Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity. Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 14.2 μM.
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Lopinavir Chemical Structure
CAS No. : 192725-17-0
This product is a controlled substance and not for sale in your territory.
Based on 15 publication(s) in Google Scholar
Other Forms of Lopinavir:
(rel)-Lopinavir-d8
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Lopinavir-d8
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Lopinavir-d7
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Lopinavir purchased from MedChemExpress. Usage Cited in:
Antiviral Res. 2022 Nov 10;105463.
[Abstract]
Lopinavir (LPV) (0, 1, 5, 10, 20 μM; 24 h) inhibits autophagy in U87 cells in a dose-dependent manner.
Lopinavir purchased from MedChemExpress. Usage Cited in:
Antiviral Res. 2022 Nov 10;105463.
[Abstract]
Lopinavir (LPV) (1, 5, 10, 20, 50 µM; 12, 24, 36, 48 h) inhibits the growth of U87 cells.
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Description
Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity[1][2]. Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 14.2 μM[3].
IC50 & Target
HIV-1
In Vitro
HIV-1 protease is an essential enzyme for production of mature, infective virus[1].
Lopinavir potently inhibits wild-type and mutant HIV protease (Ki= 1.3 to 3.6 pM), blocks the replication HIV type 1 (EC50=0.006 to 0.017 μM), and maintains high potency against mutant HIV selected by Ritonavir in vivo (EC50=≤0.06 μM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Lopinavir Related Antibodies
In Vivo
Coadministration with low-dose Ritonavir significantly improves the pharmacokinetic properties and hence the activity of Lopinavir against HIV-1 protease[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Room temperature in continental US; may vary elsewhere.
Stockage
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
1 year
-20°C
6 months
Solvant et solubilité
In Vitro:
DMSO : 250 mg/mL (397.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
1.5903 mL
7.9517 mL
15.9033 mL
5 mM
0.3181 mL
1.5903 mL
3.1807 mL
10 mM
0.1590 mL
0.7952 mL
1.5903 mL
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 25 mg/mL (39.76 mM); Clear solution
This protocol yields a clear solution of ≥ 25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (250.0 mg/mL) to 900 μLCorn oil, and mix evenly.
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
For the following dissolution methods, please prepare the working solution directly.
It is recommended to prepare fresh solutions and use them promptly within a short period of time. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution.
If precipitation or phase separation occurs during preparation,
heat and/or sonication can be used to aid dissolution.
Solubility: 20 mg/mL (31.81 mM); Suspended solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
[1]. Cvetkovic RS, et al. Lopinavir/ritonavir: a review of its use in the management of HIV infection. Drugs. 2003;63(8):769-802.
[Content Brief]
[2]. Sham HL, et al. ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease. Antimicrob Agents Chemother. 1998;42(12):3218-3224.
[Content Brief]
[3]. Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212.
[Content Brief]
[1]. Cvetkovic RS, et al. Lopinavir/ritonavir: a review of its use in the management of HIV infection. Drugs. 2003;63(8):769-802.
[2]. Sham HL, et al. ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease. Antimicrob Agents Chemother. 1998;42(12):3218-3224.
[3]. Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212.
Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
DMSO
1 mM
1.5903 mL
7.9517 mL
15.9033 mL
39.7583 mL
5 mM
0.3181 mL
1.5903 mL
3.1807 mL
7.9517 mL
10 mM
0.1590 mL
0.7952 mL
1.5903 mL
3.9758 mL
15 mM
0.1060 mL
0.5301 mL
1.0602 mL
2.6506 mL
20 mM
0.0795 mL
0.3976 mL
0.7952 mL
1.9879 mL
25 mM
0.0636 mL
0.3181 mL
0.6361 mL
1.5903 mL
30 mM
0.0530 mL
0.2651 mL
0.5301 mL
1.3253 mL
40 mM
0.0398 mL
0.1988 mL
0.3976 mL
0.9940 mL
50 mM
0.0318 mL
0.1590 mL
0.3181 mL
0.7952 mL
60 mM
0.0265 mL
0.1325 mL
0.2651 mL
0.6626 mL
80 mM
0.0199 mL
0.0994 mL
0.1988 mL
0.4970 mL
100 mM
0.0159 mL
0.0795 mL
0.1590 mL
0.3976 mL
Lopinavir Related Classifications
Anti-infectionMetabolic Enzyme/Protease
HIVHIV ProteaseSARS-CoV
Help & FAQs
Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
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