2. Anti-infection
  3. Virus Protease
  4. 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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BFB78

BFB78 Chemical Structure

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BFB78 Related Antibodies

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Description

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[1].

In Vitro

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.

BFB78 Related Antibodies
Parmacokinetics
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
In Vivo

BFB78 (50 mg/kg; i.p.; twice daily for 10 days) provides 100% therapeutic efficacy in a lethal VEEV TC-83 mouse model, with greater than 4 log10 reduction in average brain viral titers[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C3H/HeN (Charles River, Strain 025; intranasally infected with VEEV TC-83 at 1×107 PFU)[1]
Dosage: 50 mg/kg
Administration: i.p.; twice daily; until euthanasia criteria met or day 10 post-infection
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.
Molecular Weight

318.39

Formula

C16H18N2O3S
SMILES

C[C@H](NC(C1=CC=C(N1)C2=CC=CC=C2)=O)/C=C/S(C)(=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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BFB78 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BFB78BFB 78BFB-78Virus Proteasemouse liver phase I metabolic enzymesCHIKVblood-brain barriermouse liver phase II metabolic enzymeshuman liver phase II metabolic enzymesalphaviruseshuman liver phase I metabolic enzymesnsP2 proteasevenezuelan equine encephalitis viral infectionMAYVInhibitorinhibitorinhibit

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