Lopinavir (ABT-378)

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

Catalog No.S1380
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Lopinavir (ABT-378) Chemical Structure

Lopinavir (ABT-378) Chemical Structure
Molecular Weight: 628.8

Validation & Quality Control

Product Citations(1)

Customer Reviews(1)

Quality Control & MSDS

Related Compound Libraries

Lopinavir (ABT-378) is available in the following compound libraries:

Product Information

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Product Description

Biological Activity

Description Lopinavir (ABT-378) is a potent HIV protease inhibitor with Ki of 1.3 pM.
Targets HIV protease
IC50 1.3 pM (Ki) [1]
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]
Clinical Trials Lopinavir is in phase 4 clinical trial in patients with HIV Infections.
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
1

References

Chemical Information

Download Lopinavir (ABT-378) SDF
Molecular Weight (MW) 628.8
Formula

C37H48N4O5

CAS No. 192725-17-0
Synonyms ABT-378
Solubility (25°C)
  • DMSO 126 mg/mL
  • Water <1 mg/mL
  • Ethanol 126 mg/mL
Storage 2 years -20°CPowder
2 weeks4°Cin DMSO
6 months-80°Cin DMSO
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

Research Area

Customer Reviews (1)


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Source Lopinavir (ABT-378) purchased from Selleck
Method
Cell Lines
Concentrations
Incubation Time
Results

Product Citations (1)

  • Endoplasmic reticulum PI (3) P lipid binding targets malaria proteins to the host cell. [Bhattacharjee S, et al. Cell 2012;148(1-2):201-12]

    PubMed: 22265412

Tech Support & FAQs

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.

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