Nelfinavir Mesylate

Catalog No.S4282 Batch:S428205

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Technical Data

Formula

C33H49N3O7S2
Molecular Weight 663.89 CAS No. 159989-65-8
Solubility (25°C)* In vitro DMSO 100 mg/mL (150.62 mM)
Ethanol 100 mg/mL (150.62 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.83mg/ml Taking the 1 mL working solution as an example, add 50 μL of 16.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Nelfinavir Mesylate is a potent HIV protease inhibitor with Ki of 2 nM.
Targets
HIV protease [1]
(Cell-free assay)
2 nM(Ki)
In vivo In vivo studies indicate that AG1343 is well absorbed orally in a variety of species and possesses favorable pharmacokinetic properties in humans. Initial investigation of the compound in fed rats indicated an oral bioavailability of 43%. In contrast, the oral bioavailability was significantly reduced in fasted rats to 29%. Nelfinavir demonstrated significant oral bioavailabilability across a range of species including dogs (47%), marmosets (17%), and cynomolgus monkeys (26%). It has a long plasma half-life after oral dosing that is likely due to a combination of slow dissolution and absorption. nelfinavir is well absorbed in humans particularly when administered with food and possesses minimal and easily managed side effects[1].

Protocol (from reference)

Animal Study:

[1]
  • Animal Models

    Sprague-Dawley rats

  • Dosages

    12.5 to 25 mg/kg (i.v); 25 to 50 mg/kg (oral)

  • Administration

    i.v and oral administration

Selleck's Nelfinavir Mesylate has been cited by 18 publications

Stabilization of the Dimeric State of SARS-CoV-2 Main Protease by GC376 and Nirmatrelvir [ Int J Mol Sci, 2023, 24(7)6062] PubMed: 37047038
Stabilization of the Dimeric State of SARS-CoV-2 Main Protease by GC376 and Nirmatrelvir [ Int. J. Mol. Sci, 2023, 10.3390/ijms24076062] PubMed: None
Co-administration of Favipiravir and the Remdesivir Metabolite GS-441524 Effectively Reduces SARS-CoV-2 Replication in the Lungs of the Syrian Hamster Model [ mBio, 2022, 13(1):e0304421] PubMed: 35100870
Integrative multiomics and in silico analysis revealed the role of ARHGEF1 and its screened antagonist in mild and severe COVID-19 patients [ J Cell Biochem, 2022, 10.1002/jcb.30213] PubMed: 35037717
Aspartyl Protease Inhibitors as Anti-Filarial Drugs [ Pathogens, 2022, 11(6)707] PubMed: 35745561
Drug target inference by mining transcriptional data using a novel graph convolutional network framework [ Protein Cell, 2021, 10.1007/s13238-021-00885-0] PubMed: 34677780
Direct derivation of human alveolospheres for SARS-CoV-2 infection modeling and drug screening [ Cell Rep, 2021, 35(10):109218] PubMed: 34038715
Multiple Myeloma Cells Depend on the DDI2/NRF1-mediated Proteasome Stress Response for Survival [ Blood Adv, 2021, bloodadvances.2020003820] PubMed: 34649278
Characterization of fluorescent probe substrates to develop an efficient high-throughput assay for neonatal hepatic CYP3A7 inhibition screening [ Sci Rep, 2021, 11(1):19443] PubMed: 34593846
Prevention of SARS-CoV-2 Proliferation with a Novel and Potent Main Protease Inhibitor by Docking, ADMET, MM-PBSA, and Molecular Dynamics Simulation [ World Scientific, 2021, Vol. 20, No. 03, pp. 305-322] PubMed: None

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.