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Lopinavir

Name: Lopinavir
Brand: TargetMol
SKU: T1623
Price: 41 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T1623Cas No. 192725-17-0

Alias ABT-378

Lopinavir (ABT-378) is a peptidomimetic HIV protease inhibitor effective against HIV protease with the Val 82 mutation. It is less affected by serum protein binding compared to the structurally related drug ritonavir.

Lopinavir

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Purity: 99.62%

Catalog No. T1623Alias ABT-378Cas No. 192725-17-0

Pack Size	Price	USA Warehouse	Global Warehouse
50 mg	$41	In Stock	In Stock
100 mg	$66	In Stock	In Stock
200 mg	$97	In Stock	In Stock
500 mg	$198	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$45	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.62%

Color:White

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	Lopinavir (ABT-378) is a peptidomimetic HIV protease inhibitor effective against HIV protease with the Val 82 mutation. It is less affected by serum protein binding compared to the structurally related drug ritonavir.
Targets&IC50	HIV protease:1.3 pM(Ki)
In vitro	Administering Lopinavir (10 mg/kg, p.o.) to rats resulted in a maximum concentration (Cmax) of 0.8 μg/mL, with the drug's bioavailability being 25%.
In vivo	Lopinavir is an effective inhibitor of Rh123, with an IC50 value of 1.7 mM for Caco-2 cell monolayers. It binds to mutant HIV proteases (V82A, V82T, and V82F) with Ki values of 4.9, 3.7, and 3.6 pM, respectively. At a concentration of 0.5 nM, Lopinavir inhibits the activity of wild-type HIV protease by 93%. It also inhibits HIV protease activity in MT4 cells both in the presence and absence of 50% HS, with EC50 values of 102 nM and 17 nM, respectively. In liver microsomes, Lopinavir is converted to primary metabolites M-3 and M-4, a process that is NADPH-dependent. After treating LS 180V cells with Lopinavir for 72 hours, there is a reduction in intracellular Rh123 content and induction of P-glycoprotein immunoreactive protein and mRNA levels. Lopinavir exhibits an IC50 of 9.4 nM against subtype C clone C6. When acting on human liver microsomes, Lopinavir shows an IC50 of 7.3 mM against CYP3A and exerts weak inhibition on human CYP1A2, 2B6, 2C9, 2C19, and 2D6.
Synonyms	ABT-378

Chemical Properties

Molecular Weight	628.8
Formula	C₃₇H₄₈N₄O₅
Cas No.	192725-17-0
Smiles	[C@@H](C(N[C@@H](CC1=CC=CC=C1)C[C@@H]([C@H](CC2=CC=CC=C2)NC(COC3=C(C)C=CC=C3C)=O)O)=O)([C@@H](C)C)N4C(=O)NCCC4
Relative Density.	1.163 g/cm3 (Predicted)

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 116 mg/mL (184.48 mM), Sonication is recommended.

DMSO: 247.5 mg/mL (393.61 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (6.36 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	1.5903 mL	7.9517 mL	15.9033 mL	79.5165 mL
5 mM	0.3181 mL	1.5903 mL	3.1807 mL	15.9033 mL
10 mM	0.1590 mL	0.7952 mL	1.5903 mL	7.9517 mL
20 mM	0.0795 mL	0.3976 mL	0.7952 mL	3.9758 mL
50 mM	0.0318 mL	0.1590 mL	0.3181 mL	1.5903 mL
100 mM	0.0159 mL	0.0795 mL	0.1590 mL	0.7952 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc