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Lufotrelvir

Cat. No. M10872
Lufotrelvir Structure
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Biological Activity

PF-07304814 IS A PHOSPHATE PRODRUG FOR PF-00835231 THAT BINDS AND INHIBITS SARS-CoV-2 3CLpro Active, Ki is 174 nM.

Chemical Information
Molecular Weight 552.51
Formula C24H33N4O9P
CAS Number 2468015-78-1
Solubility (25°C) DMSO ≥ 60 mg/mL
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] Britton Boras, et al. Nat Commun. Preclinical characterization of an intravenous coronavirus 3CL protease inhibitor for the potential treatment of COVID19

[2] Elie Dolgin. Nature. The race for antiviral drugs to beat COVID - and the next pandemic

[3] Mohammad Hassan Baig, et al. Molecules. Is PF-00835231 a Pan-SARS-CoV-2 Mpro Inhibitor? A Comparative Study

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