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PF-00835231

Chemical Structure : PF-00835231

CAS No.: 870153-29-0

PF-00835231 (PF 00835231)

Catalog No.: PC-72752Not For Human Use, Lab Use Only.

PF-00835231 (PF00835231) is a potent inhibitor of pan-coronavirus family 3CL pro (IC50=0.27 nM, SARS CoV-2), with selectivity over human host protease targets

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Biological Activity

PF-00835231 (PF00835231) is a potent inhibitor of pan-coronavirus family 3CL pro (IC50=0.27 nM, SARS CoV-2), with selectivity over human host protease targets.
PF-00835231 inhibits SARS CoV-1 3CL pro with IC50 of 4 nM, displaying IC50 values of >10 μM against many of the other proteases and possessing modest levels of inhibition of cathepsin B (IC50 = 1.3 μM) and rhinovirus 3Cpro (IC50 = 1.7 μM).
PF-00835231 demonstrated potent inhibitory activity against all tested coronavirus 3CLpro including members of alpha-coronaviruses (NL63-CoV, HCoV-229E, PEDV, FIPV), beta-coronaviruses (HKU4-CoV, HKU5-CoV, HKU9-CoV, MHV-CoV, OC43-CoV, HKU1-CoV), and gamma-coronavirus (IBV-CoV), with Ki values ranging from 30 pM to 4 nM.
PF-00835231 exhibited viral effect against SARS-CoV-2 in cell culture, also showed potential synergy with remdesivir in HeLa-ACE2 cells.
PF-00835231 demonstrateed in vivo effect in mouse models of SARS-CoV and SARS-CoV-2 infection.

Physicochemical Properties

M.Wt 472.542
Formula C24H32N4O6
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-((S)-1-(((S)-4-Hydroxy-3-oxo-1-((S)-2-oxopyrrolidin-3-yl)butan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)-4-methoxy-1H-indole-2-carboxamide

References

1. de Vries M, et al. J Virol. 2021 Feb 23;95(10):e01819-20.

2. Liu C, et al. Antiviral Res. 2021 Mar;187:105020.

3. Hoffman RL, et al. J Med Chem. 2020 Nov 12;63(21):12725-12747.

4. Robert L Hoffman, et al. J Med Chem. 2020 Nov 12;63(21):12725-12747.

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