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

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Boceprevir (EBP 520) 是一种口服有效的选择性的 HCV NS3 protease 抑制剂，酶实验中K_i 为 14 nM，在含细胞体系的复制实验中，EC₉₀ 为 350 nM。Boceprevir 抑制 SARS-CoV-2 3CL^pro 活性。

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Boceprevir Chemical Structure

CAS No. : 394730-60-0

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥684	In-stock
5 mg	￥598	In-stock
10 mg	￥900	In-stock
25 mg	￥1591	In-stock
50 mg	￥2250	In-stock
100 mg	￥3375	In-stock
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Customer Review

Other Forms of Boceprevir:

Boceprevir-d₉ 询价
Boceprevir (Standard) 询价

MCE 顾客使用本产品发表的 32 篇科研文献

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.

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a K_i 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 3CL^pro activity^[6].

IC₅₀ & Target

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

细胞效力
(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]

体外研究
(In Vitro)

在 HCV NS3 蛋白酶连续测定中，Boceprevir (SCH 503034) 在大量运行中的平均效力为 14 nM (Ki)。在 HuH-7 细胞中进行 72 小时双顺反子亚基因组细胞复制子测定时，EC₅₀ 和 EC₉₀ 值分别测定为 0.20 μM 和 0.35 μM。 Boceprevir 还被发现是一种非常弱的 HNE 抑制剂 (Ki=26 μM)，选择性为 2200^[1]。

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

体内研究
(In Vivo)

Boceprevir，一种用于处理丙型肝炎病毒感染的 HCV 蛋白酶抑制剂。Boceprevir 的药代动力学特征在几种动物物种中进行了评估。口服给药后，Boceprevir 在大鼠 (10 mg/kg)、狗 (3 mg/kg) 和猴子 (3 mg/kg) 中被适度吸收。狗的吸收相对较快，但小鼠 (10 mg/kg)、大鼠和猴子的吸收较慢，平均吸收时间 (MAT) 为 0.5 至 1.4 小时。AUC 在狗和大鼠中良好，在小鼠中适中，在猴子中较低。绝对口服生物利用度在小鼠、大鼠和狗中适中 (26-34%)，但在猴子中较低 (4%)^[1]。Boceprevir (100 mg/kg，口服) 抑制三重转基因小鼠的 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 号

394730-60-0

性状

固体

颜色

White to off-white

中文名称

波普瑞韦；伯克匹韦；波塞匹韦

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

细胞实验：

DMSO 中的溶解度 : 180 mg/mL (346.37 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H₂O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制储备液

浓度溶剂体积质量	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
10 mM	0.1924 mL	0.9621 mL	1.9243 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

摩尔计算器
稀释计算器

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.67 mg/mL (3.21 mM); 澄清溶液

此方案可获得 ≥ 1.67 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 1.67 mg/mL (3.21 mM); 悬浊液; 超声助溶

此方案可获得 1.67 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 1.67 mg/mL (3.21 mM); 澄清溶液

此方案可获得 ≥ 1.67 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 98.79%

选择批次：

Data Sheet (652 KB) SDS (393 KB)

COA (205 KB) HNMR (463 KB) RP-HPLC (208 KB) MS (68 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Njoroge FG, et al. Challenges in modern drug discovery: a case study of boceprevir, an HCV protease inhibitor for the treatment of hepatitis C virus infection. Acc Chem Res. 2008 Jan;41(1):50-9. [Content Brief]

[2]. Yao M, et al. Conditional Inducible Triple-Transgenic Mouse Model for Rapid Real-Time Detection of HCV NS3/4A ProteaseActivity. PLoS One. 2016 Mar 4;11(3):e0150894. [Content Brief]

[3]. Coilly A, et al. Practical management of boceprevir and immunosuppressive therapy in liver transplant recipients with hepatitis C virus recurrence. Antimicrob Agents Chemother. 2012 Nov;56(11):5728-34. [Content Brief]

[4]. Berenguer M, et al. New developments in the management of hepatitis C virus infection: focus on boceprevir. Biologics. 2012;6:249-56. [Content Brief]

[5]. Burton MJ, et al. Telaprevir and boceprevir in african americans with genotype 1 chronic hepatitis C: implications for patients and providers. South Med J. 2012 Aug;105(8):431-6. [Content Brief]

[6]. Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212. [Content Brief]

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.
参考文献	[1]. Njoroge FG, et al. Challenges in modern drug discovery: a case study of boceprevir, an HCV protease inhibitor for the treatment of hepatitis C virus infection. Acc Chem Res. 2008 Jan;41(1):50-9. [Content Brief] [2]. Yao M, et al. Conditional Inducible Triple-Transgenic Mouse Model for Rapid Real-Time Detection of HCV NS3/4A ProteaseActivity. PLoS One. 2016 Mar 4;11(3):e0150894. [Content Brief] [3]. Coilly A, et al. Practical management of boceprevir and immunosuppressive therapy in liver transplant recipients with hepatitis C virus recurrence. Antimicrob Agents Chemother. 2012 Nov;56(11):5728-34. [Content Brief] [4]. Berenguer M, et al. New developments in the management of hepatitis C virus infection: focus on boceprevir. Biologics. 2012;6:249-56. [Content Brief] [5]. Burton MJ, et al. Telaprevir and boceprevir in african americans with genotype 1 chronic hepatitis C: implications for patients and providers. South Med J. 2012 Aug;105(8):431-6. [Content Brief] [6]. Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212. [Content Brief]

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.

参考文献

[1]. Njoroge FG, et al. Challenges in modern drug discovery: a case study of boceprevir, an HCV protease inhibitor for the treatment of hepatitis C virus infection. Acc Chem Res. 2008 Jan;41(1):50-9. [Content Brief]

[2]. Yao M, et al. Conditional Inducible Triple-Transgenic Mouse Model for Rapid Real-Time Detection of HCV NS3/4A ProteaseActivity. PLoS One. 2016 Mar 4;11(3):e0150894. [Content Brief]

[3]. Coilly A, et al. Practical management of boceprevir and immunosuppressive therapy in liver transplant recipients with hepatitis C virus recurrence. Antimicrob Agents Chemother. 2012 Nov;56(11):5728-34. [Content Brief]

[4]. Berenguer M, et al. New developments in the management of hepatitis C virus infection: focus on boceprevir. Biologics. 2012;6:249-56. [Content Brief]

[5]. Burton MJ, et al. Telaprevir and boceprevir in african americans with genotype 1 chronic hepatitis C: implications for patients and providers. South Med J. 2012 Aug;105(8):431-6. [Content Brief]

[6]. Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212. [Content Brief]

Boceprevir 相关分类

Infection

完整储备液配制表

可选溶剂	浓度溶剂体积质量	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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Boceprevir (Synonyms: 波普瑞韦; EBP 520; SCH 503034)

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

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MCE 顾客使用本产品发表的 32 篇科研文献

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