Lopinavir

Biological Activity

Lopinavir is a highly potent and selective HIV-1 protease inhibitor (IC₅₀ = 6.5 nM, HIV cultured in peripheral blood mononuclear cells; K_i = 1.3 pM). Displays >10⁵-fold selectivity for HIV-1 protease over mammalian proteases including renin and cathepsin D and E. Inhibits HIV-1 protease in patient HIV isolates displaying mutations that confer resistance to ritonavir (Cat. No. 5856) (IC₅₀ values in 5 - 50 nM range). Also inhibits SARS-CoV-2 replication in vitro (IC₅₀ = 26 μM)

Technical Data

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.

Background References

1. ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease.
   Sham et al.
   Antimicrob.Agents Chemother., 1998;42:3218
2. In vitro selection and characterization of human immunodeficiency virus type 1 variants with increased resistance to ABT-378, a novel protease inhibitor.
   Carrillo et al.
   J.Virol., 1998;72:7532
3. Remdesivir, lopinavir, emetine, and homoharringtonine inhibit SARS-CoV-2 replication in vitro.
   Choy et al.
   Antiviral Res., 2020;178

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