1. Anti-infection
    Metabolic Enzyme/Protease
  2. HIV Protease
    HIV
  3. Nelfinavir

Nelfinavir (Synonyms: AG1341)

Cat. No.: HY-15287 Purity: 96.90%
Handling Instructions

Nelfinavir (AG-1341) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir is a broad-spectrum, anticancer agent.

For research use only. We do not sell to patients.

Nelfinavir Chemical Structure

Nelfinavir Chemical Structure

CAS No. : 159989-64-7

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10 mM * 1  mL in DMSO USD 125 In-stock
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Based on 6 publication(s) in Google Scholar

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Description

Nelfinavir (AG-1341) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir is a broad-spectrum, anticancer agent[1][2][3].

IC50 & Target[3]

HIV-1

 

In Vitro

Nelfinavir (AG1341) (1-10 μM; 48 hours) inhibits the proliferation of multiple myeloma cells[4].
Nelfinavir inhibits 26S chymotrypsin-like proteasome activity, impairs proliferation and triggers apoptosis of the myeloma cell lines and fresh plasma cells[4].
Nelfinavir (1-10 μM; 17 hours) induces apoptosis of multiple myeloma cell lines[4].
Nelfinavir (5 μM; 0-24 hours) decreases the phosphorylation of AKT[4].
Nelfinavir activates the cleavage of caspase-3, decreases the phosphorylation of AKT, STAT-3, ERK1/2, and activates the pro-apoptotic pathway of the unfolded protein response system[4].

Cell Proliferation Assay[4]

Cell Line: RPMI, LP1, U266, OPM2 and MM1S cells
Concentration: 1, 2, 5, 10 μM
Incubation Time: 48 hours
Result: Inhibited the proliferation of RPMI, LP1, U266, OPM2 and MM1S cell lines in a dose-dependent manner with an IC50 of 1-5 μM.

Apoptosis Analysis[4]

Cell Line: LP1 and U266 cells
Concentration: 1-10 μM
Incubation Time: 17 hours
Result: Induced a dose-dependent increase in the percentage of annexin V+/propidium iodide+ cells.

Western Blot Analysis[4]

Cell Line: U266 cells
Concentration: 5 μM
Incubation Time: 0-24 hours
Result: The level of AKT phosphorylation in U266 cells decreased.
In Vivo

Nelfinavir (AG1341) (75 mg/kg; i.p.; 5 days a week for 21 days) decreases multiple myeloma cell growth in NOD/SCID mice[4].

Animal Model: NOD/SCID mice (bearing U266-luc cells)[4]
Dosage: 75 mg/kg
Administration: I.p.; 5 days a week for 21 days
Result: Decreased MM cell growth in NOD/SCID mice.
Clinical Trial
Molecular Weight

567.78

Formula

C₃₂H₄₅N₃O₄S

CAS No.

159989-64-7

SMILES

[H][[email protected]]12C[[email protected]@H](C(NC(C)(C)C)=O)N(C[[email protected]]([[email protected]@H](NC(C3=C(C)C(O)=CC=C3)=O)CSC4=CC=CC=C4)O)C[[email protected]@]1([H])CCCC2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (176.12 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7612 mL 8.8062 mL 17.6125 mL
5 mM 0.3522 mL 1.7612 mL 3.5225 mL
10 mM 0.1761 mL 0.8806 mL 1.7612 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.40 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.40 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

NelfinavirAG1341AG 1341AG-1341HIV ProteaseHIVHuman immunodeficiency virusproteaseproliferationmultiplemyelomacellsphosphorylationNOproductioninfectionInhibitorinhibitorinhibit

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