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

Chemical Structure : Y180

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Y180 (SARS-CoV-2 Mpro inhibitor Y180)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	510.544
分子式	C30H23DFN3O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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

Y180 (SARS-CoV-2 Mpro inhibitor Y180)

生物&药学活性

物理化学性质&存储条件

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Y180 (SARS-CoV-2 Mpro inhibitor Y180)

生物&药学活性

物理化学性质&存储条件

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