Home Proteases HCV Protease inhibitor Asunaprevir For research use only.

Asunaprevir

Synonyms: BMS-650032

Asunaprevir is an orally bioavailable inhibitor of the hepatitis C virus enzyme serine protease NS3 that is necessary for protein processing required for viral replication.

Asunaprevir Chemical Structure

Asunaprevir Chemical Structure

CAS: 630420-16-5

Selleck's Asunaprevir has been cited by 6 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
genotype 1b con1 replicon cells Function assay Inhibition of recombinant full length HCV genotype 4a ED43 NS3 protease in genotype 1b con1 replicon cells by luciferase reporter gene assay, EC50=0.0017μM 27564532
Huh7.5 cells Antiviral assay Antiviral activity against HCV genotype 1b Con1 expressing NS3 protease infected in human Huh7.5 cells assessed as reduction in viral RNA replication by luciferase reporter gene assay, EC50=0.003μM 27564532
HCV replicon cells Antiviral assay Antiviral activity against HCV genotype 1a H77 in HCV replicon cells assessed as reduction in viral RNA replication by luciferase reporter gene assay, EC50=0.004μM 27564532
HCV replicon cells Antiviral assay Antiviral activity against HCV genotype 2a JHF-1 in HCV replicon cells assessed as reduction in viral RNA replication by luciferase reporter gene assay, EC50=0.217μM 27564532
genotype 2a replicon cells Function assay Inhibition of recombinant full length HCV genotype 2b HC-J8 NS3 protease in genotype 2a replicon cells by luciferase reporter gene assay, EC50=0.621μM 27564532
genotype 2a replicon cells Function assay Inhibition of recombinant full length HCV genotype 3a S52 NS3 protease in genotype 2a replicon cells by luciferase reporter gene assay, EC50=1.1μM 27564532
HuH7 cells Antiviral assay 3 days Antiviral activity against HCV genotype 1b infected in human HuH7 cells at >= 10 times antiviral EC50 after 3 days by luciferase reporter assay 28430437
HuH7 cells Antiviral assay 3 days Antiviral activity against HCV genotype 1b infected in human HuH7 cells co-treated with daclatasvir after 3 days by luciferase reporter assay 28430437
HuH7 replicon cells Function assay 4 days Inhibition of HCV genotype 1b Con1 NS3 protease infected in human HuH7 replicon cells assessed as reduction in viral replication after 4 days by luciferase reporter gene assay, EC50=0.0012μM 29162454
HuH7 replicon cells Function assay 4 days Inhibition of HCV genotype 1a H77 NS3 protease infected in human HuH7 replicon cells assessed as reduction in viral replication after 4 days by luciferase reporter gene assay, EC50=0.004μM 29162454
HuH7.5 cells Antiviral assay 4 days Antiviral activity against HCV genotype 1b Con1 infected in human HuH7.5 cells assessed as inhibition of viral replication after 4 days by luciferase reporter gene assay, EC50=0.006μM 29456803
Huh7.5 replicon cells Antiviral assay 4 days Antiviral activity against HCV genotype 1b infected in human Huh7.5 replicon cells assessed as reduction in viral replication incubated for 4 days by luciferase reporter gene assay, EC50=0.006μM 29650290
Click to View More Cell Line Experimental Data

Biological Activity

Description Asunaprevir is an orally bioavailable inhibitor of the hepatitis C virus enzyme serine protease NS3 that is necessary for protein processing required for viral replication.
Targets
1b (J4L6S) [1] 1a (H77) [1] 6a (HK-6A) [1] 4a (ED43) [1] 5a (SA13) [1] Click to View More Targets
0.3 nM 0.7 nM 0.9 nM 1.6 nM 1.7 nM
In vitro
In vitro Asunaprevir (ASV) competitively binds to the NS3/4A protease complex, with Ki values of 0.4 and 0.24 nM against recombinant enzymes representing genotypes 1a (H77) and 1b (J4L6S), respectively. Asunaprevir is high selective without any significant activity against the closely related GB virus-B NS3 protease and a panel of human serine or cysteine proteases. In cell culture, ASV inhibits replication of HCV replicons representing genotypes 1 and 4, with 50% effective concentrations (EC50s) ranging from 1 to 4 nM, and has weaker activity against genotypes 2 and 3 (EC50, 67-1162 nM). Selectivity is again demonstrated by the absence of activity (EC50, >12 μM) against a panel of other RNA viruses[1].
Cell Research Cell lines Huh 7.5.1 cells
Concentrations 1 or 10 nM
Incubation Time 3, 6, 24, and 48 h
Method

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In Vivo
In vivo Plasma and tissue exposures in vivo in several animal species indicate that ASV displays a hepatotropic disposition (liver-to-plasma ratios ranging from 40- to 359-fold across species). Twenty-four hours postdose, liver exposures across all species tested are ≥110-fold above the inhibitor EC50s observed with HCV genotype-1 replicons[1].
Animal Research Animal Models male FVB mice, Sprague-Dawley rats, male beagles, male cynomolgus monkeys
Dosages 5 mg/kg (mice); 3, 5, 10, and 15 mg/kg (rats); 3 or 6 mg/kg (Dogs); 3 mg/kg (Monkeys)
Administration by oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03208322 Withdrawn Hepatitis C Bristol-Myers Squibb November 30 2018 --
NCT03004625 Completed Hepatitis C Kaohsiung Medical University Chung-Ho Memorial Hospital|Chang Gung Memorial Hospital|National Taiwan University Hospital|Taipei Veterans General Hospital Taiwan|China Medical University Hospital|National Cheng-Kung University Hospital November 2016 Phase 3
NCT02865369 Unknown status Chronic Hepatitis C Sang Gyune Kim|Seoul National University Boramae Hospital|Severance Hospital|Inha University Hospital|Korea University|Gachon University Gil Medical Center|Hanyang University Seoul Hospital|Ewha Womans University Mokdong Hospital|Bristol-Myers Squibb|Soonchunhyang University Hospital September 2016 --
NCT02580474 Completed Hepatitis C Myeong Jun Song|Bristol-Myers Squibb|Soonchunhyang University Hospital|Dankook University|Chungnam National University Hospital|Konyang University Hospital|Eulji University Hospital|Saint Vincent''s Hospital Korea|Konkuk University Hospital|Cheongju St. Mary''s Hospital Cheongju Korea|Severance Hospital|Korea University Guro Hospital|Eulji General Hospital|The Catholic University of Korea February 2016 Phase 4
NCT02496078 Completed Hepatitis C Bristol-Myers Squibb August 2015 Phase 3
NCT02309450 Withdrawn Hepatitis C Virus Genotype 4 Infection ANRS Emerging Infectious Diseases|Bristol-Myers Squibb December 2014 Phase 2

Chemical lnformation & Solubility

Molecular Weight 748.29 Formula

C35H46ClN5O9S
CAS No. 630420-16-5 SDF --
Smiles CC(C)(C)C(C(=O)N1CC(CC1C(=O)NC2(CC2C=C)C(=O)NS(=O)(=O)C3CC3)OC4=NC=C(C5=C4C=C(C=C5)Cl)OC)NC(=O)OC(C)(C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (133.63 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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