1. Anti-infection Metabolic Enzyme/Protease
  2. HCV HCV Protease
  3. Ciluprevir

Ciluprevir  (Synonyms: BILN 2061; BILN 2061ZW)

Cat. No.: HY-10242
Handling Instructions

Ciluprevir(BILN 2061) is a specific and potent peptidomimetic inhibitor of the HCV NS3 protease with an IC50 of 3.0 nM.

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

Ciluprevir Chemical Structure

Ciluprevir Chemical Structure

CAS No. : 300832-84-2

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Description

Ciluprevir(BILN 2061) is a specific and potent peptidomimetic inhibitor of the HCV NS3 protease with an IC50 of 3.0 nM.

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 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
0.071 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 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
0.4 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
0.5 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 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
0.8 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
0.9 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 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 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
1.2 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 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
1.4 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 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
1.5 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
1.7 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]
Clinical Trial
Molecular Weight

774.93

Formula

C40H50N6O8S

CAS No.
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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    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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