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Inhibitor of human immunodeficiency virus (HIV) protease (Ki values are <0.1 and 0.12 nM for HIV-2 and HIV-1 protease respectively). Exhibits high antiviral activity and low cytotoxicity. In silico docking models predict potential as an inhibitor of SARS-CoV-2 3CLpro.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 766.95. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||2.61 mL||13.04 mL||26.08 mL|
|2.5 mM||0.52 mL||2.61 mL||5.22 mL|
|5 mM||0.26 mL||1.3 mL||2.61 mL|
|25 mM||0.05 mL||0.26 mL||0.52 mL|
References are publications that support the biological activity of the product.
Krausslich et al (1992) Specific inhibitor of human immunodeficiency virus proteinase prevents the cytotoxic effects of a single-chain proteinase dimer and restores particle formation. J.Virol. 66 567 PMID: 1727499
Tucker et al (1992) A series of potent HIV-1 protease inhibitors containing a hydroxyethyl secondary amine transition state isostere: synthesis, enzyme inhibition, and antiviral activity. J.Med.Chem. 35 2525 PMID: 1635054
Kaldor et al (1995) Isophthalic acid derivatives: amino acid surrogates for the inhibition of HIV-1 protease. Bioorg.Med.Chem.Lett. 5 721
Roberts et al (1990) Rational design of peptide-based HIV proteinase inhibitors. Science 248 358 PMID: 2183354
Hall and Hai-Feng et al (2020) A search for medications to treat COVID-19 via in silico molecular docking models of the SARS-CoV-2 spike glycoprotein and 3CL protease. Travel Med.Infect.Dis. 35 PMID: 32294562
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1 Citation for Saquinavir mesylate
Citations are publications that use Tocris products. Selected citations for Saquinavir mesylate include:
Lan et al (2014) Provirus activation plus CD59 blockage triggers antibody-dependent complement-mediated lysis of latently HIV-1-infected cells. J Immunol 193 3577 PMID: 25149467
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