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BMS-433771 

Cat. No. M30272
BMS-433771  Structure
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Biological Activity

BMS-433771 is a potent orally active inhibitor of respiratory syncytial virus (RSV). BMS-433771 is active against both A and B groups of RSV, with an average EC50 of 20 nM. BMS-433771 can be used for the research of respiratory tract disease.

Chemical Information
Molecular Weight 377.44
Formula C21H23N5O2
CAS Number 543700-68-1
Form Solid
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Keith D Combrink, et al. Bioorg Med Chem Lett. Respiratory syncytial virus fusion inhibitors. Part 6: an examination of the effect of structural variation of the benzimidazol-2-one heterocycle moiety

[2] Kuo-Long Yu, et al. Bioorg Med Chem Lett. Respiratory syncytial virus fusion inhibitors. Part 4: optimization for oral bioavailability

[3] Christopher Cianci, et al. J Antimicrob Chemother. Antiviral activity and molecular mechanism of an orally active respiratory syncytial virus fusion inhibitor

[4] Christopher Cianci, et al. Antimicrob Agents Chemother. Oral efficacy of a respiratory syncytial virus inhibitor in rodent models of infection

[5] Christopher Cianci, et al. Antimicrob Agents Chemother. Orally active fusion inhibitor of respiratory syncytial virus

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Keywords: BMS-433771  supplier, RSV, inhibitors, activators


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