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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
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
- 화학식: C40H49BrN6O9S
- 분자량:869.82
-
보관:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | EC50 |
3.1 nM
Compound: BI 201335
|
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
|
[PMID: 20823284] |
| Huh-7 | EC50 |
43 nM
Compound: BI 201335
|
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
|
[PMID: 20823284] |
| Huh-7 | EC50 |
50 nM
Compound: BI 201335
|
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
|
[PMID: 20823284] |
| Huh-7 | EC50 |
6.5 nM
Compound: BI 201335
|
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
|
[PMID: 20823284] |
| Huh-7 | CC50 |
30 μM
Compound: BI 201335
|
Cytotoxicity activity against human HuH7 cells by MTT assay
Cytotoxicity activity against human HuH7 cells by MTT assay
|
[PMID: 20823284] |
| Huh-7 | EC50 |
6.5 nM
Compound: BI201335
|
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] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 801283-95-4
-
Appearance Solid
-
분자량 869.82
-
화학식 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
-
Synonyms
BI 201335
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선적
Room temperature in continental US; may vary elsewhere.
-
보관
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
용액&용해도
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)
순도&문서
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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 |