PLpro inhibitor is a potent papain-like protease (PLpro) inhibitor with IC50 of 2.6 μM. PLpro inhibitor shows significant antiviral activity with EC50 values of 13.1 μM, without toxicity up to the highest concentration tested.
|Solubility (25°C)||DMSO 10 mM|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
 Brendan T Freitas, et al. ACS Infect Dis. Characterization and Noncovalent Inhibition of the Deubiquitinase and deISGylase Activity of SARS-CoV-2 Papain-Like Protease
 Kiira Ratia, et al. Proc Natl Acad Sci U S A. A noncovalent class of papain-like protease/deubiquitinase inhibitors blocks SARS virus replication
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