Catalog No.S1380 Synonyms: ABT-378
Molecular Weight(MW): 628.8
Lopinavir is a potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay.
Cited by 7 Publications
2 Customer Reviews
Low-micromolar amounts of chloroquine, chlorpromazine, loperamide, and lopinavir inhibit MERS-CoV-induced cytopathology. Huh7 cells in 96-well plates were infected with MERS-CoV isolate EMC/2012 (MOI, 0.005) in the presence of 0 to 20 uM LPV. Cells were incubated for 2 days, and cell viability was monitored using an MTS assay. In addition, the potential toxicity of compound treatment only was monitored in parallel mock-infected Huh7 cell cultures. Graphs show the results (averages and standard deviations [SD]) of a representative experiment that was performed in quadruplicate. All experiments were repeated at least twice. For each compound, the calculated EC50, CC50, and SI values are given.
Antimicrob Agents Chemother 2014 58(8), 4875-84. Lopinavir purchased from Selleck.
Sodium butyrate and lopinavir treatment represent pharmacological aging models that reproduce key properties of cellular aging. LLC-PK1 cells were incubated with vehicle (controls), sodium butyrate or lopinavir and assessed for different indicators of aging. (A) The number of cells that scored positive for SA-β-galactosidase activity increased significantly upon treatment with sodium butyrate or lopinavir. Data are shown for three independent experiments as average + SEM. Results were normalized to controls and depicted as arbitrary units (AU). (B) Sodium butyrate and lopinavir increase cell size, cause nuclear dysmorphy, reduce cell proliferation, while lamin A becomes more abundant. Confocal images were acquired for 5-ethynyl-2′-deoxyuridine (EdU) and lamin A (Materials and methods). Representative images are shown for control and treated samples. Scale bar, 20 μm. (C) Nuclear fluorescence was quantified for EdU and lamin A for at least three independent experiments. Pixel intensities were measured for > 100 cells for each experiment per condition. NaBu, sodium butyrate, D, DMSO, Lopi, lopinavir. **, p < 0.01; ***, p < 0.001.
Biochim Biophys Acta, 2017, 1864(3):475-486. Lopinavir purchased from Selleck.
Purity & Quality Control
Choose Selective HIV Protease Inhibitors
|Description||Lopinavir is a potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay.|
Lopinavir binds to mutant HIV protease (V82A, V82F and V82T) with Ki of 4.9 pM, 3.7 pM and 3.6 pM, respectively. Lopinavir inhibits 93% of wild-type HIV protease activity at 0.5 nM. Lopinavir inhibits HIV protease activity in the absence and presence of 50% HS with EC50 of 17 nM and 102 nM, respectively, in MT4 cells.  Lopinavir is converted to several metabolites in an NADPH-dependent manner in liver microsomes with the primary metabolites M-3 and M-4.  Lopinavir is a potent inhibitor of Rh123 efflux in Caco-2 monolayers with IC50 of 1.7 mM. Lopinavir exposure (72 hours) in LS 180V cells reduces the content of intracellular Rh123. Lopinavir induces P-glycoprotein immunoreactive protein and messenger RNA levels in LS 180V cells.  Lopinavir inhibits subtype C clone C6 with IC50 of 9.4 nM.  Lopinavir inhibits CYP3A with IC50 of 7.3 mM in human liver microsomes, while produces negligible or weak inhibition of human CYP1A2, 2B6, 2C9, 2C19 and 2D6. 
|In vivo||Lopinavir (10 mg/kg, orally) results in Cmax of 0.8 μg/mL and oral bioavailability of 25% in rats. |
-  Sham HL, et al. Antimicrob Agents Chemother, 1998, 42(12), 3218-3224.
-  Kumar GN, et al. Drug Metab Dispos, 1999, 27(1), 86-91.
-  Vishnuvardhan D, et al. AIDS, 2003, 17(7), 1092-1094.
|In vitro||DMSO||126 mg/mL (200.38 mM)|
|Ethanol||126 mg/mL (200.38 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01700790||Terminated||Drug: Lopinavir/ritonavir and ritonavir||AIDS|Tuberculosis||University of Miami|Oswaldo Cruz Foundation||February 2016||Phase 4|
|NCT01660477||Completed||Drug: Isavuconazole|Drug: Lopinavir/ritonavir||Pharmacokinetics of Isavuconazole|Pharmacokinetics of Lopinavir/Ritonavir|Healthy Volunteers||Astellas Pharma Global Development Inc.|Basilea Pharmaceutica International Ltd|Astellas Pharma Inc||June 2012||Phase 1|
|NCT01581853||Completed||Drug: Lopinavir/ritonavir 800 mg / 200mg||HIV||Daniel Podzamczer|Hospital Universitari de Bellvitge||May 2012||Phase 4|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
How should I go about proceeding with in vitro work to attain high concentration of the chemical?
S1380 Lopinavir can be dissolved in 2% DMSO, 49%PEG and 49%culture medium at 5 mg/ml.