[2] | 5 mg/kg | p.o. | / | / | / | 0-0.1 μM·h | 0-0.1 μM |
| Dog[2] | 2 mg/kg | i.v. | 11 mL/min/kg | 0.3 L/kg | 72 min | 4.1 μM·h | / |
| Dog[2] | 5 mg/kg | p.o. | / | / | / | 1.2 μM·h | 0.5 μM |
| Rhesus monkey[2] | 2 mg/kg | i.v. | 18 mL/min/kg | 0.4 L/kg | 78 min | 2.5 μM·h | / |
| Rhesus monkey[2] | 5 mg/kg | p.o. | / | / | / | 0.05-0.2 μM·h | 0.01-0.20 μM |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 923590-37-8
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性状 Solid
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分子量 757.94
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分子式 C38H55N5O9S
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Color White to off-white
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SMILES
O=S(NC([C@@]1(NC([C@H]2N(C([C@@H](NC(OCC(CCCC3)(C)C)=O)C(C)(C)C)=O)C[C@H](OC(N4CC5=C3C=CC=C5C4)=O)C2)=O)C[C@H]1CC)=O)(C6CC6)=O
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別名
MK-7009
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
純度とドキュメンテーション
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データシート (276 KB)
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SDS (418 KB)
- English - EN (418 KB)
- Français - FR (418 KB)
- Deutsch - DE (418 KB)
- Norwegian - NO (418 KB)
- Español - ES (418 KB)
- Swedish - SV (418 KB)
- Italian - IT (418 KB)
- Korean - KR (418 KB)
- Portuguese - PT (418 KB)
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取扱説明書 (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[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 c [Content Brief]
[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-m [Content Brief]
[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.Discove [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Vaniprevir 関連分類
HY-10243 関連分類
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