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.
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- 화학식: C16H18N2O3S
- 분자량:318.39
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보관:
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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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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.
Chemical Information
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분자량 318.39
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BFB78 Related Classifications
HY-181969 Related Classifications
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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