Lopinavir-d8

Lopinavir-d₈ is intended for use as an internal standard for the quantification of lopinavir by GC- or LC-MS. Lopinavir is a potent HIV-1 protease inhibitor (K_i = 1.3 pM for wild-type enzyme).¹ It inhibits the replication of clinical isolates of HIV-1 (EC₅₀s = 5-52 nM). Lopinavir reduces the infectious virus yield and viral RNA copy numbers in the culture supernatant of Vero E6 cells infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2; EC₅₀s = 26.63 and 26.10 µM, respectively).² It reduces lung and kidney viral load, bronchointerstitial pneumonia, and pulmonary inflammatory cell infiltration in a marmoset model of Middle East respiratory syndrome coronavirus (MERS-CoV) infection when administered in combination with ritonavir .³

1.Sham, H.L., Kempf, D.J., Molla, A., et al.ABT-378, a highly potent inhibitor of the human immunodeficiency virus proteaseAntimicrob. Agents Chemother.42(12)3218-3224(1998) 2.Choy, K.-T., Wong, A.-Y., Kaewpreedee, P., et al.Remdesivir, lopinavir, emetine, and homoharringtonine inhibit SARS-CoV-2 replication in vitroAntiviral Res.178104786(2020) 3.Chan, J.-F., Yao, Y., Yeung, M.-L., et al.Treatment with lopinavir/ritonavir or interferon-β1b improves outcome of MERS-CoV infection in a nonhuman primate model of common marmosetJ. Infect. Dis.212(12)1904-1913(2015)