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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
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.
- 純度 : 98.58%
- CAS 番号: 801283-95-4
- 分子式: C40H49BrN6O9S
- 分子量:869.82
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保管条件:
-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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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
製品説明
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] |
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 801283-95-4
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性状 Solid
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分子量 869.82
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分子式 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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別名
BI 201335
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶剤 & 溶解度
体外:
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
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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.
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
[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 関連分類
HY-15256 関連分類
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