Nelfinavir Mesylate

Catalog No.S4282 Synonyms: Viracept, AG1343

Nelfinavir Mesylate Chemical Structure

Molecular Weight(MW): 663.89

Nelfinavir Mesylate is a potent HIV protease inhibitor with Ki of 2 nM.

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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

Animal Research:

[1]

+ Expand
  • Animal Models: Sprague-Dawley rats
  • Formulation: 5% dextrose
  • Dosages: 12.5 to 25 mg/kg (i.v); 25 to 50 mg/kg (oral)
  • Administration: i.v and oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (150.62 mM)
Ethanol 100 mg/mL (150.62 mM)
Water 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.

Chemical Information

Molecular Weight 663.89
Formula

C33H49N3O7S2

CAS No. 159989-65-8
Storage powder
in solvent
Synonyms Viracept, AG1343

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03829020 Not yet recruiting Recurrent Plasma Cell Myeloma|Refractory Plasma Cell Myeloma Mayo Clinic|National Cancer Institute (NCI) March 1 2019 Phase 1
NCT03829020 Not yet recruiting Recurrent Plasma Cell Myeloma|Refractory Plasma Cell Myeloma Mayo Clinic|National Cancer Institute (NCI) March 1 2019 Phase 1
NCT03050060 Recruiting Metastatic Renal Cell Cancer|Recurrent Melanoma|Recurrent Non-Small Cell Lung Carcinoma|Recurrent Renal Cell Carcinoma|Stage IV Cutaneous Melanoma AJCC v6 and v7|Stage IV Non-Small Cell Lung Cancer AJCC v7|Stage IV Renal Cell Cancer AJCC v7 University of Washington|National Cancer Institute (NCI) June 9 2017 Phase 2
NCT03050060 Recruiting Metastatic Renal Cell Cancer|Recurrent Melanoma|Recurrent Non-Small Cell Lung Carcinoma|Recurrent Renal Cell Carcinoma|Stage IV Cutaneous Melanoma AJCC v6 and v7|Stage IV Non-Small Cell Lung Cancer AJCC v7|Stage IV Renal Cell Cancer AJCC v7 University of Washington|National Cancer Institute (NCI) June 9 2017 Phase 2
NCT03077451 Recruiting Recurrent Kaposi Sarcoma|Skin Kaposi Sarcoma AIDS Malignancy Consortium|National Cancer Institute (NCI)|The EMMES Corporation|University of Arkansas|University of California Los Angeles|AIDS and Cancer Specimen Resource March 13 2017 Phase 2
NCT03077451 Recruiting Recurrent Kaposi Sarcoma|Skin Kaposi Sarcoma AIDS Malignancy Consortium|National Cancer Institute (NCI)|The EMMES Corporation|University of Arkansas|University of California Los Angeles|AIDS and Cancer Specimen Resource March 13 2017 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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HIV Protease Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID