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Olgotrelvir

Chemical Structure : Olgotrelvir

CAS No.: 2763596-72-9

Olgotrelvir (STI-1558)

Catalog No.: 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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    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 516.54
    Formula C22H29N4NaO7S
    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

    sodium (2S)-2-((S)-2-(1H-indole-2-carboxamido)-4-methylpentanamido)-1-hydroxy-3-((S)-2-oxopyrrolidin-3-yl)propane-1-sulfonate

    References

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

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