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  1. Anti-infection Metabolic Enzyme/Protease
  2. HCV Protease HCV SARS-CoV
  3. Boceprevir

Boceprevir  (Synonyms: 波普瑞韋; EBP 520; SCH 503034)

目錄號: HY-10237 純度: 98.79%
COA 產(chǎn)品使用指南

Boceprevir (EBP 520) 是一種口服有效的選擇性的 HCV NS3 protease 抑制劑,酶實(shí)驗(yàn)中Ki 為 14 nM,在含細(xì)胞體系的復(fù)制實(shí)驗(yàn)中,EC90 為 350 nM。Boceprevir 抑制 SARS-CoV-2 3CLpro 活性。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào),我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Boceprevir Chemical Structure

Boceprevir Chemical Structure

CAS No. : 394730-60-0

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Customer Review

Other Forms of Boceprevir:

MCE 顧客使用本產(chǎn)品發(fā)表的 32 篇科研文獻(xiàn)

WB
Proliferation Assay

    Boceprevir purchased from MCE. Usage Cited in: Antimicrob Agents Chemother. 2015 Dec;59(12):7666-7670.  [Abstract]

    Effects of antiviral drugs on cellular uptake of fluorescein by BeWo cells. The cells are incubated with 1 μM fluorescein in the presence of 100 μM compounds for 10 min at 37°C.

    Boceprevir purchased from MCE. Usage Cited in: Virology. 2014 May;456-457:300-9.  [Abstract]

    Jurkat cells are transfected with plasmids expressing (A) HCV NS3/4A or (B) HPgV NS3/4AB-HA. Telaprevir, Boceprevir, and Danoprevir are added at concentrations of 100 μM, 16.6 μM, 2.7 μM, or 0 μM in 0.1% DMSO. Lysates are harvested after 24 h and resolved by immunoblots probed with anti-HCV NS3 (A) or anti-HA (B). The position of HCV NS3/4A (~75kDa), HCV NS3 (~73kDa), NS3/4AB-HA, and NS4B-HA (~30kDa) are indicated. Molecular markers are on the right.
    • 生物活性

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a Ki of 14 nM in both enzyme assay and an EC90 of 350 nM in cell-based replicon assay[1][2][3][4][5]. Boceprevir inhibits SARS-CoV-2 3CLpro activity[6].

    IC50 & Target

    Ki: 14 nM (HCV NS3 protease)[1]

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    Hepatocyte CC50
    > 5 μM
    Compound: 1, SCH-503034, boceprevir
    Cytotoxicity against human hepatocytes assessed as effect on GAPDH RNA level by MTS assay
    Cytotoxicity against human hepatocytes assessed as effect on GAPDH RNA level by MTS assay
    [PMID: 19456105]
    Huh-5-2 CC50
    > 33 μM
    Compound: SCH-503034
    Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay
    Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay
    [PMID: 18625766]
    Huh-5-2 EC50
    1.4 μM
    Compound: SCH-503034
    Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh5-2 cells assessed as reduction in replicon RNA after 4 days by luciferase assay
    Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh5-2 cells assessed as reduction in replicon RNA after 4 days by luciferase assay
    [PMID: 18625766]
    Huh-7 CC50
    > 100 μM
    Compound: SCH503034
    Cytotoxicity against human Huh7.5 cells assessed as cell viability after 48 hrs by Alamar blue assay
    Cytotoxicity against human Huh7.5 cells assessed as cell viability after 48 hrs by Alamar blue assay
    [PMID: 23583031]
    Huh-7 CC50
    > 70000 nM
    Compound: Boceprevir
    Cytotoxicity activity against human HuH7 cells by MTT assay
    Cytotoxicity activity against human HuH7 cells by MTT assay
    [PMID: 20823284]
    Huh-7 EC50
    0.8 μM
    Compound: SCH503034
    Antiviral activity against Hepatitis C virus subtype 2a J6/JFH transfected in human Huh7.5 cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay
    Antiviral activity against Hepatitis C virus subtype 2a J6/JFH transfected in human Huh7.5 cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay
    [PMID: 23583031]
    Huh-7 EC50
    100 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168A mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168A mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    101 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168N mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168N mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    1077 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80K and R155K mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80K and R155K mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    110 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 V36L mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 V36L mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    1106 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 T54S mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 T54S mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    113 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80R and D168A mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80R and D168A mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    127 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80G mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80G mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    1328 nM
    Compound: Boceprevir, SCH-503034
    Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7 cells assessed as GAPDH RNA or 18S rRNA level after 3 days selected with 40 uM HCV-796 and 400 nM boceprevir by qRT-PCR analysis
    Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7 cells assessed as GAPDH RNA or 18S rRNA level after 3 days selected with 40 uM HCV-796 and 400 nM boceprevir by qRT-PCR analysis
    [PMID: 18936191]
    Huh-7 EC50
    133 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80L mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80L mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    1454 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 V36A mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 V36A mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    148 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing WT NS3 infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    1546 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 V170A mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 V170A mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    1554 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 F43S and Q80R mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 F43S and Q80R mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    1577 nM
    Compound: Boceprevir, SCH-503034
    Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7 cells assessed as GAPDH RNA or 18S rRNA level after 3 days selected with 40 nM HCV-796 and 800 nM boceprevir by qRT-PCR analysis
    Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7 cells assessed as GAPDH RNA or 18S rRNA level after 3 days selected with 40 nM HCV-796 and 800 nM boceprevir by qRT-PCR analysis
    [PMID: 18936191]
    Huh-7 EC50
    16 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 S138T mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 S138T mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    165 nM
    Compound: Boceprevir, SCH-503034
    Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7 cells assessed as GAPDH RNA or 18S rRNA level after 3 days by qRT-PCR analysis
    Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7 cells assessed as GAPDH RNA or 18S rRNA level after 3 days by qRT-PCR analysis
    [PMID: 18936191]
    Huh-7 EC50
    174 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155Q mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155Q mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    193 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168Y mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168Y mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    1937 nM
    Compound: Boceprevir, SCH-503034
    Antiviral activity against Hepatitis C virus genotype 1b Con1 harboring NS3 G282S mutant infected in human HuH7.5 cells after 72 hrs by gaussia luciferase reporter assay
    Antiviral activity against Hepatitis C virus genotype 1b Con1 harboring NS3 G282S mutant infected in human HuH7.5 cells after 72 hrs by gaussia luciferase reporter assay
    [PMID: 18936191]
    Huh-7 EC50
    20 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80H and D168E mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80H and D168E mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    200 nM
    Compound: 2, SCH-503034
    Antiviral activity against HCV replication infected in human HuH7 cells after 72 hrs by replicon assay in presence of 5% FCS
    Antiviral activity against HCV replication infected in human HuH7 cells after 72 hrs by replicon assay in presence of 5% FCS
    [PMID: 19285390]
    Huh-7 EC50
    200 nM
    Compound: Boceprevir, SCH-503034
    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
    [PMID: 20541424]
    Huh-7 EC50
    201.2 nM
    Compound: SCH-503034, Boceprevir
    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
    [PMID: 20855726]
    Huh-7 EC50
    210 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 V170T mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 V170T mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    2152 nM
    Compound: Boceprevir, SCH-503034
    Antiviral activity against Hepatitis C virus genotype 1b Con1 harboring NS3 E176G mutant infected in human HuH7.5 cells after 72 hrs by gaussia luciferase reporter assay
    Antiviral activity against Hepatitis C virus genotype 1b Con1 harboring NS3 E176G mutant infected in human HuH7.5 cells after 72 hrs by gaussia luciferase reporter assay
    [PMID: 18936191]
    Huh-7 EC50
    217 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 V36M mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 V36M mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    242 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 F43I mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 F43I mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    268 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 T54A mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 T54A mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    275.8 nM
    Compound: SCH-503034, Boceprevir
    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
    [PMID: 20855726]
    Huh-7 EC50
    279 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168I mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168I mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    299 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168T mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168T mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    3170 nM
    Compound: Boceprevir, SCH-503034
    Antiviral activity against Hepatitis C virus genotype 1b Con1 harboring NS3 V170A mutant infected in human HuH7.5 cells after 72 hrs by gaussia luciferase reporter assay
    Antiviral activity against Hepatitis C virus genotype 1b Con1 harboring NS3 V170A mutant infected in human HuH7.5 cells after 72 hrs by gaussia luciferase reporter assay
    [PMID: 18936191]
    Huh-7 EC50
    33 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R109K mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R109K mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    333 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 F43S mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 F43S mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    377 nM
    Compound: Boceprevir, SCH-503034
    Antiviral activity against Hepatitis C virus genotype 1b Con1 harboring NS3 V158M mutant infected in human HuH7.5 cells after 72 hrs by gaussia luciferase reporter assay
    Antiviral activity against Hepatitis C virus genotype 1b Con1 harboring NS3 V158M mutant infected in human HuH7.5 cells after 72 hrs by gaussia luciferase reporter assay
    [PMID: 18936191]
    Huh-7 EC50
    417 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 F43S and D168E mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 F43S and D168E mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    4362 nM
    Compound: Boceprevir, SCH-503034
    Antiviral activity against Hepatitis C virus genotype 1b Con1 harboring V170A and C316Y mutations mutant infected in human HuH7.5 cells after 72 hrs by gaussia luciferase reporter assay
    Antiviral activity against Hepatitis C virus genotype 1b Con1 harboring V170A and C316Y mutations mutant infected in human HuH7.5 cells after 72 hrs by gaussia luciferase reporter assay
    [PMID: 18936191]
    Huh-7 EC50
    4467 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155G mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155G mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    520 nM
    Compound: Boceprevir
    Antiviral activity against HCV 1b infected in Huh7 cells assessed as inhibition of viral replication after 72 hrs by RT-PCR
    Antiviral activity against HCV 1b infected in Huh7 cells assessed as inhibition of viral replication after 72 hrs by RT-PCR
    [PMID: 20823284]
    Huh-7 EC50
    525 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 A156S mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 A156S mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    527 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 F43V mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 F43V mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    5343 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155I mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155I mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    5463 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155T mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155T mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    550 nM
    Compound: Boceprevir
    Antiviral activity against HCV 1a infected in Huh7 cells assessed as inhibition of viral replication after 72 hrs by RT-PCR
    Antiviral activity against HCV 1a infected in Huh7 cells assessed as inhibition of viral replication after 72 hrs by RT-PCR
    [PMID: 20823284]
    Huh-7 EC50
    608 nM
    Compound: Boceprevir, SCH-503034
    Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7.5 cells after 72 hrs by gaussia luciferase reporter assay
    Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human HuH7.5 cells after 72 hrs by gaussia luciferase reporter assay
    [PMID: 18936191]
    Huh-7 EC50
    62 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80R and D168E mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80R and D168E mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    63 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168G mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168G mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    647 nM
    Compound: Boceprevir, SCH-503034
    Antiviral activity against Hepatitis C virus genotype 1b Con1 harboring NS5B I424V mutant infected in human HuH7.5 cells after 72 hrs by gaussia luciferase reporter assay
    Antiviral activity against Hepatitis C virus genotype 1b Con1 harboring NS5B I424V mutant infected in human HuH7.5 cells after 72 hrs by gaussia luciferase reporter assay
    [PMID: 18936191]
    Huh-7 EC50
    65 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 A156G mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 A156G mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    680 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80R and R155K mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80R and R155K mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    69 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168E mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168E mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    7227 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 A156T mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 A156T mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    73 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168H mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168H mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    738 nM
    Compound: Boceprevir, SCH-503034
    Antiviral activity against Hepatitis C virus genotype 1b Con1 harboring NS3 K583T mutant infected in human HuH7.5 cells after 72 hrs by gaussia luciferase reporter assay
    Antiviral activity against Hepatitis C virus genotype 1b Con1 harboring NS3 K583T mutant infected in human HuH7.5 cells after 72 hrs by gaussia luciferase reporter assay
    [PMID: 18936191]
    Huh-7 EC50
    743 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155K mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155K mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    78 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80H mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80H mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    781 nM
    Compound: Boceprevir, SCH-503034
    Antiviral activity against Hepatitis C virus genotype 1b Con1 harboring NS5B C316Y mutant infected in human HuH7.5 cells after 72 hrs by gaussia luciferase reporter assay
    Antiviral activity against Hepatitis C virus genotype 1b Con1 harboring NS5B C316Y mutant infected in human HuH7.5 cells after 72 hrs by gaussia luciferase reporter assay
    [PMID: 18936191]
    Huh-7 EC50
    792 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155M mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 R155M mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    795 nM
    Compound: Boceprevir, SCH-503034
    Antiviral activity against Hepatitis C virus genotype 1b Con1 harboring NS5B C445F mutant infected in human HuH7.5 cells after 72 hrs by gaussia luciferase reporter assay
    Antiviral activity against Hepatitis C virus genotype 1b Con1 harboring NS5B C445F mutant infected in human HuH7.5 cells after 72 hrs by gaussia luciferase reporter assay
    [PMID: 18936191]
    Huh-7 EC50
    821 nM
    Compound: Boceprevir, SCH-503034
    Antiviral activity against Hepatitis C virus genotype 1b Con1 harboring C316Y and C445F mutations mutant infected in human HuH7.5 cells after 72 hrs by gaussia luciferase reporter assay
    Antiviral activity against Hepatitis C virus genotype 1b Con1 harboring C316Y and C445F mutations mutant infected in human HuH7.5 cells after 72 hrs by gaussia luciferase reporter assay
    [PMID: 18936191]
    Huh-7 EC50
    83 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168V mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 D168V mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    85 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80R mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80R mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    91.5 nM
    Compound: SCH-503034, Boceprevir
    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
    [PMID: 20855726]
    Huh-7 EC50
    94 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80K mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q80K mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    Huh-7 EC50
    9673 nM
    Compound: Boceprevir
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 A156V mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 A156V mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay
    [PMID: 20176898]
    體外研究
    (In Vitro)

    HCV NS3 蛋白酶連續(xù)測定中,Boceprevir (SCH 503034) 在大量運(yùn)行中的平均效力為 14 nM (Ki)。在 HuH-7 細(xì)胞中進(jìn)行 72 小時(shí)雙順反子亞基因組細(xì)胞復(fù)制子測定時(shí),EC50 和 EC90 值分別測定為 0.20 μM 和 0.35 μM。 Boceprevir 還被發(fā)現(xiàn)是一種非常弱的 HNE 抑制劑 (Ki=26 μM),選擇性為 2200[1]。

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

    體內(nèi)研究
    (In Vivo)

    Boceprevir,一種用于處理丙型肝炎病毒感染的 HCV 蛋白酶抑制劑。Boceprevir 的藥代動(dòng)力學(xué)特征在幾種動(dòng)物物種中進(jìn)行了評估??诜o藥后,Boceprevir 在大鼠 (10 mg/kg)、狗 (3 mg/kg) 和猴子 (3 mg/kg) 中被適度吸收。狗的吸收相對較快,但小鼠 (10 mg/kg)、大鼠和猴子的吸收較慢,平均吸收時(shí)間 (MAT) 為 0.5 至 1.4 小時(shí)。AUC 在狗和大鼠中良好,在小鼠中適中,在猴子中較低。絕對口服生物利用度在小鼠、大鼠和狗中適中 (26-34%),但在猴子中較低 (4%)[1]。Boceprevir (100 mg/kg,口服) 抑制三重轉(zhuǎn)基因小鼠的 HCV NS3/4A 蛋白酶活性[2]。

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

    Clinical Trial
    分子量

    519.68

    Formula

    C27H45N5O5

    CAS 號
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    波普瑞韋;伯克匹韋;波塞匹韋

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.

    儲存方式
    Powder -20°C 3 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn): 

    DMSO 中的溶解度 : 180 mg/mL (346.37 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 1.9243 mL 9.6213 mL 19.2426 mL
    5 mM 0.3849 mL 1.9243 mL 3.8485 mL
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時(shí),請?jiān)?個(gè)月內(nèi)使用,-20°C儲存時(shí),請?jiān)?個(gè)月內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動(dòng)物實(shí)驗(yàn):

    請根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1.67 mg/mL (3.21 mM); 澄清溶液

      此方案可獲得 ≥ 1.67 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 16.7 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 1.67 mg/mL (3.21 mM); 懸濁液; 超聲助溶

      此方案可獲得 1.67 mg/mL的均勻懸濁液,懸濁液可用于口服和腹腔注射。

      1 mL 工作液為例,取 100 μL 16.7 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

      2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。
    動(dòng)物溶解方案計(jì)算器
    請輸入動(dòng)物實(shí)驗(yàn)的基本信息:

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    由于實(shí)驗(yàn)過程有損耗,建議您多配一只動(dòng)物的量
    請輸入您的動(dòng)物體內(nèi)配方組成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購。 ,Tween 80,均可在 MCE 網(wǎng)站選購。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
    您所需的儲備液濃度超過該產(chǎn)品的實(shí)測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術(shù)支持聯(lián)系。
    動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液,加入 μL 。 μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上,請謹(jǐn)慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 98.79%

    參考文獻(xiàn)
    Animal Administration
    [2]

    Mice[2]
    Boceprevir is purchased from MedChem Express. To evaluate the effect of Boceprevir, triple-transgenic mice are induced with Doxycycline (Dox) for 10 days (n=5 per group). On the third day after Dox induction, when plasma Gluc activity reaches its peak, the mice are administered either Boceprevir (100 mg/kg) or DMSO via oral gavage twice daily for 7 days. During this period, blood is collected from the caudal vein daily to detect plasma Gluc activity.

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

    參考文獻(xiàn)

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時(shí),請?jiān)?個(gè)月內(nèi)使用,-20°C儲存時(shí),請?jiān)?個(gè)月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9243 mL 9.6213 mL 19.2426 mL 48.1065 mL
    5 mM 0.3849 mL 1.9243 mL 3.8485 mL 9.6213 mL
    10 mM 0.1924 mL 0.9621 mL 1.9243 mL 4.8107 mL
    15 mM 0.1283 mL 0.6414 mL 1.2828 mL 3.2071 mL
    20 mM 0.0962 mL 0.4811 mL 0.9621 mL 2.4053 mL
    25 mM 0.0770 mL 0.3849 mL 0.7697 mL 1.9243 mL
    30 mM 0.0641 mL 0.3207 mL 0.6414 mL 1.6036 mL
    40 mM 0.0481 mL 0.2405 mL 0.4811 mL 1.2027 mL
    50 mM 0.0385 mL 0.1924 mL 0.3849 mL 0.9621 mL
    60 mM 0.0321 mL 0.1604 mL 0.3207 mL 0.8018 mL
    80 mM 0.0241 mL 0.1203 mL 0.2405 mL 0.6013 mL
    100 mM 0.0192 mL 0.0962 mL 0.1924 mL 0.4811 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Inquiry Information

    產(chǎn)品名稱:
    Boceprevir
    目錄號:
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