BFB78
BFB78 is a blood-brain barrier-permeable nsP2 protease inhibitor. BFB78 potently and broadly inhibits the purified nsP2 proteases of various alphaviruses, with IC50 values ranging from 21.6 nM (Mayaro virus; MAYV) to 130.7 nM (Chikungunya virus; CHIKV). BFB78 blocks viral replication in cell culture systems and reduces viral titers in the brains of mice. BFB78 can be used in studies related to Venezuelan equine encephalitis virus (VEEV) 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。
- 分子式: C16H18N2O3S
- 分子量:318.39
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
BFB78 (49 h) inhibits viral replication of WEEV, VEEV and MAYV in cultured cells, with EC50 values of 1.1 μM, 1.6 μM and 1.2 μM, respectively[1].
BFB78 (72 h) exhibits low cytotoxicity in Hep G2 cells, SVG p12 astrocytes and Vero 76 cells, with CC50 values > 32 μM across all tested cell lines[1].
BFB78 (2 μM; 0-120 min) exhibits extremely high metabolic stability in mouse and human liver S9 fractions as well as microsomes, with a half-life of > 120 min in all tested metabolic systems[1].
BFB78 (5 μM) exhibits high permeability across MDCKII cell monolayers and shows low levels of P-gp-mediated efflux in MDR1-MDCKII cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Cmax | T1/2 | AUC0-∞ | Vz | CL | MRT |
|---|---|---|---|---|---|---|---|---|
| Mice[1] | 40 mg/kg | p.o. | 1353 ng/mL | 133 min | 175098 min·ng/mL | 43711 mL/kg | 228 mL/min/kg | 166 min |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C3H/HeN (Charles River, Strain 025; intranasally infected with VEEV TC-83 at 1×107 PFU)[1]
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Dosage:50 mg/kg
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Administration:i.p.; twice daily; until euthanasia criteria met or day 10 post-infection
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Result:Achieved 100% survival of treated mice until euthanasia on day 11 post-infection.
Reduced viral titers in mouse brain tissue by an average of more than 4 log10 compared with vehicle-treated animals.
Mitigated weight loss in infected mice relative to vehicle-treated and comparator-treated animals.
化学情報
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分子量 318.39
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分子式 C16H18N2O3S
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SMILES
C[C@H](NC(C1=CC=C(N1)C2=CC=CC=C2)=O)/C=C/S(C)(=O)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
BFB78 関連分類
HY-181969 関連分類
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- BFB78
- BFB 78
- BFB-78
- Virus Protease
- mouse liver phase I metabolic enzymes
- CHIKV
- blood-brain barrier
- mouse liver phase II metabolic enzymes
- human liver phase II metabolic enzymes
- alphaviruses
- human liver phase I metabolic enzymes
- nsP2 protease
- venezuelan equine encephalitis viral infection
- MAYV
- Inhibitor
- inhibitor
- inhibit