Size | Price | Stock | Qty |
---|---|---|---|
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
Other Sizes |
|
Nelfinavir (formerly AG-1341) is a novel, potent and orally bioavailable HIV-1 protease inhibitor/PI with a Ki of 2 nM. It is used an an antiviral agent for the treatment of HIV infection. Nelfinavir belongs to the class of drugs known as protease inhibitors (PIs) and like other PIs is almost always used in combination with other antiretroviral drugs.
ln Vitro |
Multiple myeloma cell growth is inhibited by nelfinavir (AG1341) (1-10 μM; 48) [4]. Fresh nelfinavir (1-10 μM; 17 hours) causes inflammation in multiple myeloma cell lines and inhibits 26S chymotrypsin amyloid chromosomal activity, damages ischemia, and causes cellular burst in myeloma cell lines [4]. [4] Nelfinavir (5 μM; 0–24 hours) decreases AKT phosphorylation. Anise dye increases caspase-3 stability, decreases ERK1/2, AKT, and STAT-3 phosphorylation, and activates the unfolded protein response system [4]. Another SARS-CoV 3CL pro adaptor with an IC50 of 35.93 μM is nelfinavir.
|
---|---|
ln Vivo |
In NOD/SCID mice, nelfinavir (AG1341) (75 mg/kg; i.p.; 5 days per week for 21 days) inhibits the proliferation of multiple myeloma cells [4].
|
Cell Assay |
Cell proliferation assay [4]
Cell Types: RPMI, LP1, U266, OPM2 and MM1S Cell Tested Concentrations: 1, 2, 5, 10 μM Incubation Duration: 48 hrs (hours) Experimental Results: Inhibition of RPMI , LP1, U266, proliferation. OPM2 and MM1S cell lines were dose-dependent, with IC50 of 1-5 μM. Apoptosis analysis [4] Cell Types: LP1 and U266 Cell Tested Concentrations: 1-10 μM Incubation Duration: 17 hrs (hours) Experimental Results: A dose-dependent increase in the percentage of Annexin V+/propidium iodide+ cells was induced. Western Blot Analysis [4] Cell Types: U266 cells Tested Concentrations: 5 μM Incubation Duration: 0-24 hrs (hours) Experimental Results: AKT phosphorylation level diminished in U266 cells. |
Animal Protocol |
Animal/Disease Models: NOD/SCID (severe combined immunodeficient) mouse (carrying U266-luc cells) [4]
Doses: 75 mg/kg Route of Administration: intraperitoneal (ip) injection; 5 days a week for 21 days Experimental Results: MM cells in NOD/SCID (severe combined immunodeficient) mouse diminished growth. |
References |
[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.
[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. [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. [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. [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. |
Molecular Formula |
C32H45N3O4S
|
---|---|
Molecular Weight |
567.789
|
Exact Mass |
567.3131
|
Elemental Analysis |
C, 67.69; H, 7.99; N, 7.40; O, 11.27; S, 5.65
|
CAS # |
159989-64-7
|
Related CAS # |
Nelfinavir Mesylate;159989-65-8;Nelfinavir-d3;1217629-70-3
|
Appearance |
Solid powder
|
SMILES |
O=C([C@H]1N(C[C@@H](O)[C@@H](NC(C2=CC=CC(O)=C2C)=O)CSC3=CC=CC=C3)C[C@@]4([H])CCCC[C@@]4([H])C1)NC(C)(C)C
|
InChi Key |
QAGYKUNXZHXKMR-HKWSIXNMSA-N
|
InChi Code |
InChI=1S/C32H45N3O4S/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/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)/t22-,23+,26-,27-,29+/m0/s1
|
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
|
Synonyms |
Nelfinavir free base; AG-1343; AG 1343; AG1343; Nelfinavir; Viracept.
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (176.12 mM
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.40 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 25.0 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: ≥ 2.5 mg/mL (4.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (4.40 mM) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.7612 mL | 8.8061 mL | 17.6121 mL | |
5 mM | 0.3522 mL | 1.7612 mL | 3.5224 mL | |
10 mM | 0.1761 mL | 0.8806 mL | 1.7612 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.