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Lopinavir

Manufactured by Merck Group
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Lopinavir is a laboratory product manufactured by Merck Group. It is a protease inhibitor used in research applications.

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Lab products found in correlation

Ritonavir, by Merck Group (8 mentions) Darunavir, by Merck Group (4 mentions) Amprenavir, by Merck Group (4 mentions) Chloroquine, by Merck Group (3 mentions) Digoxin, by Merck Group (2 mentions) Nelfinavir, by Apexbio (2 mentions) Ribavirin, by Merck Group (2 mentions) Saquinavir, by Merck Group (2 mentions) Atazanavir, by Selleck Chemicals (2 mentions) Atazanavir, by Merck Group (2 mentions) Nevirapine, by Merck Group (2 mentions) Verapamil, by Merck Group (2 mentions) Metformin, by Merck Group (2 mentions) Hoechst 33342, by Thermo Fisher Scientific (2 mentions) Nafamostat, by Tokyo Chemical Industry (1 mentions) Hydroxychloroquine, by Tokyo Chemical Industry (1 mentions) Chloroquine, by Selleck Chemicals (1 mentions) Veroe6, by Japanese Collection of Research Bioresources Cell Bank (1 mentions) Veroe6 tmprss2 cell, by Japanese Collection of Research Bioresources Cell Bank (1 mentions) Favipiravir, by MedChemExpress (1 mentions)

24 protocols using lopinavir

1

Evaluating Antiviral Agents Against SARS-CoV-2

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VeroE6 cells and TMPRSS2-overexpressing VeroE6 (VeroE6TMPRSS2) cells were obtained from the Japanese Collection of Research Bioresources (JCRB) Cell Bank (Osaka, Japan). VeroE6 cells were maintained in Dulbecco’s modified Eagle’s medium (d-MEM) supplemented with 10% fetal bovine serum (FCS), 100 μg/ml of penicillin, and 100 μg/ml of streptomycin. VeroE6TMPRSS2 cells were maintained in d-MEM as mentioned above in the presence of 1 mg/ml of G418. SARS-CoV-2 strain JPN/TY/WK-521 (SARS-CoV-2WK-521) was obtained from the National Institute of Infectious Diseases (Tokyo, Japan).
The antiviral agents lopinavir (Sigma-Aldrich, St. Louis, MO); nelfinavir, nafamostat, hydroxychloroquine, and nitazoxanide (Tokyo Chemical Industry, Tokyo, Japan); favipiravir (MedChemExpress, Monmouth Junction, NJ); and chloroquine (Selleck, Sylvanfield Drive, Houston, TX) were purchased. Remdesivir was obtained from Clifford Lane, National Institute of Allergy and Infectious Diseases, National Institutes of Health, Bethesda, MD. GRL-0820 and GRL-0920 were synthesized by A. K. Ghosh. Each compound except remdesivir was dissolved in DMSO at 20 mM, and remdesivir was prepared with saline solution at 5 mM concentrations as stock solutions.
Hattori S.I., Higshi-Kuwata N., Raghavaiah J., Das D., Bulut H., Davis D.A., Takamatsu Y., Matsuda K., Takamune N., Kishimoto N., Okamura T., Misumi S., Yarchoan R., Maeda K., Ghosh A.K, & Mitsuya H. (2020). GRL-0920, an Indole Chloropyridinyl Ester, Completely Blocks SARS-CoV-2 Infection. mBio, 11(4), e01833-20.
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2

Fluorescent Probe Assay for Transporter Inhibition

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5-(and-6)-carboxy-2′,7′-dichlorofluorescein (CDCF) and 5-(and-6)-carboxy-2′,7′-dichlorofluorescein diacetate (CDCFDA) were purchased from AAT Bioquest (Sunnyvale, CA, United States). Digoxin, estrone 3-sulfate (E3S), and lopinavir were purchased from Sigma-Aldrich (St. Louis, MO, United States). Nelfinavir was obtained from APExBIO Technology (Houston, TX, United States). Darunavir was purchased from Toronto Research Chemicals (North York, ON, Canada). A rabbit monoclonal P-gp antibody (ab120904), a rabbit monoclonal MRP2 antibody (ab172630) and a rabbit monoclonal GAPDH antibody (ab181602) were purchased from Abcam (Cambridge, MA, United States), and a rabbit monoclonal BCRP antibody (CST42078) was obtained from Cell Signaling Technology (Danvers, MA, United States). All other chemicals and solvents were of the highest grade commercially available.
Feng D., Zhong G., Zuo Q., Wan Y., Xu W., He C., Lin C., Huang D., Chen F, & Huang L. (2022). Knockout of ABC transporters by CRISPR/Cas9 contributes to reliable and accurate transporter substrate identification for drug discovery. Frontiers in Pharmacology, 13, 1015940.
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3

HIV-1 Neutralization Assay in TZM-bl Cells

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Virus stocks were produced and quantified by p24 ELISA as described above and used to infect TZM-bl indicator cells (65 (link), 66 (link)). TZM-bl cells were plated in white 96-well plates using 4,000 cells per 0.1 mL medium per well. The medium was removed 24 h later and replaced with virus and medium to a final volume of 0.2 mL per well. Cells were infected with 1 ng p24 of virus per well. Each infection was performed in triplicate (technical replicates), and uninfected cells were included as controls. Six hours after infection, the medium was removed and fresh medium containing 0.5 μM of the protease inhibitor lopinavir (Sigma) was added to prevent reinfection. Luciferase activity was measured 72 h postinfection using a 96-well luminometer (LUMIstar Galaxy; BMG LABTECH, Cary, NC, USA). Data were analyzed by first subtracting the average luminescence from uninfected cells from that observed with infected cells. Next, luciferase activity was normalized to that of NL4-3, which was set to 100%.
Rawson J.M., Nikolaitchik O.A., Yoo J.A., Somoulay X., Brown M.A., Mbuntcha Bogni F.S., Pathak V.K., Soheilian F., Slack R.L., Sarafianos S.G, & Hu W.S. (2022). Adaptation of HIV-1/HIV-2 Chimeras with Defects in Genome Packaging and Viral Replication. mBio, 13(5), e02220-22.
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4

Evaluating Antivirals Against SARS-CoV-2

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The following compounds were tested to determine their effects on 3CLpro activity, cytotoxicity, or inhibition of SARS-CoV-2 replication: cobicistat (sc-500831; Santa Cruz Biotechnology), remdesivir (S8932; Selleckchem Chemicals), tipranavir (sc-220260; Santa Cruz Biotechnology), nelfinavir mesylate hydrate (PZ0013; Sigma-Aldrich), darunavir and lopinavir (both obtained through the AIDS Research and Reference Reagent Program, Division of AIDS, NIAID), MG-132 (M8699; Sigma‐Aldrich), and GC376 (BPS Bioscience).
Shytaj I.L., Fares M., Gallucci L., Lucic B., Tolba M.M., Zimmermann L., Adler J.M., Xing N., Bushe J., Gruber A.D., Ambiel I., Taha Ayoub A., Cortese M., Neufeldt C.J., Stolp B., Sobhy M.H., Fathy M., Zhao M., Laketa V., Diaz R.S., Sutton R.E., Chlanda P., Boulant S., Bartenschlager R., Stanifer M.L., Fackler O.T., Trimpert J., Savarino A, & Lusic M. (2022). The FDA-Approved Drug Cobicistat Synergizes with Remdesivir To Inhibit SARS-CoV-2 Replication In Vitro and Decreases Viral Titers and Disease Progression in Syrian Hamsters. mBio, 13(2), e03705-21.
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5

Monocyte M1/M2 Polarization Modulation by Cigarette Smoke and Lopinavir

Cited 1 time
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The human monocytic cell lines U937 and U1 were cultured in RPMI 1640 medium supplemented with 10% FBS. U937 was purchased from American Type Culture Collection (ATCC Manassas, VA) and U1 cell lines were obtained from NIH AIDS Reagent Program (Germantown, MD). U937 and U1 cells were treated with cytokines to effect polarization for 48 hours. LPS (100 ng/ml, E. Coli origin, Sigma-Aldrich, L2630, St. Louis, Mo, USA) combined with IFN-γ (20ng/ml, Life Technologies, PHC4031, Carlsbad, CA, USA) were used for M1 polarization. LPS (100 ng/mL) with IL-4 (10 ng/mL, CST, 8919SF, Danvers, MA, USA) and IL-13 (10 ng/mL, CST, 8905SF, Danvers, MA, USA) were used to stimulate M2 polarization. No cytokines were added to unstimulated control cells. Cells were treated with cigarette smoke condensate (CSC) (40 μg/ml, Murty Pharmaceuticals, KY, USA), a concentration which approximates concentrations observed in smokers, [13 (link), 56 (link)] with or without the antiretroviral protease inhibitor lopinavir (Sigma Aldrich, 1370101, St. Louis, MO, USA) (LPV) for 24 h before harvesting.
Mu Y., Patters B.J., Midde N.M., He H., Kumar S, & Cory T.J. (2018). Tobacco and Antiretrovirals Modulate Transporter, Metabolic Enzyme, and Antioxidant Enzyme Expression and Function in Polarized Macrophages. Current HIV Research, 16(5), 354-363.
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6

Anti-Viral Drug Solubilization Protocol

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Lopinavir, ritonavir, amprenavir, and darunavir were purchased Sigma or Cambridge Biosciences in powder form. The drugs were solubilised in DMSO at a stock concertation of 5 mM concentration and then further diluted to 100 μM in 200 mM ammonium acetate supplemented with 0.5% C8E4.
Mehmood S., Marcoux J., Gault J., Quigley A., Michaelis S., Young S.G., Carpenter E.P, & Robinson C.V. (2016). Mass spectrometry captures off-target drug binding and provides mechanistic insights into the human metalloprotease ZMPSTE24. Nature chemistry, 8(12), 1152-1158.
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7

Exploring Pharmacological Modulation

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Mitoxantrone, rhodamine 123, GF120918 (Elacridar), Ko143, hydrocortisone, prednisolone, dexamethasone, ivermectin, lopinavir, hydroxychloroquine, chloroquine and oseltamivir and MTT were purchased from Sigma-Aldrich. Hoechst 33342 and TRIzol were purchased from Invitrogen. All other reagents were commercial products of the highest available purity.
Dutra J.D., Scheiffer G., Kronenberger T., Gomes L.J., Zanzarini I., dos Santos K.K., Tonduru A.K., Poso A., Rego F.G., Picheth G., Valdameri G, & Moure V.R. (2023). Structural and molecular characterization of lopinavir and ivermectin as breast cancer resistance protein (BCRP/ABCG2) inhibitors. EXCLI Journal, 22, 1155-1172.
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8

Anti-SARS-CoV-2 N Protein Assay

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Isoginkgetin (MW-566.51 g/mol), % purity ≥ 98% (HPLC) and afzelin (432.38 g/mol), % purity ≥ 90% (LC/MS-UV) were purchased from Sigma-Aldrich, and chloroquine, lopinavir, and remdesivir (used as reference compounds) were bought from Sigma-Aldrich, SelleckChem, and MedChemExpress, respectively. The anti-SARS-CoV-2 N protein antibody was purchased from Sino Biological Inc. (China), with Hoechst-33342 and the Alexa Fluor-488 goat anti-rabbit IgG (H + L) secondary antibody purchased from Molecular Probes. Also, paraformaldehyde (PFA) (a 32% aqueous solution) and normal goat serum were obtained from Vector Laboratories, Inc. (Burlingame, CA) and Electron Microscopy Sciences (Hatfield, PA), respectively. chloroquine was mixed in Dulbecco's Phosphate-Buffered Saline (DPBS; Welgene). For in vitro studies, all reagents were well mixed in DMSO.
Raj V., Lee J.H., Shim J.J, & Lee J. (2022). Antiviral activities of 4H-chromen-4-one scaffold-containing flavonoids against SARS–CoV–2 using computational and in vitro approaches. Journal of Molecular Liquids, 353, 118775.
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9

Antivirals and Chloroquine Evaluation

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DMSO, dexamethasone (D4902), ribavirin (R9644), lopinavir (SML0491), ritonavir (SML1222), hydroxychloroquine sulphate (HO915), chloroquine diphosphate (C6628), and azithromycin dihydrate (A9834) were supplied by Sigma-Aldrich (Overijse, Belgium). In the case of the latter 3 drugs, the salt forms were purchased to avoid limitations due to the low solubility of the drugs. Remdesivir (30354-10) was purchased from Sanbio (Uden, The Netherlands), and favipiravir (FF29069) was obtained from Biosynth Carbosynth (Compton, United Kingdom). The peptide mimetic 10Panx1 was synthesised in-house by means of solid-phase peptide synthesis with a purity of >98%. Lanthanum trichloride was supplied by Merck Chemical n.v./s.a. (Overijse, Belgium). All other reagents were obtained from various suppliers at the highest analytical grade possible. Each drug was dissolved in the respective solvent (Table 1).
Caufriez A., Tabernilla A., Van Campenhout R., Cooreman A., Leroy K., Sanz Serrano J., Kadam P., dos Santos Rodrigues B., Lamouroux A., Ballet S, & Vinken M. (2022). Effects of Drugs Formerly Suggested for COVID-19 Repurposing on Pannexin1 Channels. International Journal of Molecular Sciences, 23(10), 5664.
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10

Antimicrobial Library Compound Preparation

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The antimicrobial library, consisting of 112 compounds (68 antibacterials; 39 antivirals; and five other) was purchased from Selleck Chemicals (Burlington, ON, Canada) and contained the PIs, NFV, indinavir, amprenavir, and atazanavir. Additional PIs – lopinavir, ritonavir, darunavir (DRV), and saquinavir were purchased from Sigma-Aldrich (St Louis, MO, USA). Compounds were dissolved in dimethylsulfoxide (DMSO) to a stock concentration of 10 mM. Subsequent dilutions were made using cell culture media, as needed, to gain concentrations of 40 to 10−6 µM.
Meier-Stephenson V., Riemer J, & Narendran A. (2017). The HIV protease inhibitor, nelfinavir, as a novel therapeutic approach for the treatment of refractory pediatric leukemia. OncoTargets and therapy, 10, 2581-2593.
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