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Compound 212-148

Chemical Structure : Compound 212-148

CAS No.:

Compound 212-148

Catalog No.: PC-21419Not For Human Use, Lab Use Only.

Compound 212-148 a bispecific, dual inhibitor of both TMPRSS2 and cysteine proteases cathepsin L/B (CTSL/CTSB) with IC50 of 1.38 uM and 2.13/64.07 nM, respectively, demonstrates antiviral activity against various SARS-CoV-2 variants.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Compound 212-148 a bispecific, dual inhibitor of both TMPRSS2 and cysteine proteases cathepsin L/B (CTSL/CTSB) with IC50 of 1.38 uM and 2.13/64.07 nM, respectively, demonstrates antiviral activity against various SARS-CoV-2 variants.
Compound 212-148 simultaneously blocks TMPRSS2- and CTSL/CTSB-mediated viral entry pathways, exhibits synergistic antiviral activity against SARS-CoV-2.
Compound 212-148 inhibits the entry of pseudotyped SARS-CoV-2 Omicron variants BA.2.12.1 and BA.4 & BA.5 with a similar EC50 value of 0.4  nM in Huh-7 cells.
Compound 212-148 inhibits the SARS-CoV-2 Omicron BA.2 and Delta variants infection with EC50 values of 64.4 and 235.2 nM, respectively, in Calu-3 cells.

Physicochemical Properties

M.Wt 765.93
Formula C41H47N7O6S
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

2-(4-(((S)-1-oxo-3-phenyl-1-(((S,E)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl)amino)propan-2-yl)carbamoyl)piperazin-1-yl)ethyl 4-((diaminomethylene)amino)benzoate

References

1. Haofeng Wang, et al. Nat Commun. 2023 Nov 21;14(1):7574.

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