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Saquinavir mesylate

Cat. No. 4418

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Alternative Name: Ro 31-8959

Chemical Name: (2S)-N1-[(1S,2R)-3-[(3S,4aS,8aS)-3-[[(1,1-dimethylethyl)amino]carbonyl]octahydro-2(1H)-isoquinolinyl]-2-hydroxy-1-(phenylmethyl)propyl]-2-[(2-quinolinylcarbonyl)amino]butanediamide methanesulfonate

Biological Activity

Inhibitor of human immunodeficiency virus (HIV) protease (K_i values are <0.1 and 0.12 nM for HIV-2 and HIV-1 protease respectively). Exhibits high antiviral activity and low cytotoxicity.

Technical Data

M.Wt:

766.95

Formula:

C₃₈H₅₀N₆O₅.CH₄O₃S

Solubility:

Soluble to 50 mM in DMSO

Purity:

>99 %

Storage:

Store at +4°C

CAS No:

149845-06-7

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

Safety Data Sheet: View Safety Data Sheet

References

Roberts et al (1990) Rational design of peptide-based HIV proteinase inhibitors. Science 248 358. PMID: 2183354.

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.

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