Nelfinavir Mesylate
Based on 19 publication(s) in Google Scholar
Nelfinavir Mesylate (AG 1343 Mesylate) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir Mesylate (AG 1343 Mesylate) is a broad-spectrum, anticancer agent.
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- Reinheit : 99.75%
- CAS. Nr.: 159989-65-8
- Formel: C33H49N3O7S2
- Molecular Weight:663.89
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Nelfinavir Mesylate
More- Signal Transduct Target Ther. 2025 Dec 15;10(1):406. [Abstract]
- Signal Transduct Target Ther. 2021 May 29;6(1):212. [Abstract]
- Nat Commun. 2020 Sep 4;11(1):4417. [Abstract]
- Mol Ther Oncol. 2026 Jan 23;34(1):201137. [Abstract]
- J Med Chem. 2021 Mar 11;64(5):2725-2738. [Abstract]
- Cells. 2022 Nov 12;11(22):3580. [Abstract]
- Int J Antimicrob Agents. 2019 Dec;54(6):814-819. [Abstract]
- Cell Signal. 2020 Nov:75:109775. [Abstract]
- Acta Biochim Biophys Sin (Shanghai). 2026 Aug 11.
- Mol Oncol. 2026 Jun 5. [Abstract]
- Antiviral Res. 2022 Jun;202:105311. [Abstract]
- Antimicrob Agents Chemother. 2020 Aug 20;64(9):e00872-20. [Abstract]
- Viruses. 2022 Jun 23;14(7):1369. [Abstract]
- PLoS One. 2015 Aug 11;10(8):e0134707. [Abstract]
- Res Sq. 2026 Jun 1.
- Patent. US20250123269A1.
- bioRxiv. 2024 November 03.
- bioRxiv. 2021 Feb 1.
- bioRxiv. 2020 May.
Customer Validation & Images
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WB
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Histological Imaging/Staining
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Histological Imaging/Staining
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
HIV-1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CCRF-CEM | ED50 |
14 nM
Compound: 11a (AG1343)
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Concentration required to inhibit against HIV strain IIIB in CEM cell
Concentration required to inhibit against HIV strain IIIB in CEM cell
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[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 3CLpro 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. Further protocols information, click here.
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Cell Line:RPMI, LP1, U266, OPM2 and MM1S cells
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Concentration:1, 2, 5, 10 μM
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Incubation Time:48 hours
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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.
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Cell Line:LP1 and U266 cells
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Concentration:1-10 μM
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Incubation Time:17 hours
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Result:Induced a dose-dependent increase in the percentage of annexin V+/propidium iodide+ cells.
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Cell Line:U266 cells
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Concentration:5 μM
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Incubation Time:0-24 hours
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Result:The level of AKT phosphorylation in U266 cells decreased.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/SCID mice (bearing U266-luc cells)[4]
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Dosage:75 mg/kg
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Administration:I.p.; 5 days a week for 21 days
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Result:Decreased MM cell growth in NOD/SCID mice.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 159989-65-8
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Appearance Solid
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Molecular Weight 663.89
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Formel C33H49N3O7S2
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Color White to yellow
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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
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Synonyms
AG 1343 Mesylate
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (19)
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Journal Impact Factor
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Most Recent
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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.
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Int J Antimicrob Agents
2019 Dec;54(6):814-819. PMID: 31479744 -
Cell Signal
2020 Nov:75:109775. PMID: 32916277 -
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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.
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Antimicrob Agents Chemother
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 -
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Lösungsmittel & Löslichkeit
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)
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
Reinheit & Dokumentation
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Data Sheet (287 KB)
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Handling Instructions (2659 KB)
Verweise
[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]
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| 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 |
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