Lopinavir (ABT-378)

Catalog No.S1380

For research use only.

Lopinavir (ABT-378) is a potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay.

Lopinavir (ABT-378) Chemical Structure

CAS No. 192725-17-0

Selleck's Lopinavir (ABT-378) has been cited by 29 publications

Purity & Quality Control

Choose Selective HIV Protease Inhibitors

Other HIV Protease Products

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 NFPYV2ZHfW6ldHnvckBie3OjeR?= MojLRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXOiCHSF:gbY4hVVR{IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YheDJ2IFfh[{Bxem:2ZXnuJIV5eHKnc4Ppc44h[nliTWTUJIF{e2G7LDDFR|UxRTBwMECyOkDPxE1? MlLXNVc{PzF6MUG=
HEK293 cells NVzr[HdwTnWwY4Tpc44h[XO|YYm= M4j1flQ5KGh? NX;2VmY1SW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5Qhf2muZDD0fZBmKEiLVkGgUmw1NTNiaX6gTGVMOjl|IHPlcIx{KGGodHXyJFQ5KGi{czDifUBz\XCuaXPheIlwdi2mZX\m[YN1cX[nIHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\S2kYYPl[EBxcGWwb4T5dIlkKGG|c3H5MEBGSzVyPUCuNFAzQCEQvF2= M1zUNVE4PjN6Nkm0
human MT4 cells Ml7ZSpVv[3Srb36gZZN{[Xl? MojJOUBl[Xm| NXfjXWlzSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEmYMjDNV{Bqdm[nY4Tl[EBqdiCqdX3hckBOXDRiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB3cXK3czDwdo9lfWO2aX;uJIFnfGW{IEWg[IF6eyCkeTDM[Y51cS2UVDDhZ5Rqfmm2eTDhd5NigSxiRVO1NF0xNjByNjFOwG0> M1LsXlE4PTd4OES4
human PBMC cells MVfGeY5kfGmxbjDhd5NigQ>? NVXadZVwPSCmYYnz NYj0VJVISW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEmYMjDNV{Bqdm[nY4Tl[EBqdiCqdX3hckBRSk2FIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yhfmm{dYOgdJJw\HWldHnvckBi\nSncjC1JIRigXNiYomgUIVvfGlvUmSgZYN1cX[rdImgZZN{[XluIFXDOVA:OC5yMUWg{txO NVP2NmhsOTd3N{[4OFg>
In vivo Lopinavir (10 mg/kg, orally) results in Cmax of 0.8 μg/mL and oral bioavailability of 25% in rats. [1]

Protocol (from reference)

Animal Research:[1]
  • Animal Models: Sprague-Dawley-derived rats or cynomolgus monkeys
  • Dosages: 10 mg/kg
  • Administration: Orally

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

Chemical Information

Molecular Weight 628.8
Formula

C37H48N4O5

CAS No. 192725-17-0
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04335123 Completed Drug: Losartan COVID-19 University of Kansas Medical Center April 4 2020 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.

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.

Tags: buy Lopinavir (ABT-378) | Lopinavir (ABT-378) supplier | purchase Lopinavir (ABT-378) | Lopinavir (ABT-378) cost | Lopinavir (ABT-378) manufacturer | order Lopinavir (ABT-378) | Lopinavir (ABT-378) distributor