Name: Lopinavir (ABT-378)
Brand: Selleck Chemicals
SKU: S1380
Availability: InStock
Rating: 5 (45 reviews)

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	HDAC Caspase Proteasome Secretase MMP HCV Protease Cysteine Protease DPP Tyrosinase Serine Protease
Other HIV Protease Inhibitors	Pepstatin A Limonin Temsavir (BMS-626529) Rosamultin Bevirimat Dextran sulfate sodium (DSS) Mericitabine NBD-556 GS-6207 Azvudine

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description
MT2 cells	Function assay		Antiviral activity against HIV2 EHO in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.0026 μM
HEK293 cells	Function assay	48 h	Antiviral activity against wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay, EC50=0.0028 μM
human MT4 cells	Function assay	5 days	Antiviral activity against HIV2 MS infected in human MT4 cells assessed as inhibition of virus production after 5 days by Lenti-RT activity assay, EC50=0.006 μM
human PBMC cells	Function assay	5 days	Antiviral activity against HIV2 MS infected in human PBMC cells assessed as inhibition of virus production after 5 days by Lenti-RT activity assay, EC50=0.015 μM
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (159.03 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	30%PEG400 1 0.5%Tween80 2 5%propylene glycol Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	30.000mg/ml (47.71mM)	Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O to adjust the volume. to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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: μL

Number of animals:

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.

Chemical Information, Storage & Stability

Molecular Weight	628.8	Formula	C₃₇H₄₈N₄O₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	192725-17-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	ABT-378			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

Mechanism of Action

Targets/IC₅₀/Ki	HIV protease (Cell-free assay) 1.3 pM(Ki)
In vitro	Lopinavir (ABT-378) binds to mutant HIV protease (V82A, V82F and V82T) with Ki of 4.9 pM, 3.7 pM and 3.6 pM, respectively. It inhibits 93% of wild-type HIV protease activity at 0.5 nM, and also suppresses HIV protease activity in the absence and presence of 50% HS with EC50 of 17 nM and 102 nM, respectively, in MT4 cells. This compound is converted to several metabolites in an NADPH-dependent manner in liver microsomes with the primary metabolites M-3 and M-4. It is a potent inhibitor of Rh123 efflux in Caco-2 monolayers with IC50 of 1.7 mM. Its exposure (72 hours) in LS 180V cells reduces the content of intracellular Rh123, and it induces P-glycoprotein immunoreactive protein and messenger RNA levels in LS 180V cells. It inhibits subtype C clone C6 with IC50 of 9.4 nM. Additionally, it inhibits CYP3A with IC50 of 7.3 mM in human liver microsomes, while producing negligible or weak inhibition of human CYP1A2, 2B6, 2C9, 2C19 and 2D6.
In vivo	Lopinavir (ABT-378) (10 mg/kg, orally) results in Cmax of 0.8 μg/mL and oral bioavailability of 25% in rats.
References	[1] https://pubmed.ncbi.nlm.nih.gov/9835517/ [2] https://pubmed.ncbi.nlm.nih.gov/9884314/ [3] https://pubmed.ncbi.nlm.nih.gov/12700464/ [4] https://pubmed.ncbi.nlm.nih.gov/12936979/ [5] https://pubmed.ncbi.nlm.nih.gov/12724045/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04335123	Completed	COVID-19	University of Kansas Medical Center	April 4 2020	Phase 1
NCT04307693	Terminated	COVID-19	Asan Medical Center	March 11 2020	Phase 2

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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 it?

Answer:
It can be dissolved in 2% DMSO, 49% PEG and 49% culture medium at 5 mg/ml.

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Lopinavir (ABT-378) HIV Protease inhibitor

Chemical Structure

Molecular Weight: 628.8