Cat. No.: HY-10242

Ciluprevir

(Synonyms: BILN 2061; BILN 2061ZW)

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Based on 1 Customer Validation

Ciluprevir (BILN 2061; BILN 2061ZW) is an orally active macrocyclic peptide inhibitor of hepatitis C virus (HCV)NS3 protease, with an IC₅₀ of 3 nM. Ciluprevir has Kᵢ values of 0.66 nM and 0.30 nM against genotypes 1b and 1a, respectively. Ciluprevir inhibits HCV RNA replication with an EC₅₀ of 1.2 nM, and its EC50 values against genotypes 1b and 1a are 3 nM and 4 nM, respectively. Ciluprevir shows no significant inhibition against human leukocyte elastase and hepatic cathepsin B. Ciluprevir can be used for genotype 1 HCV infection.

For research use only. We do not sell to patients.

Purity: 98.08%
CAS No.: 300832-84-2
Formula: C₄₀H₅₀N₆O₈S
Molecular Weight:774.93

Storage:

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

Ciluprevir Chemical Structure

CAS No.: 300832-84-2

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- Parmacokinetics
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All DNA/RNA Synthesis Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Huh-5-2	CC₅₀	>3 μM Compound: BILN-2061	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	0.04 μM Compound: BILN-2061	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	>0.1 μM Compound: 4; BILN 2061	Cytotoxicity against human HuH7 cell Cytotoxicity against human HuH7 cell	[PMID: 29477077]
Huh-7	CC₅₀	5.3 μM Compound: BILN-2061	Cytotoxicity against human Huh7.5 cells Cytotoxicity against human Huh7.5 cells	[PMID: 19896376]
Huh-7	CC₅₀	5.3 μM Compound: BILN-2061	Cytotoxicity against human Huh7.5 cells Cytotoxicity against human Huh7.5 cells	[PMID: 21440437]
Huh-7	EC₅₀	0.001 μM Compound: 3	Antiviral activity against HCV genotype 1b infected in Huh7 cells assessed as inhibition of viral replication by cell-based replicon assay Antiviral activity against HCV genotype 1b infected in Huh7 cells assessed as inhibition of viral replication by cell-based replicon assay	[PMID: 21601450]
Huh-7	EC₅₀	0.00163 μM Compound: 1, BILN-2061	Inhibition of HCV replication in human HuH7-Rep cells containing subgenomic bicistronic clone Inhibition of HCV replication in human HuH7-Rep cells containing subgenomic bicistronic clone	[PMID: 18722116]
Huh-7	EC₅₀	0.071 μM Compound: BILN-2061	Antiviral activity against Hepatitis C virus JFH-1 J6 infected in human HuH7.5 cells assessed as inhibition of virus propagation measured after 72 hrs of transfer to fresh media Antiviral activity against Hepatitis C virus JFH-1 J6 infected in human HuH7.5 cells assessed as inhibition of virus propagation measured after 72 hrs of transfer to fresh media	[PMID: 21440437]
Huh-7	EC₅₀	0.072 μM Compound: BILN-2061	Antiviral activity against Hepatitis C virus JFH-1 J6 infected in human HuH7.5 cells assessed as inhibition of virus propagation measured after 72 hrs Antiviral activity against Hepatitis C virus JFH-1 J6 infected in human HuH7.5 cells assessed as inhibition of virus propagation measured after 72 hrs	[PMID: 21440437]
Huh-7	EC₅₀	0.4 nM Compound: BILN-2061	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	0.4 nM Compound: BILN-2061	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	0.4 nM Compound: BILN-2061	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	0.5 nM Compound: BILN-2061	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	0.7 nM Compound: BILN-2061	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	0.8 nM Compound: BILN-2061	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	0.8 nM Compound: BILN-2061	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	0.8 nM Compound: BILN-2061	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	0.9 nM Compound: BILN-2061	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	1 nM Compound: BILN-2061	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	1 nM Compound: BILN-2061	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	1 nM Compound: BILN-2061	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	1.2 nM Compound: BILN-2061	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	1.4 nM Compound: BILN-2061	Antiviral activity against HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by qRT-PCR analysis Antiviral activity against HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by qRT-PCR analysis	[PMID: 20176894]
Huh-7	EC₅₀	1.4 nM Compound: BILN-2061	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	1.4 nM Compound: BILN-2061	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	1.4 nM Compound: BILN-2061	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	1.5 nM Compound: BILN-2061	Antiviral activity against cyclosporine A/NIM811-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by qRT-PCR analysis Antiviral activity against cyclosporine A/NIM811-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by qRT-PCR analysis	[PMID: 20176894]
Huh-7	EC₅₀	1.5 nM Compound: BILN-2061	Antiviral activity against wild-type Hepatitis C virus genotype 1b N infected in human Huh7 cells Antiviral activity against wild-type Hepatitis C virus genotype 1b N infected in human Huh7 cells	[PMID: 18086851]
Huh-7	EC₅₀	1.7 nM Compound: BILN-2061	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	1002 nM Compound: BILN-2061	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	1039 nM Compound: BILN-2061	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	1066 nM Compound: BILN-2061	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	1518 nM Compound: BILN-2061	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]
Huh-7	EC₅₀	18 nM Compound: BILN-2061	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	1813 nM Compound: BILN-2061	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	2.3 nM Compound: BILN-2061	Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q41R mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay Antiviral activity against Hepatitis C virus subtype 1b expressing NS3 Q41R mutant infected in HuH7 cells after 48 hrs by by luciferase reporter assay	[PMID: 20176898]
Huh-7	EC₅₀	2.4 nM Compound: BILN-2061	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	2.8 nM Compound: 3, BILN-2061	Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human Huh7 cells assessed as inhibition of NS4A expression by ELISA Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human Huh7 cells assessed as inhibition of NS4A expression by ELISA	[PMID: 25155387]
Huh-7	EC₅₀	20715 nM Compound: BILN-2061	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	2099 nM Compound: BILN-2061	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	215 nM Compound: BILN-2061	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	22 nM Compound: BILN-2061	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	248 nM Compound: BILN-2061	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	29 nM Compound: BILN-2061	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	3 nM Compound: BILN-2061	Antiviral activity against HCV 1a containing chimeric genotype 1a-H77/1b-con1 subgenom in human Huh7 cells assessed as reduction in viral RNA after 7 days by RT-PCR Antiviral activity against HCV 1a containing chimeric genotype 1a-H77/1b-con1 subgenom in human Huh7 cells assessed as reduction in viral RNA after 7 days by RT-PCR	[PMID: 19226162]
Huh-7	EC₅₀	3 nM Compound: BILN-2061	Antiviral activity against HCV isolate Con1 in human Huh7 cells assessed as reduction in viral RNA after 7 days by RT-PCR Antiviral activity against HCV isolate Con1 in human Huh7 cells assessed as reduction in viral RNA after 7 days by RT-PCR	[PMID: 19226162]
Huh-7	EC₅₀	3 nM Compound: BILN-2061	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	304 nM Compound: BILN-2061	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	35 nM Compound: BILN-2061	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	4 nM Compound: BILN 2061	Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7 cells by subgenomic replicon-based luciferase assay Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7 cells by subgenomic replicon-based luciferase assay	[PMID: 24900813]
Huh-7	EC₅₀	4 nM Compound: Ciluprevir, BILN-2061	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	4.8 nM Compound: BILN-2061	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	40 nM Compound: BILN-2061	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	489 nM Compound: BILN-2061	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	5.8 nM Compound: BILN-2061	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	52 nM Compound: BILN-2061	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	520 nM Compound: BILN-2061	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	685 nM Compound: BILN-2061	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	705 nM Compound: BILN-2061	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	707 nM Compound: BILN-2061	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	84 nM Compound: BILN-2061	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	87 nM Compound: BILN-2061	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]

In Vitro

Ciluprevir potently inhibits viral replication in Huh-7 hepatoma cells harboring HCV genotype 1b subgenomic NS2-NS5b replicons^[3].

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

Parmacokinetics

Species	Dose	Route	C_max	AUC_0-∞	F	T_1/2	V_ss	CL
Rat^[1]	20 mg/kg	p.o.	2.5 μM	12.5 μM·h	42 %	/	/	/
Rat^[1]	5 mg/kg	i.v.	/	/	42 %	1.3 h	1.0 L/kg	13 mL/min/kg

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 300832-84-2
Appearance Solid
Molecular Weight 774.93
Formula C₄₀H₅₀N₆O₈S
Color Light yellow to yellow
SMILES

O=C1N2C[C@@H](C[C@]2(C(N[C@@]3(C[C@]3(/C=C\CCCCC[C@@H]1NC(OC4CCCC4)=O)[H])C(O)=O)=O)[H])OC5=CC(C6=CSC(NC(C)C)=N6)=NC7=CC(OC)=CC=C75
Synonyms

BILN 2061; BILN 2061ZW
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 12.5 mg/mL (16.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.2904 mL

6.4522 mL

12.9044 mL

5 mM

0.2581 mL

1.2904 mL

2.5809 mL

10 mM

0.1290 mL

0.6452 mL

1.2904 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
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- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Llinàs-Brunet M, et al. Structure-activity study on a novel series of macrocyclic inhibitors of the hepatitis C virus NS3 protease leading to the discovery of BILN 2061. J Med Chem. 2004;47(7):1605-1608. [Content Brief]

[2]. Lamarre D, et al. An NS3 protease inhibitor with antiviral effects in humans infected with hepatitis C virus. Nature. 2003 Nov 13;426(6963):186-9.
[Content Brief]

[3]. Reiser M, et al. Antiviral efficacy of NS3-serine protease inhibitor BILN-2061 in patients with chronic genotype 2 and 3 hepatitis C. Hepatology. 2005 Apr;41(4):832-5.
[Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.2904 mL	6.4522 mL	12.9044 mL	32.2610 mL
	5 mM	0.2581 mL	1.2904 mL	2.5809 mL	6.4522 mL
	10 mM	0.1290 mL	0.6452 mL	1.2904 mL	3.2261 mL
	15 mM	0.0860 mL	0.4301 mL	0.8603 mL	2.1507 mL

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Ciluprevir

Macrocyclic Compound Library

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

All DNA/RNA Synthesis Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Ciluprevir

Macrocyclic Compound Library

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

All DNA/RNA Synthesis Isoforms

Biological Activity

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References

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Complete Stock Solution Preparation Table

Ciluprevir Related Classifications

HY-10242 Related Classifications