Lopinavir

Catalog No.S1380 Synonyms: ABT-378

Lopinavir Chemical Structure

Molecular Weight(MW): 628.8

Lopinavir is a potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay.

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In DMSO USD 82 In stock
USD 90 In stock
USD 570 In stock
USD 970 In stock
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Cited by 6 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

Biological Activity

Description Lopinavir is a potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay.
Targets
HIV protease [1]
(Cell-free assay)
1.3 pM(Ki)
In vitro

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. [1] Lopinavir is converted to several metabolites in an NADPH-dependent manner in liver microsomes with the primary metabolites M-3 and M-4. [2] 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. [3] Lopinavir inhibits subtype C clone C6 with IC50 of 9.4 nM. [4] 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. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MT2 cells NHHmRlBHfW6ldHnvckBie3OjeR?= M4LBTWFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhKXjJiRVjPJIlvKE2WMjDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKHB{NDDHZYcheHKxdHXpckBmgHC{ZYPzbY9vKGK7IF3UWEBie3OjeTygSWM2OD1yLkCwNlYh|ryP MnrHNVc{PzF6MUG=
HEK293 cells MVzGeY5kfGmxbjDhd5NigQ>? MnTNOFghcA>? NXvPT|R5SW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5Qhf2muZDD0fZBmKEiLVkGgUmw1NTNiaX6gTGVMOjl|IHPlcIx{KGGodHXyJFQ5KGi{czDifUBz\XCuaXPheIlwdi2mZX\m[YN1cX[nIHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\S2kYYPl[EBxcGWwb4T5dIlkKGG|c3H5MEBGSzVyPUCuNFAzQCEQvF2= M2CxflE4PjN6Nkm0
human MT4 cells NGfBbVJHfW6ldHnvckBie3OjeR?= MYq1JIRigXN? MYHBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDITXYzKE2VIHnu[oVkfGWmIHnuJIh2dWGwIF3UOEBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oII\pdpV{KHC{b3T1Z5Rqd25iYX\0[ZIhPSCmYYnzJIJ6KEynboTpMXJVKGGldHn2bZR6KGG|c3H5MEBGSzVyPUCuNFA3KM7:TR?= NEXKWooyPzV5Nki0PC=>
human PBMC cells MoK4SpVv[3Srb36gZZN{[Xl? NYDtXJNOPSCmYYnz MXHBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDITXYzKE2VIHnu[oVkfGWmIHnuJIh2dWGwIGDCUWMh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjD2bZJ2eyCycn;keYN1cW:wIHHmeIVzKDViZHH5d{BjgSCOZX70bU1TXCCjY4Tpeol1gSCjc4PhfUwhTUN3ME2wMlAyPSEQvF2= MYmxO|U4Pjh2OB?=

... Click to View More Cell Line Experimental Data

In vivo Lopinavir (10 mg/kg, orally) results in Cmax of 0.8 μg/mL and oral bioavailability of 25% in rats. [1]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: Sprague-Dawley-derived rats or cynomolgus monkeys
  • Formulation: Mixture of ethanol-propylene glycol-D5W
  • Dosages: 10 mg/kg
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 126 mg/mL (200.38 mM)
Ethanol 126 mg/mL (200.38 mM)
Water Insoluble
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.
30 mg/mL

* 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.

Chemical Information

Molecular Weight 628.8
Formula

C37H48N4O5

CAS No. 192725-17-0
Storage powder
in solvent
Synonyms ABT-378

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03394196 Recruiting HIV-2 Infection University of Washington|Clinique des Maladies Infectieuses CHNU de Fann Dakar Senegal|Centre de Sante de Ziguinchor Casamance Senegal|Janssen Pharmaceutica|Merck Sharp & Dohme Corp.|National Institute of Allergy and Infectious Diseases (NIAID) July 4 2018 Not Applicable
NCT03394196 Recruiting HIV-2 Infection University of Washington|Clinique des Maladies Infectieuses CHNU de Fann Dakar Senegal|Centre de Sante de Ziguinchor Casamance Senegal|Janssen Pharmaceutica|Merck Sharp & Dohme Corp.|National Institute of Allergy and Infectious Diseases (NIAID) July 4 2018 Not Applicable
NCT03227653 Completed Efavirenz|Child Behavior|Cognitive Symptom|Medication Adherence|Drug-Related Side Effects and Adverse Reactions Radboud University|Kilimanjaro Christian Medical Centre Tanzania|Kilimanjaro Clinical Research Institute June 19 2017 --
NCT03227653 Completed Efavirenz|Child Behavior|Cognitive Symptom|Medication Adherence|Drug-Related Side Effects and Adverse Reactions Radboud University|Kilimanjaro Christian Medical Centre Tanzania|Kilimanjaro Clinical Research Institute June 19 2017 --
NCT03070470 Completed Drug-induced QT Prolongation|Pharmacokinetics|Pharmacodynamics Food and Drug Administration (FDA)|Spaulding Clinical Research LLC March 14 2017 Phase 1
NCT03070470 Completed Drug-induced QT Prolongation|Pharmacokinetics|Pharmacodynamics Food and Drug Administration (FDA)|Spaulding Clinical Research LLC March 14 2017 Phase 1

Tech Support

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.

Handling Instructions

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Frequently Asked Questions

  • Question 1:

    How should I go about proceeding with in vitro work to attain high concentration of the chemical?

  • Answer:

    S1380 Lopinavir can be dissolved in 2% DMSO, 49%PEG and 49%culture medium at 5 mg/ml.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID