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首页-新冠病毒相关-SARS-CoV-2 Inhibitors-Jun8-76-3A
Jun8-76-3A

Chemical Structure : Jun8-76-3A

CAS No.: 2596275-66-8

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Jun8-76-3A (SARS-CoV-2 Mpro inhibitor)

货号: PC-72194Not For Human Use, Lab Use Only.

Jun8-76-3A is a potent, highly selective noncovalent SARS-CoV-2 main protease (Mpro) inhibitor with IC50 of 0.2 uM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    Jun8-76-3A is a potent, highly selective noncovalent SARS-CoV-2 main protease (Mpro) inhibitor with IC50 of 0.2 uM.
    Jun8-76-3A also comparably and potently inhibits SARS-CoV Mpro with IC50 of 0.27 uM, does not inhibit papain-like protease (PLpro, IC50>20 uM).
    Jun8-76-3A selectively inhibited SARS-CoV-2 Mpro and SARS-CoV Mpro with high potency but not other viral proteases (MERS-CoV Mpro, HCoV-OC43 Mpro, EV-A71 3Cpro, EV-D68 3Cpro, EV-A71 2Apro, EV-D68 2Apro, and SARS-CoV-2 PLpro), which was similar to ML188, Jun8-76-3A only showed weak inhibition against calpain 1 and cathepsin L with IC50 of 6.00 μM and 10.5 μM, respectively, corresponding to selectivity indexes of 40 and 70 with regard to SARS-CoV-2 Mpro inhibition.
    Jun8-76-3A demobnstrated high cellular antiviral activity against SARS CoV-2 (USA-WA1/2020 isolate) in Vero E6 cells with EC50 of 1.27 uM, without cytotoxicity (CC50>100 uM), which is similar to the antiviral potency of the covalent inhibitor GC376 (EC50=1.51 uM).
    Jun8-76-3A is highly selective compared to the covalent inhibitor GC376.

    物理化学性质&存储条件

    分子量 501.586
    分子式 C32H27N3O3
    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-([1,1'-biphenyl]-4-yl)-N-((R)-2-oxo-2-(((S)-1-phenylethyl)amino)-1-(pyridin-3-yl)ethyl)furan-2-carboxamide

    参考文献

    1. Naoya Kitamura, et al. J Med Chem. 2021 Apr 23;10.1021/acs.jmedchem.1c00509.

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