Nelfinavir (AG 1343) Mesylate

For research use only.

Catalog No.S4282 Synonyms: Viracept

13 publications

Nelfinavir (AG 1343) Mesylate Chemical Structure

CAS No. 159989-65-8

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

Selleck's Nelfinavir (AG 1343) Mesylate has been cited by 13 publications

Purity & Quality Control

Choose Selective HIV Protease Inhibitors

Biological Activity

Description Nelfinavir Mesylate (Viracept, AG1343) is a potent HIV protease inhibitor with Ki of 2 nM.
Targets
HIV protease [1]
(Cell-free assay)
2 nM(Ki)
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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OHS-50 NFe2SW9yUFSVIHHzd4F6 MUjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy| NHnvfnU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
RD M37zUpFJXFNiYYPzZZk> MWrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWkRiY3XscJM> MlvuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
MG 63 (6-TG R) MoW2dWhVWyCjc4PhfS=> M2Dve5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCPRzC2N{ApPi2WRzDSLUBk\Wyucx?= NIHG[Fk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
MT2 NVnCVYFLSW62aY\pdoFtKGG|c3H5 M4qxe|Uh\GG7cx?= MlW0RY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4Sge4lt\CC2eYDlJGhKXjFiM1KgbY5n\WO2ZXSgbY4hcHWvYX6gUXQzKGOnbHzzJIF{e2W|c3XkJIF{KH[rcoXzMYlv\HWlZXSgZ5l1d3CjdHjpZ{Bm\m[nY4SgZYZ1\XJiNTDkZZl{KGK7IGjUWEBie3OjeTygSWM2OD1yLkCwOFnPxE1w MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1PFQwLz6FaFXNRmw9N2F-
HepG2 M3[xUGN6fG:2b4jpZ4l1gSCjc4PhfS=> NY\EeJBrPSCmYYnz MmXCR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTIVxTzJiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHHmeIVzKDViZHH5d{BjgSC[VGSgZZN{[XluIFPDOVA:Py52zszNMi=> MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1PFQwLz6FaFXNRmw9N2F-
skeletal myoblast cells MXrDfZRwfG:6aXPpeJkh[XO|YYm= MUW3NkBpd3W{cx?= MkXaSG5FUTpiQ4n0c5RwgGmlaYT5JIlvKF[rdILvMEA4OiCqb4XyMEBqdiC{YYSgd4tmdGW2YXygcZlw[myjc4SgZ4VtdHNuIFnDOVA:OTJwMEZOwG0v NY\Ne4d2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTh2Lze+R4hGVUKOPD;hQi=>
MT2 MlKyR5l1d3SxeHnjbZR6KGG|c3H5 MnrlOUBl[Xm| MVrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNWFIh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGGodHXyJFUh\GG7czDifUBZXFRiYYPzZZktKEOFNUC9NVkvOc7:TT6= MojtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVg1Nyd-Q3jFUWJNRC:jPh?=

... Click to View More Cell Line Experimental Data

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
  • 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)
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

Molecular Weight 663.89
Formula

C33H49N3O7S2

CAS No. 159989-65-8
Storage powder
in solvent
Synonyms Viracept
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)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

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

If you have any other enquiries, please leave a message.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID