For research use only.
CAS No. 192725-17-0
Lopinavir (ABT-378) is a potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay.
Selleck's Lopinavir (ABT-378) has been cited by 22 publications
Purity & Quality Control
Choose Selective HIV Protease Inhibitors
|Description||Lopinavir (ABT-378) 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)|
|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.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04307693||Terminated||Drug: Lopinavir/ritonavir|Drug: Hydroxychloroquine sulfate||COVID-19||Asan Medical Center||March 11 2020||Phase 2|
|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|
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.