Y180 | SARS-CoV-2 Mpro inhibitor | Probechem Biochemicals

Chemical Structure : Y180

Y180 (SARS-CoV-2 Mpro inhibitor Y180)

Catalog No.: PC-38696Not For Human Use, Lab Use Only.

Y180 is a highly potent, selective, covalent, and orally active SARS-CoV-2 main protease (Mpro) inhibitor with IC50 of 8.1 nM in enzymatic assays, binding Ki value of 1 nM.

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Biological Activity

Y180 is a highly potent, selective, covalent, and orally active SARS-CoV-2 main protease (Mpro) inhibitor with IC50 of 8.1 nM in enzymatic assays, binding Ki value of 1 nM.
Y180 showed almost no activity against several common mammalian proteases with similar structure, including caspase 2, chymotrypsin, thrombin, cathepsin B, cathepsin D and cathepsin L (IC50>100 uM).
Y180 protected against wild-type SARS-CoV-2, B.1.1.7 (Alpha), B.1.617.1 (Kappa) and P.3 (Theta), with EC50 of 11.4, 20.3, 34.4 and 23.7 nM, respectively.
Y180 displayed a remarkable antiviral potency and substantially ameliorated the virus-induced tissue damage in both nasal turbinate and lung of B.1.1.7-infected K18-human ACE2 (K18-hACE2) transgenic mice.
Y180 improved the survival of mice in the lethal B.1.617.1 infection model, also highly effective against the B.1.1.529 (Omicron) variant both in vitro and in vivo.

Physicochemical Properties

M.Wt	510.544
Formula	C30H23DFN3O4
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-(dibenzo[b,d]furan-3-yl)-N-((R)-2-(((S)-1-(4-fluorophenyl)ethyl)amino)-2-oxo-1-(pyridin-3-yl)ethyl-1-d)-2-oxopropanamide

References

1. Quan BX, et al. Nat Microbiol. 2022 May;7(5):716-725.

Y180 (SARS-CoV-2 Mpro inhibitor Y180)

Biological Activity

Physicochemical Properties

References

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