Faldaprevir
Based on 1 Customer Validation
Faldaprevir (BI 201335) is a potent, orally active and selective noncovalent inhibitor of NS3/4A protease of HCV (hepatitis C virus) genotypes 1a and 1b, with Ki values of 2.6 and 2.0 nM, respectively. Faldaprevir inhibits HCV RNA replication, with EC50 values of 6.5 and 3.1 nM, respectively. Faldaprevir has potent antiviral activity against chronic HCV infection.
For research use only. We do not sell to patients.
The Faldaprevir was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
- Purity : 98.58%
- CAS No.: 801283-95-4
- Formula: C40H49BrN6O9S
- Molecular Weight:869.82
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Storage:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | EC50 |
3.1 nM
Compound: BI 201335
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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
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[PMID: 20823284] |
| Huh-7 | EC50 |
43 nM
Compound: BI 201335
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Antiviral activity against HCV 2a infected in Huh7 cells assessed as inhibition of viral replication after 72 hrs by RT-PCR
Antiviral activity against HCV 2a infected in Huh7 cells assessed as inhibition of viral replication after 72 hrs by RT-PCR
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[PMID: 20823284] |
| Huh-7 | EC50 |
50 nM
Compound: BI 201335
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Antiviral activity against HCV 2a clone JFH1 infected in Huh7 cells assessed as inhibition of viral replication after 72 hrs by RT-PCR
Antiviral activity against HCV 2a clone JFH1 infected in Huh7 cells assessed as inhibition of viral replication after 72 hrs by RT-PCR
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[PMID: 20823284] |
| Huh-7 | EC50 |
6.5 nM
Compound: BI 201335
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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
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[PMID: 20823284] |
| Huh-7 | CC50 |
30 μM
Compound: BI 201335
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Cytotoxicity activity against human HuH7 cells by MTT assay
Cytotoxicity activity against human HuH7 cells by MTT assay
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[PMID: 20823284] |
| Huh-7 | EC50 |
6.5 nM
Compound: BI201335
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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
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[PMID: 24900813] |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 801283-95-4
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Appearance Solid
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Molecular Weight 869.82
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Formula C40H49BrN6O9S
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Color White to off-white
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SMILES
O=C([C@H](C[C@H]1OC2=CC(C3=CSC(NC(C(C)C)=O)=N3)=NC4=C2C=CC(OC)=C4Br)N(C1)C([C@H](C(C)(C)C)NC(OC5CCCC5)=O)=O)N[C@@]([C@@H]6C=C)(C6)C(O)=O
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Synonyms
BI 201335
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
In Vitro:
DMSO : 2 mg/mL (2.30 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
[1]. Llinàs-Brunet M, et al. Discovery of a potent and selective noncovalent linear inhibitor of the hepatitis C virus NS3 protease (BI 201335). J Med Chem. 2010 Sep 9;53(17):6466-76. [Content Brief]
[2]. Zeuzem S, et al. Faldaprevir (BI 201335), deleobuvir (BI 207127) and ribavirin oral therapy for treatment-naive HCV genotype 1: SOUND-C1 final results. Antivir Ther. 2013;18(8):1015-9. [Content Brief]
Complete Stock Solution Preparation Table
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 (protect from light, stored under nitrogen). 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 | 1.1497 mL | 5.7483 mL | 11.4966 mL | 28.7416 mL |
Faldaprevir Related Classifications
HY-15256 Related Classifications
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