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.

Size Price Stock Quantity  
In DMSO USD 82 In stock
USD 90 In stock
USD 570 In stock
USD 970 In stock

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1 Customer Review

  • 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.

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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]

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
+ 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 <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02845843 Not yet recruiting Middle East Respiratory Syndrome Coronavirus (MERS-CoV) King Abdullah International Medical Research Center July 2016 Phase 2|Phase 3
NCT02671383 Recruiting HIV Infections Willem Daniel Francois Venter|Medical Research Council, South Africa|University of Witwatersrand, South Africa July 2016 Phase 3
NCT02712801 Not yet recruiting HIV/AIDS and Infections National Center for Women and Childrens Health, China CDC|National Center for AIDS/STD Control and Prevention, China CDC|Maternal and Child Health Hospital of Yunan Province|Maternal and Child Health Hospital of Sichuan Province|Maternal and Child Health Hospital of Guangxi Province|Maternal and Child Health Hospital of Xinjiang Uygur Autonomous Region|Maternal and Child Health Hospital of Guangdong Province April 2016 Phase 4
NCT02150993 Recruiting HIV-2 Infection French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS) January 2016 Phase 2|Phase 3
NCT01700790 Recruiting AIDS|Tuberculosis University of Miami|Oswaldo Cruz Foundation January 2016 Phase 4
NCT02581202 Active, not recruiting HIV-1 Infection AbbVie December 2015 --

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.

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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.

HIV Protease Signaling Pathway Map

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