Nelfinavir Mesylate

Catalog No.S4282 Synonyms: Viracept, AG1343

Nelfinavir Mesylate Chemical Structure

Molecular Weight(MW): 663.89

Nelfinavir Mesylate is a potent HIV protease inhibitor with Ki of 2 nM.

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Cited by 5 publications

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Biological Activity

Description Nelfinavir Mesylate is a potent HIV protease inhibitor with Ki of 2 nM.
Targets
HIV protease [1]
(Cell-free assay)
2 nM(Ki)
Assay
Methods Test Index PMID
Growth inhibition assay
Cell viability; 

PubMed: 22271897     


Histograms show the proliferation of RPMI, LP1, U266, OPM2 and MM1S cell lines treated with nelfinavir (1 μM to 10 μM).

22271897
Western blot
p-eIF2Aα / eIF2Aα / ATF4 / GRP78 / CHOP ; 

PubMed: 21697087     


U251 cells were mock-treated (0) or treated with Nelfinavir (NFV) (20 μm) for 4 or 24 h then whole cell lysates were immunoblotted for P-eIF2α, eIF2α, ATF4, GRP78, CHOP, and Ran, as indicated. 

SOD1 / SOD2 / catalase ; 

PubMed: 27280849     


Protein lysates derived from MDA-MB231, MCF-7, or breast epithelial cells, treated with 10 μM nelfinavir for the indicated time points, were immunoblotted with anti- SOD1, anti-SOD2 and anti-catalase. Beta-actin was used as loading control. 

PAX3 / MITF ; 

PubMed: 26977879     


Western blot of the indicated cell lines treated with 10 μM nelfinavir for 24 hr for PAX3, MITF, and ERK2.

21697087 27280849 26977879
Immunofluorescence
LC3 / p62 ; 

PubMed: 27330277     


Immunofluorescence of cells treated with control 0.1% dimethyl sulfoxide or 10 μM nelfinavir for 24 hours. Scale bars indicate 10 μm and apply to all images. Punctate LC3 were quantified as autophagosomes and punctate p62 were quantified as sequestosomes, **P<0.01, ***P<0.001. (C and D) Western blot of lysates prepared following 24 hours of drug treatment. Nelfinavir was used at 10 μM and the autophagy clearance inhibitor chloroquine at 10 μM. 

PAX3 / MITF ; 

PubMed: 26977879     


Immunofluorescence analysis for PAX3 and MITF in WM266-4 cells left untreated or treated with 10 μM nelfinavir for 24 hr; scale bars, 50 μm.

p-SMAD2 ; 

PubMed: 26977879     


Immunofluorescence analysis for phospho-SMAD2 in melanoma cells treated with nelfinavir; scale bars, 10 μm

27330277 26977879
In vivo In vivo studies indicate that AG1343 is well absorbed orally in a variety of species and possesses favorable pharmacokinetic properties in humans. Initial investigation of the compound in fed rats indicated an oral bioavailability of 43%. In contrast, the oral bioavailability was significantly reduced in fasted rats to 29%. Nelfinavir demonstrated significant oral bioavailabilability across a range of species including dogs (47%), marmosets (17%), and cynomolgus monkeys (26%). It has a long plasma half-life after oral dosing that is likely due to a combination of slow dissolution and absorption. nelfinavir is well absorbed in humans particularly when administered with food and possesses minimal and easily managed side effects[1].

Protocol

Animal Research:

[1]
- Collapse
  • Animal Models: Sprague-Dawley rats
  • Formulation: 5% dextrose
  • Dosages: 12.5 to 25 mg/kg (i.v); 25 to 50 mg/kg (oral)
  • Administration: i.v and oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (150.62 mM)
Ethanol 100 mg/mL (150.62 mM)
Water 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 Information

Molecular Weight 663.89
Formula

C33H49N3O7S2
CAS No. 159989-65-8
Storage powder
in solvent
Synonyms Viracept, AG1343

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID