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.
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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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3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
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|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||30% PEG400+0.5% Tween80+5% propylene glycol||30 mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02845843||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||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|Guangdong Provincial Maternal and Child Health Hospital||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||--|
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