Cat. No.: HY-15287A

Nelfinavir Mesylate

(Synonyms: AG 1343 Mesylate)

18 Cited Publications

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Based on 18 publication(s) in Google Scholar

Nelfinavir Mesylate (AG 1343 Mesylate) is a potent and orally bioavailable HIV-1 protease inhibitor (K_i=2 nM) for HIV infection. Nelfinavir Mesylate (AG 1343 Mesylate) is a broad-spectrum, anticancer agent.

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Pureté: 99.04%
CAS No.: 159989-65-8
Formule: C₃₃H₄₉N₃O₇S₂
Masse moléculaire:663.89

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Nelfinavir Mesylate Chemical Structure

CAS No.: 159989-65-8

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (18)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

HIV-1

Voir tous les produits spécifiques à Isoform HIV :

Cellular Effect

Cell Line	Type	Value	Description	References
CCRF-CEM	ED₅₀	14 nM Compound: 11a (AG1343)	Concentration required to inhibit against HIV strain IIIB in CEM cell Concentration required to inhibit against HIV strain IIIB in CEM cell	[PMID: 9397180]

In Vitro

Nelfinavir (AG1341) Mesylate (1-10 μM; 48 hours) inhibits the proliferation of multiple myeloma cells^[4].
Nelfinavir Mesylate inhibits 26S chymotrypsin-like proteasome activity, impairs proliferation and triggers apoptosis of the myeloma cell lines and fresh plasma cells^[4].
Nelfinavir Mesylate (1-10 μM; 17 hours) induces apoptosis of multiple myeloma cell lines^[4].
Nelfinavir Mesylate (5 μM; 0-24 hours) decreases the phosphorylation of AKT^[4].
Nelfinavir Mesylate 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].
Nelfinavir is also a SARS-CoV 3CL^pro inhibitor with an IC₅₀ of 35.93 μM^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 159989-65-8
Appearance Solid
Masse moléculaire 663.89
Formule C₃₃H₄₉N₃O₇S₂
Color White to yellow
SMILES

[H][C@]12C[C@@H](C(NC(C)(C)C)=O)N(C[C@H]([C@@H](NC(C3=C(C)C(O)=CC=C3)=O)CSC4=CC=CC=C4)O)C[C@@]1([H])CCCC2.CS(=O)(O)=O
Synonyms

AG 1343 Mesylate
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (18)

All Histological Imaging/StainingBio/Physico-chemical AssayCell Migration/Invasion AssayWB

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Journal Impact Factor

Signal Transduct Target Ther

Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]

2025 Dec 15;10(1):406. PMID: 41392286
Signal Transduct Target Ther

Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. [Abstract]

2021 May 29;6(1):212. PMID: 34052830
Nat Commun

Both Boceprevir and GC376 efficaciously inhibit SARS-CoV-2 by targeting its main protease. [Abstract]

2020 Sep 4;11(1):4417. PMID: 32887884
Mol Ther Oncol

Potency-enhancing mutations in E3-19K and i-leader increase the cytolytic activity of the PH20/ SPAM1-armed oncolytic adenovirus Ad5Δ24RGD. [Abstract]

2026 Jan 23;34(1):201137. PMID: 41716467
J Med Chem

Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration. [Abstract]

2021 Mar 11;64(5):2725-2738. PMID: 33619967
Cells

Targeting Wnt/β-Catenin Signaling Exacerbates Ferroptosis and Increases the Efficacy of Melanoma Immunotherapy via the Regulation of MITF. [Abstract]

2022 Nov 12;11(22):3580. PMID: 36429010

Nelfinavir Mesylate purchased from MedChemExpress. Usage Cited in: Cells. 2022 Nov 12;11(22):3580. [Abstract]

Nelfinavir Mesylate (5 µM; 24 h) suppresses expression of MITF in A2058 and A375 cells.
Int J Antimicrob Agents

Efficacy of antiretroviral compounds against Toxoplasma gondii in vitro. [Abstract]

2019 Dec;54(6):814-819. PMID: 31479744
Cell Signal

Nelfinavir inhibits human DDI2 and potentiates cytotoxicity of proteasome inhibitors. [Abstract]

2020 Nov;75:109775. PMID: 32916277
Mol Oncol

Patient therapy outcome modeling in cancer organoids is improved by cancer-associated fibroblasts and organoid assembly convolution. [Abstract]

2026 Jun 5. PMID: 42246237
Antiviral Res

HIV protease inhibitors Nelfinavir and Lopinavir/Ritonavir markedly improve lung pathology in SARS-CoV-2-infected Syrian hamsters despite lack of an antiviral effect. [Abstract]

2022 Jun;202:105311. PMID: 35390430

Nelfinavir Mesylate purchased from MedChemExpress. Usage Cited in: Antiviral Res. 2022 Jun;202:105311. [Abstract]

Cumulative severity score from H&E-stained slides of lungs from SARS-CoV-2-infected hamsters at 4 dpi treated with vehicle, 15 mg/kg Nelfinavir BID, or 50 mg/kg Nelfinavir BID (Nelfinavir:i.p., twice daily for four consecutive days).

Nelfinavir Mesylate purchased from MedChemExpress. Usage Cited in: Antiviral Res. 2022 Jun;202:105311. [Abstract]

Representative H&E-stained slides of lungs from vehicle control (top panel) and 50 mg/kg BID Nelfinavir-treated (bottom panel) SARS-CoV-2-infected hamsters at 4 dpi. Top panel: bronchopneumonia centred on a bronchiol (black arrows) in a vehicle-treated hamster (scale bar at 100 μm). Bottom panel: severe interstitial inflammation with mostly PMN and congestion in a Nelfinavir-treated hamster (scale bar at 100 μm). Black arrows indicate bronchiol (insert at higher magnification, scale bar at 50 μm).

Nelfinavir Mesylate purchased from MedChemExpress. Usage Cited in: Antiviral Res. 2022 Jun;202:105311. [Abstract]

Haematological analysis revealed increases in white blood cell, platelet, and neutrophil counts in Nelfinavir-treated (50 mg/kg, i.p., twice daily for four consecutive days) uninfected animals as compared to the vehicle control.

Nelfinavir Mesylate purchased from MedChemExpress. Usage Cited in: Antiviral Res. 2022 Jun;202:105311. [Abstract]

The neutrophils of Nelfinavir-treated (50 mg/kg, i.p., twice daily for four consecutive days) animals had a higher granularity intensity (Neut-GI) and a higher reactivity intensity (Neut-RI).

Nelfinavir Mesylate purchased from MedChemExpress. Usage Cited in: Antiviral Res. 2022 Jun;202:105311. [Abstract]

Nelfinavir (50 μg/ml, 1 h) significantly enhanced the migration of human neutrophils towards the CXCR1 and CXCR2 agonist CXCL8 (5 and 25 ng/ml) in the Boyden microchamber assay in vitro.
Antimicrob Agents Chemother

Discovery of M Protease Inhibitors Encoded by SARS-CoV-2. [Abstract]

2020 Aug 20;64(9):e00872-20. PMID: 32669265
Viruses

A Newly Engineered A549 Cell Line Expressing ACE2 and TMPRSS2 Is Highly Permissive to SARS-CoV-2, Including the Delta and Omicron Variants. [Abstract]

2022 Jun 23;14(7):1369. PMID: 35891350
PLoS One

The Novel Cyclophilin Inhibitor CPI-431-32 Concurrently Blocks HCV and HIV-1 Infections via a Similar Mechanism of Action. [Abstract]

2015 Aug 11;10(8):e0134707. PMID: 26263487
Res Sq

2026 Jun 1.
Patent

US20250123269A1.
bioRxiv

2024 November 03.
bioRxiv

2021 Feb 1.
bioRxiv

2020 May.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (150.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.5063 mL

7.5314 mL

15.0627 mL

5 mM

0.3013 mL

1.5063 mL

3.0125 mL

10 mM

0.1506 mL

0.7531 mL

1.5063 mL

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

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

Solubility: ≥ 5 mg/mL (7.53 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (7.53 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (7.53 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.5 mg/mL (3.77 mM); Clear solution

Protocol 5

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (3.77 mM); Clear solution

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 10 mg/mL (15.06 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (287 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
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OR (2659 KB)
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Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Mondal D, et al. Nelfinavir suppresses signaling and nitric oxide production by human aortic endothelial cells: protective effects of thiazolidinediones. Ochsner J. 2013 Spring;13(1):76-90. [Content Brief]

[2]. Gills JJ, et al. Nelfinavir, A lead HIV protease inhibitor, is a broad-spectrum, anticancer agent that inducesendoplasmic reticulum stress, autophagy, and apoptosis in vitro and in vivo. Clin Cancer Res. 2007 Sep 1;13(17):5183-94. [Content Brief]

[3]. Kaldor SW, et al. Nelfinavir mesylate (AG1343): a potent, orally bioavailable inhibitor of HIV-1 protease. J Med Chem. 1997 Nov 21;40(24):3979-85. [Content Brief]

[4]. Bono C, et al. The human immunodeficiency virus-1 protease inhibitor nelfinavir impairs proteasome activity and inhibits the proliferation of multiple myeloma cells in vitro and in vivo. Haematologica. 2012;97(7):1101‐1109. [Content Brief]

[5]. Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.5063 mL	7.5314 mL	15.0627 mL	37.6568 mL
	5 mM	0.3013 mL	1.5063 mL	3.0125 mL	7.5314 mL
	10 mM	0.1506 mL	0.7531 mL	1.5063 mL	3.7657 mL
	15 mM	0.1004 mL	0.5021 mL	1.0042 mL	2.5105 mL
	20 mM	0.0753 mL	0.3766 mL	0.7531 mL	1.8828 mL
	25 mM	0.0603 mL	0.3013 mL	0.6025 mL	1.5063 mL
	30 mM	0.0502 mL	0.2510 mL	0.5021 mL	1.2552 mL
	40 mM	0.0377 mL	0.1883 mL	0.3766 mL	0.9414 mL
	50 mM	0.0301 mL	0.1506 mL	0.3013 mL	0.7531 mL
	60 mM	0.0251 mL	0.1255 mL	0.2510 mL	0.6276 mL
	80 mM	0.0188 mL	0.0941 mL	0.1883 mL	0.4707 mL
	100 mM	0.0151 mL	0.0753 mL	0.1506 mL	0.3766 mL

Keywords

Nelfinavir Mesylate

18 Cited Publications

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Nelfinavir Mesylate

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Publications Citing Use of MedChemExpress (MCE) Nelfinavir Mesylate

Voir tous les produits spécifiques à Isoform HIV

Activité biologique

Chemical Information

Publications (18)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Nelfinavir Mesylate Related Classifications

HY-15287A Related Classifications