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Biological Data Biological description Potent and selective HIV-1 protease inhibitor (EC50 = 6.5 nM, against HIV cultured in peripheral blood mononuclear cells.
More potent at inhibiting HIV-1 than ritonavir in vitro but shows poor bioavailability in vivo.
Shows antiviral effect against SARS-CoV, MERS-CoV, and hCoV-229E in vitro, (mean EC50 ranged from 6.6 to 17.1µM).
Inhibits SARS-CoV-2 replication in vitro in Vero E6 cells (EC50 = < 100µM).
Also acts as a potent ER stress inducer.
Solubility & Handling Storage instructions -20°C
Solubility overview Soluble in DMSO (100 mM), and in ethanol (100 mM)
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use
Chemical Data Chemical name (2S)-N-[(2S,4S,5S)-5-[2-(2,6-dimethylphenoxy)acetamido]-4-hydroxy-1,6-diphenylhexan-2-yl]-3-methyl-2-(2-oxo-1,3-diazinan-1-yl)butanamide
Chemical structure
Molecular Formula C37 H48 N4 O5
SMILES O=C(N[C@@H](Cc1ccccc1)[C@@H](O)C[C@@H](NC(=O)[C@@H](N2C(=O)NCCC2)C(C)C)Cc3ccccc3)COc4c(cccc4C)C
InChi InChI=1S/C37H48N4O5/c1-25(2)34(41-20-12-19-38-37(41)45)36(44)39-30(21-28-15-7-5-8-16-28)23-32(42)31(22-29-17-9-6-10-18-29)40-33(43)24-46-35-26(3)13-11-14-27(35)4/h5-11,13-18,25,30-32,34,42H,12,19-24H2,1-4H3,(H,38,45)(H,39,44)(H,40,43)/t30-,31-,32-,34-/m0/
InChiKey KJHKTHWMRKYKJE-SUGCFTRWSA-N
References for Lopinavir References are publications that support the biological activity of the product
Remdesivir, lopinavir, emetine, and homoharringtonine inhibit SARS-CoV-2 replication in vitro Choy et al (2020) Antiviral Res. 178 : 104786 ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease Sham et al (1998) Antimicrob Agents Chemother 42(12) : 3218-24 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 (1998) J Virol. 72(9) : 7532-41
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Potent and selective HIV-1 protease inhibitor