Description

Product Description

Bictegravir is a synthetic antiviral compound engineered for laboratory research focused on HIV treatment and integrase inhibition. It selectively binds to the active site of HIV integrase, obstructing the strand transfer reaction necessary for viral DNA integration into host cell chromosomes. By preventing integration, Bictegravir halts viral replication at a critical step, making it a valuable tool for mechanistic studies, resistance profiling, and drug development research.

Structurally, Bictegravir possesses a tricyclic carbamoyl pyridone core with functional moieties that enhance chelation with magnesium ions in the integrase active site. This high-affinity binding provides potent inhibitory activity and favorable pharmacokinetic stability in cell-based assays. Researchers employ Bictegravir to investigate the dynamics of integrase–DNA interactions, study viral resistance mutations, and evaluate synergistic effects with reverse transcriptase inhibitors or protease inhibitors.

Preclinical investigations have demonstrated that Bictegravir can reduce viral replication in various human cell lines, including T-cells and macrophages, at nanomolar concentrations. Its utility extends to combination studies, examining additive or synergistic effects with other antiretrovirals, as well as in high-throughput screening for novel antiviral compounds. Bictegravir also serves as a benchmark reference compound for integrase inhibitor development and structural biology studies.

Due to its stability and reproducibility in vitro, Bictegravir is suitable for research into drug metabolism, pharmacodynamics, and mechanisms of HIV resistance. Scientists leverage Bictegravir in assays for quantifying integrase inhibition, studying viral DNA integration efficiency, and evaluating the impact of specific amino acid mutations in the HIV integrase enzyme. This breadth of research applications positions Bictegravir as an essential compound for academic, pharmaceutical, and biotechnology laboratories focused on HIV and retroviral studies.

Product Specifications

Mechanism of Action

Bictegravir selectively inhibits HIV integrase by binding to the active site and coordinating with two magnesium ions essential for catalyzing strand transfer. This blocks the insertion of viral DNA into the host genome, effectively halting HIV replication at the integration stage. Bictegravir exhibits the following mechanisms:

1. Strand Transfer Inhibition
   Bictegravir binds integrase and prevents the covalent insertion of viral DNA ends into the host genome. Structural studies show high-affinity chelation with catalytic magnesium ions, which is critical for enzyme inhibition.

2. Resistance Profile Studies
   Bictegravir serves as a reference for investigating integrase inhibitor-resistant HIV variants. It is utilized in site-directed mutagenesis assays to study the impact of specific amino acid substitutions on drug efficacy.

3. Synergistic Antiviral Effects
   In combination studies, Bictegravir is co-administered with reverse transcriptase or protease inhibitors in cell-based assays to assess additive or synergistic antiviral effects.

4. Cellular Pharmacodynamics
   Bictegravir modulates intracellular viral DNA accumulation by preventing integration, allowing researchers to quantify pre-integration complexes and analyze drug-dependent viral kinetics.

5. Structural and Biochemical Assays
   Bictegravir is used in crystallographic studies of integrase-DNA complexes, enabling detailed mechanistic insights into inhibitor binding and enzyme inhibition.

   

Side Effects (Research Context)

In preclinical laboratory studies, Bictegravir is generally well-tolerated in cell-based assays at nanomolar concentrations. Researchers should monitor cytotoxicity, particularly at higher doses or in prolonged exposure studies. Standard laboratory safety procedures are recommended, including handling under appropriate biosafety levels, wearing PPE, and following chemical handling protocols. Bictegravir is not intended for human or veterinary use.

Keywords

 HIV integrase inhibitor, GS-9883, antiviral research, integrase inhibition, retroviral studies, peptide wholesale China, factory peptide supplier, research chemical, high purity compound, OEM research chemical production

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Disclaimer

All products listed are intended for laboratory research use only and not for human or veterinary use. They are not drugs, medical devices, or diagnostics and should not be administered to humans or animals. Researchers must handle all materials in accordance with institutional biosafety and chemical safety guidelines. The information provided is for scientific reference only and does not imply therapeutic efficacy, safety, or regulatory approval.