Raltegravir 99.82%

Raltegravir is a potent integrase strand transfer inhibitor (INSTI) widely studied for its activity against retroviral integrase enzymes. It inhibits wild-type prototype foamy virus integrase (WT PFV IN) with an IC50 of 90 nM and S217Q PFV integrase with an IC50 of 40 nM in cell-free assays.

Raltegravir is recognised as the first approved HIV-1 integrase inhibitor and is used extensively in antiviral, retrovirology, integrase biology, viral replication, and drug-resistance research. It shows strong selectivity for HIV-1 integrase over several related Mg²⁺-dependent enzymes, including HCV polymerase, HIV reverse transcriptase, HIV RNase H, and human α-, β-, and γ-polymerases.

Key Features

• Potent integrase strand transfer inhibitor
• First approved HIV-1 integrase inhibitor
• Inhibits WT PFV integrase with IC50 of 90 nM
• Inhibits S217Q PFV integrase with IC50 of 40 nM
• Demonstrates strong selectivity for HIV-1 integrase over related Mg²⁺-dependent enzymes
• Active in HIV-1, HIV-2, PFV, and SIV-related research models
• Used to study viral integration, replication inhibition, and integrase inhibitor resistance
• Metabolized primarily through glucuronidation in pharmacology studies
• For research use only

Target Profile

Biological Activity

Raltegravir blocks the strand transfer step of retroviral integration, preventing integration of viral DNA into the host genome. This makes it a valuable tool compound for studying retroviral replication and integrase enzyme function.

In vitro studies show that Raltegravir has potent activity against HIV-1, with reported inhibitory activity in human T lymphoid cell cultures. It is also active against HIV-2 in CEMx174 cells and has shown inhibition of SIVmac251 replication in acutely infected human lymphoid CD4+ T-cell lines such as MT-4 and CEMx174.

In Vitro Research Applications

Cell-Based Research Data

PFV Integration Assay Summary

Raltegravir has been evaluated using a quantitative PFV integrase strand transfer assay. The assay measures integration of donor DNA into target DNA in the presence of integrase and magnesium-dependent reaction conditions.

In Vivo Research Summary

Raltegravir has been studied in nonhuman primate models of progressing SIVmac251 infection, where it produced viro-immunological improvement in research settings.

Technical Summary

Storage and Handling Notes

Raltegravir should be handled as a research compound by trained laboratory personnel using appropriate chemical safety procedures.

Recommended handling considerations include:

• Store according to supplier recommendations
• Prepare stock solutions using a suitable solvent as directed by the product documentation
• Avoid repeated freeze-thaw cycles of prepared aliquots
• Protect solutions from unnecessary exposure to light and moisture
• Use appropriate PPE, including gloves, lab coat, and eye protection
• Dispose of chemical waste according to institutional safety procedures

Raltegravir is a potent integrase strand transfer inhibitor used in HIV, SIV, PFV, and broader retrovirology research. With nanomolar activity against PFV integrase targets, strong selectivity for HIV-1 integrase over related Mg²⁺-dependent enzymes, and demonstrated antiviral activity in cellular and animal research models, it is a valuable compound for studying viral integration, replication inhibition, integrase resistance, and antiviral drug mechanisms.