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PLpro inhibitor

Cat. No. M9641
PLpro inhibitor Structure
Size Price Availability Quantity
5mg USD 406  USD406 In stock
10mg USD 581  USD581 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 346.42
Formula C22H22N2O2
CAS Number 1093070-14-4
Solubility (25°C) DMSO 10 mM
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] 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

[2] 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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