Description

Product Description

SKF 107457 is a small-molecule inhibitor of HIV-1 protease, a critical enzyme required for the replication and maturation of the human immunodeficiency virus (HIV). By targeting this enzyme, SKF107457 prevents the cleavage of viral polyproteins, thereby inhibiting the production of mature, infectious viral particles. Due to its mechanism of action, SKF 107457 plays an important role in AIDS research, particularly in studies focused on viral life cycle, antiviral drug resistance, and protease inhibitor development.

As one of the earlier research tools in the class of HIV-1 protease inhibitors, SKF 107457 remains relevant for mechanistic studies, structure-activity relationship (SAR) exploration, and comparative drug profiling. Although not developed as a clinical therapeutic, it provides unique insights into the molecular interactions between inhibitors and the HIV protease active site.

Key research highlights:

• Inhibition of HIV-1 Protease: SKF 107457 binds to the active site of HIV-1 protease, blocking substrate access and enzymatic activity.

• Interruption of Viral Replication: Prevents cleavage of the viral Gag-Pol polyprotein, resulting in immature and non-infectious virions.

• Resistance Studies: Serves as a benchmark molecule for studying mutations in HIV-1 protease that confer drug resistance.

• Structural Biology Tool: Used in crystallography and computational docking studies to evaluate enzyme-inhibitor interactions.

SKF 107457 demonstrates excellent stability under laboratory conditions and provides consistent activity in preclinical models. Its availability in GMP-compliant format ensures that researchers have access to highly reliable and reproducible compounds, making it a valuable standard in HIV/AIDS research laboratories worldwide.

Product Specifications

SKF 107457 offers high chemical purity and batch-to-batch consistency, both essential for molecular virology and pharmacology studies. It is typically dissolved in DMSO for use in cell-based assays. Researchers working in structural virology and computational modeling often employ SKF 107457 to investigate ligand-protease binding dynamics and to test resistance-associated mutations.

Mechanism of Action & Research Applications

HIV-1 protease is a dimeric aspartyl protease that cleaves viral polyproteins (Gag and Gag-Pol) into functional proteins required for viral assembly and maturation. Without protease activity, HIV produces immature viral particles that are non-infectious.

Mechanism of Action of SKF 107457:

• Protease Active Site Binding: SKF 107457 fits into the catalytic pocket of HIV-1 protease, blocking substrate access.

• Inhibition of Cleavage: Prevents processing of Gag-Pol polyproteins.

• Failure of Maturation: Leads to formation of immature viral capsids incapable of initiating new infections.

Research Applications:

1. HIV Replication Studies – SKF 107457 is used to map viral replication stages affected by protease inhibition.

2. Drug Resistance Mechanisms – Helps identify mutations in protease that reduce inhibitor binding affinity.

3. Comparative Protease Inhibitor Studies – Benchmark for evaluating potency and selectivity of new inhibitors.

4. Viral Assembly and Morphology – Used to study structural differences between normal and protease-inhibited virions.

5. Computational Docking Studies – Provides structural data for drug design and molecular modeling.

6. Synergy Research – Can be tested in combination with reverse transcriptase inhibitors to simulate multi-drug regimens.

SKF 107457 remains an indispensable molecule in virology labs for decoding viral life cycles, protease function, and resistance evolution. While clinical protease inhibitors have largely replaced it in therapeutic development, its role as a research tool continues to contribute significantly to our understanding of HIV biology.

Side Effects (For Reference in Research Models)

In laboratory and preclinical research, SKF 107457 has been reported to produce the following effects:

• Cellular Toxicity: At high concentrations, cytotoxicity may be observed in cell culture.

• Off-Target Enzyme Inhibition: Possible inhibition of other aspartyl proteases in mammalian cells.

• Resistance Emergence: Long-term culture with SKF 107457 can select for protease mutations, affecting experimental reproducibility.

• Solubility Issues: Poor aqueous solubility may limit in vivo applications without proper formulation.

Experimental Considerations:

• Careful dose titration is required to balance antiviral efficacy and cytotoxicity.

• Proper solvent handling is necessary to ensure reproducibility.

• Controls must be included to account for solvent effects (e.g., DMSO).

• Results should be interpreted with consideration of potential off-target activity.

Disclaimer

For laboratory research use only. Not for human or veterinary use.

Keywords

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