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BMS-585248 

Cat. No. M30378
BMS-585248  Structure
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Biological Activity

BMS-585248 is a potent, third-generation HIV-1 attachment inhibitor with a promising initial in vitro and in vivo pharmacokinetic profile.

Chemical Information
Molecular Weight 447.42
Formula C22H18FN7O3
CAS Number 619331-12-3
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Rahul V Patel, et al. Bioorg Med Chem. Pyrroloaryls and pyrroloheteroaryls: Inhibitors of the HIV fusion/attachment, reverse transcriptase and integrase

[2] Alicia Regueiro-Ren, et al. J Med Chem. Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment 13. Synthesis and profiling of a novel amminium prodrug of the HIV-1 attachment inhibitor BMS-585248

[3] Alicia Regueiro-Ren, et al. J Med Chem. Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 12. Structure-activity relationships associated with 4-fluoro-6-azaindole derivatives leading to the identification of 1-(4-benzoylpiperazin-1-yl)-2-(4-fluoro-7-[1,2,3]triazol-1-yl-1h-p䲧癐Ỵ癑㧀癏羹瘸盋ܯƌܯð�瘺嶁瘶

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Keywords: BMS-585248  supplier, HIV Protease, inhibitors, activators


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