Lopinavir

Catalog No.S1380

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

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Lopinavir Chemical Structure

Lopinavir Chemical Structure
Molecular Weight: 628.8

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Related Compound Libraries

Lopinavir is available in the following compound libraries:

Product Information

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Product Description

Biological Activity

Description Lopinavir is a potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay.
Targets HIV protease [1]
(Cell-free assay)
IC50 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]
In vivo Lopinavir (10 mg/kg, orally) results in Cmax of 0.8 μg/mL and oral bioavailability of 25% in rats. [1]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

HIV protease inhibition Inhibition of the activity of recombinant wild-type and mutant HIV type 1 (HIV-1) proteases is measured by a continuous fluorometric assay with the internally quenched fluorogenic substrate DABCYL-GABA-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-EDANS. The apparent Ki is estimated by nonlinear regression by the equation for tightly binding inhibitors.

Animal Study: [1]

Animal Models Sprague-Dawley-derived rats or cynomolgus monkeys
Formulation Mixture of ethanol-propylene glycol-D5W
Dosages 10 mg/kg
Administration Orally

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Sham HL, et al. Antimicrob Agents Chemother, 1998, 42(12), 3218-3224.

[2] Kumar GN, et al. Drug Metab Dispos, 1999, 27(1), 86-91.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02845843 Not yet recruiting Middle East Respiratory Syndrome Coronavirus (MERS-CoV) King Abdullah International Medical Research Center July 2016 Phase 2|Phase 3
NCT02671383 Recruiting HIV Infections Willem Daniel Francois Venter|Medical Research Council, S  ...more Willem Daniel Francois Venter|Medical Research Council, South Africa|University of Witwatersrand, South Africa July 2016 Phase 3
NCT02712801 Not yet recruiting HIV/AIDS and Infections National Center for Women and Childrens Health, China CDC  ...more National Center for Women and Childrens Health, China CDC|National Center for AIDS/STD Control and Prevention, China CDC|Maternal and Child Health Hospital of Yunan Province|Maternal and Child Health Hospital of Sichuan Province|Maternal and Child Health Hospital of Guangxi Province|Maternal and Child Health Hospital of Xinjiang Uygur Autonomous Region|Maternal and Child Health Hospital of Guangdong Province April 2016 Phase 4
NCT02150993 Recruiting HIV-2 Infection French National Institute for Health and Medical Research  ...more French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS) January 2016 Phase 2|Phase 3
NCT01700790 Recruiting AIDS|Tuberculosis University of Miami|Oswaldo Cruz Foundation January 2016 Phase 4

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Chemical Information

Download Lopinavir SDF
Molecular Weight (MW) 628.8
Formula

C37H48N4O5

CAS No. 192725-17-0
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms ABT-378
Solubility (25°C) * In vitro DMSO 126 mg/mL (200.38 mM)
Ethanol 126 mg/mL (200.38 mM)
Water <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name (S)-N-((2S,4S,5S)-5-(2-(2,6-dimethylphenoxy)acetamido)-4-hydroxy-1,6-diphenylhexan-2-yl)-3-methyl-2-(2-oxo-tetrahydropyrimidin-1(2H)-yl)butanamide

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.

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.

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

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