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首页-新冠病毒相关-SARS-CoV-2 Inhibitors-GZNL-P36
GZNL-P36

Chemical Structure : GZNL-P36

CAS No.:

GZNL-P36

货号: PC-23545Not For Human Use, Lab Use Only.

GZNL-P36 is a potent, selective and orally bioavailable SARS-CoV-2 papain-like protease (PLpro) inhibitor with IC50 of 6.45 nM, ITC Kd value of 24.6 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

GZNL-P36 is a potent, selective and orally bioavailable SARS-CoV-2 papain-like protease (PLpro) inhibitor with IC50 of 6.45 nM, ITC Kd value of 24.6 nM.
GZNL-P36 dose-dependently protects cells from death with 50% effective concentration (EC50) values for wild type (WT), Omicron BA.5 and XBB.1 is 111.0 nM, 306.2 nM and 58.2 nM, respectively.
GZNL-P36 possesses similar effective anti-viral activity for SARS-CoV-2 and its variants, compared with S-217622 (Ensitrelvir).
GZNL-P36 also exhibits anti-viral activity for the other coronaviruses, such as HCoV-NL63 (EC50: 81.6 nM) and HCoV-229E (EC50: 2.66 μM).
Oral administration of the GZNL-P36 results in significantly improved survival and notable reductions in lung viral loads and lesions in SARS-CoV-2 infection mouse model, consistent with RNA-seq data analysis.

物理化学性质&存储条件

分子量 466.59
分子式 C29H30N4O2
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

2-methyl-N-(1-(1-methyl-2-oxo-1,2-dihydrobenzo[cd]indol-6-yl)cyclopropyl)-5-(6-methyl-3,6-diazabicyclo[3.1.1]heptan-3-yl)benzamide

参考文献

1. Lu Y, et al. Nat Commun. 2024 Nov 23;15(1):10169.

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