Lopinavir (ABT-378)

For research use only.

Catalog No.S1380

22 publications

Lopinavir (ABT-378) Chemical Structure

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.

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10mM (1mL in DMSO) USD 82 In stock
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Selleck's Lopinavir (ABT-378) has been cited by 22 publications

Purity & Quality Control

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Biological Activity

Description Lopinavir (ABT-378) 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 M2HlRWZ2dmO2aX;uJIF{e2G7 NUW0XXhvSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEmYMjDFTG8hcW5iTWSyJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZicEK0JGdi\yCycn;0[YlvKGW6cILld5Nqd25iYomgUXRVKGG|c3H5MEBGSzVyPUCuNFAzPiEQvF2= MknwNVc{PzF6MUG=
HEK293 cells MlflSpVv[3Srb36gZZN{[Xl? M1XWWVQ5KGh? MkmxRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4Sge4lt\CC2eYDlJGhKXjFiTly0MVMhcW5iSFXLNlk{KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDy[ZBtcWOjdHnvck1l\W[oZXP0bZZmKGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[U1j[XOnZDDwbIVvd3S7cHnjJIF{e2G7LDDFR|UxRTBwMECyPEDPxE1? MVWxO|Y{QDZ7NB?=
human MT4 cells MW\GeY5kfGmxbjDhd5NigQ>? NXXmW41vPSCmYYnz MnfIRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXOiCPUzDpcoZm[3SnZDDpckBpfW2jbjDNWFQh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjD2bZJ2eyCycn;keYN1cW:wIHHmeIVzKDViZHH5d{BjgSCOZX70bU1TXCCjY4Tpeol1gSCjc4PhfUwhTUN3ME2wMlAxPiEQvF2= MWCxO|U4Pjh2OB?=
human PBMC cells M2naSGZ2dmO2aX;uJIF{e2G7 MXO1JIRigXN? MUPBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDITXYzKE2VIHnu[oVkfGWmIHnuJIh2dWGwIGDCUWMh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjD2bZJ2eyCycn;keYN1cW:wIHHmeIVzKDViZHH5d{BjgSCOZX70bU1TXCCjY4Tpeol1gSCjc4PhfUwhTUN3ME2wMlAyPSEQvF2= NED5Vo4yPzV5Nki0PC=>

... 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]
- Collapse
  • Animal Models: Sprague-Dawley-derived rats or cynomolgus monkeys
  • Dosages: 10 mg/kg
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 126 mg/mL (200.38 mM)
Water Insoluble
Ethanol '126 mg/mL
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 N/A
Smiles CC1=C(C(=CC=C1)C)OCC(=O)NC(CC2=CC=CC=C2)C(CC(CC3=CC=CC=C3)NC(=O)C(C(C)C)N4CCCNC4=O)O

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
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Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

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Molarity Calculator

Mass Concentration Volume Molecular Weight

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

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

Tel: +1-832-582-8158 Ext:3

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID