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Lopinavir

Cat. No. 7052 Submit a Review Datasheet / COA / SDS
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Description: Highly potent and selective HIV-1 protease inhibitor
Alternative Names: ABT-378
Chemical Name: (αS)-N-[(1S,3S,4S)-4-[[2-(2,6-Dimethylphenoxy)acetyl]amino]-3-hydroxy-5-phenyl-1-(phenylmethyl)pentyl]tetrahydro-α-(1-methylethyl)-2-oxo-1(2H)-pyrimidineacetamide
Purity: ≥98% (HPLC)
Datasheet
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Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for Lopinavir

Lopinavir is a highly potent and selective HIV-1 protease inhibitor (IC50 = 6.5 nM, HIV cultured in peripheral blood mononuclear cells; Ki = 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)

Compound Libraries for Lopinavir

Lopinavir is also offered as part of the Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

Technical Data for Lopinavir

M. Wt 628.8
Formula C37H48N4O5
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 192725-17-0
PubChem ID 92727
InChI Key KJHKTHWMRKYKJE-SUGCFTRWSA-N
Smiles CC([C@@H](C(N[C@@H](CC1=CC=CC=C1)C[C@@H]([C@@H](NC(COC2=C(C=CC=C2C)C)=O)CC3=CC=CC=C3)O)=O)N4CCCNC4=O)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.

Solubility Data for Lopinavir

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 62.88 100
ethanol 62.88 100

Preparing Stock Solutions for Lopinavir

The following data is based on the product molecular weight 628.8. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.59 mL 7.95 mL 15.9 mL
5 mM 0.32 mL 1.59 mL 3.18 mL
10 mM 0.16 mL 0.8 mL 1.59 mL
50 mM 0.03 mL 0.16 mL 0.32 mL

Molarity Calculator

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References for Lopinavir

References are publications that support the biological activity of the product.

Sham et al (1998) ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease. Antimicrob.Agents Chemother. 42 3218 PMID: 9835517

Carrillo et al (1998) In vitro selection and characterization of human immunodeficiency virus type 1 variants with increased resistance to ABT-378, a novel protease inhibitor. J.Virol. 72 7532 PMID: 9696850

Choy et al (2020) Remdesivir, lopinavir, emetine, and homoharringtonine inhibit SARS-CoV-2 replication in vitro. Antiviral Res. 178 PMID: 32251767

If you know of a relevant reference for Lopinavir, please let us know.

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Citations for Lopinavir

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