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Pomotrelvir

Cat. No. M41266
Pomotrelvir Structure
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Biological Activity

Pomotrelvir (PBI-0451) is a selective, orally active SARS-CoV-2 3CL protease inhibitor.

Chemical Information
Molecular Weight 455.94
Formula C23H26ClN5O3
CAS Number 2713437-86-4
Form Solid
Solubility (25°C) DMSO 100 mg/mL (Need ultrasonic)
Storage 4°C, protect from light, sealed
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] Xiao Tong et al. Antimicrob Agents Chemother. Evaluation of in vitro antiviral activity of SARS-CoV-2 Mpro inhibitor pomotrelvir and cross-resistance to nirmatrelvir resistance substitutions

[2] Ziping Yang et al. Drug Metab Dispos. Characterization of Pharmacokinetics, Biotransformation and Elimination of Pomotrelvir Orally Administered in Healthy Male Adults Using Two [14C]-Labeled Microtracers with Separate Labeling Positions

[3] Ziping Yang et al. CPT Pharmacometrics Syst Pharmacol. A comprehensive evaluation in clinic and physiologically-based pharmacokinetic modeling and simulation to confirm lack of cytochrome P450-mediated drug-drug interaction potential for pomotrelvir

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