Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Nelfinavir (also known as AG-1341), is the mesylate salt of nelfinavir, an HIV-1 protease inhibitor with unique, strong, and orally bioavailable antiviral effects. It is used to treat HIV infection as an antiviral agent.
Targets |
HIV-1
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ln Vitro |
Nelfinavir (AG1341) Mesylate (1-10 μM; 48 hours) suppresses the growth of several myeloma cells[4].
Nelfinavir Mesylate suppresses the activity of 26S chymotrypsin-like proteasomes, hinders myeloma cell line proliferation, and induces apoptosis in newly generated plasma cells[4]. Nelfinavir Mesylate (1-10 μM; 17 hours) cell lines undergo apoptosis when exposed to nelfinavir mesylate[4]. Nelfinavir Mesylate (5 μM; 0-24 hours) decreases the phosphorylation of AKT[4]. Nelfinavir Mesylate causes caspase-3 to cleave, phosphorylates AKT, STAT-3, and ERK1/2, and triggers the unfolded protein response system's pro-apoptotic pathway[4]. Nelfinavir has an IC50 of 35.93 μM, making it another SARS-CoV 3CLpro inhibitor[5]. |
ln Vivo |
Nelfinavir Mesylate (75 mg/kg; i.p.; 5 days a week for 21 days) inhibits the growth of multiple myeloma cells in NOD/SCID mice.
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Animal Protocol |
NOD/SCID mice (bearing U266-luc cells)[4]
75 mg/kg I.p.; 5 days a week for 21 days |
References |
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Molecular Formula |
C33H49N3O7S2
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Molecular Weight |
663.8881
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Exact Mass |
663.30
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Elemental Analysis |
C, 59.70; H, 7.44; N, 6.33; O, 16.87; S, 9.66
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CAS # |
159989-65-8
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Related CAS # |
Nelfinavir;159989-64-7
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Appearance |
Solid powder
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SMILES |
CC1=C(C=CC=C1O)C(=O)N[C@@H](CSC2=CC=CC=C2)[C@@H](CN3C[C@H]4CCCC[C@H]4C[C@H]3C(=O)NC(C)(C)C)O.CS(=O)(=O)O
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InChi Key |
NQHXCOAXSHGTIA-SKXNDZRYSA-N
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InChi Code |
InChI=1S/C32H45N3O4S.CH4O3S/c1-21-25(15-10-16-28(21)36)30(38)33-26(20-40-24-13-6-5-7-14-24)29(37)19-35-18-23-12-9-8-11-22(23)17-27(35)31(39)34-32(2,3)4;1-5(2,3)4/h5-7,10,13-16,22-23,26-27,29,36-37H,8-9,11-12,17-20H2,1-4H3,(H,33,38)(H,34,39);1H3,(H,2,3,4)/t22-,23+,26-,27-,29+;/m0./s1
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Chemical Name |
(3S,4aS,8aS)-N-tert-butyl-2-[(2R,3R)-2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-phenylsulfanylbutyl]-3,4,4a,5,6,7,8,8a-octahydro-1H-isoquinoline-3-carboxamide;methanesulfonic acid
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Synonyms |
Nelfinavir mesylate hydrate; AG-1343; AG1343; AG 1343; Nelfinavir; Viracept
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~100 mg/mL (~150.6 mM)
Ethanol: ~100 mg/mL (~150.6 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (7.53 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (7.53 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (7.53 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (3.77 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: ≥ 2.5 mg/mL (3.77 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT03829020 | Active Recruiting |
Drug: Nelfinavir Mesylate Drug: Bortezomib |
Recurrent Plasma Cell Myeloma Refractory Plasma Cell Myeloma |
Mayo Clinic | April 17, 2019 | Phase 1 |
NCT03256916 | Recruiting | Drug: Nelfinavir Drug: Cisplatin |
Carcinoma Cervix,Stage III | Tata Memorial Hospital | January 16, 2018 | Phase 3 |
NCT04169763 | Recruiting | Drug: Nelfinavir Drug: Cisplatin |
Stage II Vulvar Cancer AJCC v8 Stage III Vulvar Cancer AJCC v8 |
M.D. Anderson Cancer Center | August 7, 2020 | Phase 1 |
NCT05036226 | Recruiting | Combination Product: Hydroxychloroquine, Metformin, Sirolimus Combination Product: Hydroxychloroquine, Metformin, Sirolimus, Dasatanib |
Prostate Cancer Recurrent | Medical University of South Carolina |
March 3, 2022 | Phase 1 Phase 2 |
NCT00476606 | Active Recruiting |
Drug: Nevirapine, Efavirenz Drug: Zidovudine, Stavudine, Didanosine, Lamivudine |
HIV Infections | The HIV Netherlands Australia Thailand Research Collaboration |
March 2003 |
Nelfinavir inhibits proliferation of MM cell lines in vitro even in the presence of pro-survival cytokines. Haematologica . 2012 Jul;97(7):1101-9. td> |
Nelfinavir cooperates with anti-myeloma agents to inhibit the proliferation of multiple myeloma cells. Haematologica . 2012 Jul;97(7):1101-9. td> |
Nelfinavir induces the cleavage of pro-caspase 3 and apoptosis in MM cell lines. Haematologica . 2012 Jul;97(7):1101-9. td> |
Nelfinavir induces caspase-independent vacuolization and ER stress. Clin Cancer Res . 2007 Sep 1;13(17):5183-94. td> |
Nelfinavir inhibits NSCLC tumor growth in vivo, and induces markers of apoptosis, ER stress, and autophagy. Clin Cancer Res . 2007 Sep 1;13(17):5183-94. td> |
Effect of chronic exposure to nelfinavir (NEL) on insulin-induced nitric oxide (NO) production by human aortic endothelial cells. Ochsner J . 2013 Spring;13(1):76-90. td> |
Effect of chronic nelfinavir (NEL) exposure on the activation of second messengers of the insulin (INS) signaling cascade. Ochsner J . 2013 Spring;13(1):76-90. td> |