Nelfinavir Mesylate

For research use only.

Catalog No.S4282 Synonyms: Viracept, AG1343

8 publications

CAS No. 159989-65-8

Nelfinavir Mesylate (Viracept, AG1343) is a potent HIV protease inhibitor with K_i of 2 nM.

Selleck's Nelfinavir Mesylate has been cited by 8 publications

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Biological Activity

Description

Nelfinavir Mesylate (Viracept, AG1343) is a potent HIV protease inhibitor with K_i 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 Haematologica 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 J Biol Chem 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 PLoS One 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 Cancer Cell 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 Drug Des Devel Ther 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 Cancer Cell 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 Cancer Cell 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 Dosages: 12.5 to 25 mg/kg (i.v); 25 to 50 mg/kg (oral) Administration: i.v and oral administration (Only for Reference)

References

[1] Kaldor SW, et al.J Med Chem, 1997,40(24):3979-85.

Solubility (25°C)

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

* 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 Download Nelfinavir Mesylate SDF

Molecular Weight	663.89
Formula	C₃₃H₄₉N₃O₇S₂
CAS No.	159989-65-8
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	Viracept, AG1343
Smiles	CC1=C(C=CC=C1O)C(=O)NC(CSC2=CC=CC=C2)C(CN3CC4CCCCC4CC3C(=O)NC(C)(C)C)O.CS(=O)(=O)O

In vivo Formulation Calculator (Clear solution)

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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 DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，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.

Bio Calculators

Molarity Calculator

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The Serial Dilution Calculator Equation

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Molecular Weight Calculator

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Molarity Calculator

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.

Handling Instructions

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Nelfinavir Mesylate