Name: Asunaprevir
Brand: Selleck Chemicals
SKU: S4935
Availability: InStock
Rating: 5 (8 reviews)

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	HDAC Caspase Proteasome Secretase MMP Cysteine Protease DPP Tyrosinase HIV Protease Serine Protease
Other HCV Protease Products	Lomibuvir (VX-222) Danoprevir PSI-6206 (GS-331007) 2'-C-Methylcytidine Tegobuvir Tizoxanide Herba taxilli Extract Mecarbinate

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (133.63 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (6.68mM)
	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	13.000mg/ml (17.37mM)
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

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%

Calculation results:

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.

Chemical Information, Storage & Stability

Molecular Weight	748.29	Formula	C₃₅H₄₆ClN₅O₉S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	630420-16-5	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	BMS-650032			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

Mechanism of Action

Targets/IC₅₀/Ki	1b (J4L6S) 0.3 nM 1a (H77) 0.7 nM 6a (HK-6A) 0.9 nM 4a (ED43) 1.6 nM 5a (SA13) 1.7 nM 2a (HC-J6) 15 nM 2b (HC-J8) 78 nM
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. This compound 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, it 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.
In vivo	Plasma and tissue exposures in vivo in several animal species indicate that this compound 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/22869577/ [2] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5397474/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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Asunaprevir HCV Protease inhibitor

Chemical Structure

Molecular Weight: 748.29