Olgotrelvir (STI-1558) | SARS-CoV-2 Mpro inhibitor | Probechem Biochemicals

Chemical Structure : Olgotrelvir

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Olgotrelvir (STI-1558, STI 1558)

货号: PC-21709Not For Human Use, Lab Use Only.

Olgotrelvir (STI-1558) is a next-generation antiviral targeting SARS-CoV-2 Mpro and host lysosomal cysteine protease cathepsin L (CTSL) with high antiviral activity, Olgotrelvir is the prodrug of AC1115.

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生物&药学活性

Olgotrelvir (STI-1558) is a next-generation antiviral targeting SARS-CoV-2 Mpro and host lysosomal cysteine protease cathepsin L (CTSL) with high antiviral activity, Olgotrelvir is the prodrug of AC1115.
Olgotrelvir (STI-1558) is readily converted to its active form AC1115 in biorelevant media and human blood.
Olgotrelvir (STI-1558) shows a covalent linkage between the aldehyde warhead and the sulfur atom of C145 at the Mpro catalytic active site.
Olgotrelvir (STI-1558) displays antiviral activity against SARS-CoV-2 VOCs in Vero E6 cells, including WA-1, Alpha, Beta, Delta, Lambda, and Gamma variants with EC50 of 0.28-4.26 uM, without cytotoxicity up to 100 uM.
Olgotrelvir (STI-1558) displays antiviral effects in the EpiAirway system composed of differentiated normal human bronchial epithelial cells (dNHBE) with EC50 of <41 nM.
Olgotrelvir (STI-1558) (1,000 mg/kg, BID, p.o.) significantly reduces viral RNA shedding, exhibits strong in vivo antiviral activity in K18-hACE2 transgenic mice.
Olgotrelvir (STI-1558) preventsmice from weight loss caused by SARS-CoV-2 infection and blocks pro-inflammatory cytokine release.

物理化学性质&存储条件

分子量	516.54
分子式	C22H29N4NaO7S
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	sodium (2S)-2-((S)-2-(1H-indole-2-carboxamido)-4-methylpentanamido)-1-hydroxy-3-((S)-2-oxopyrrolidin-3-yl)propane-1-sulfonate

参考文献

1. Long Mao, et al. Med. 2024 Jan 12;5(1):42-61.e23.

Olgotrelvir (STI-1558, STI 1558)

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物理化学性质&存储条件

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Olgotrelvir (STI-1558, STI 1558)

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