Home Microbiology Integrase inhibitor - COVID-19 inhibitor Bictegravir For research use only.

Bictegravir

Synonyms: GS-9883

Bictegravir (GS-9883) is a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase.

Bictegravir Chemical Structure

Bictegravir Chemical Structure

CAS No. 1611493-60-7

Purity & Quality Control

Bictegravir Related Products

Signaling Pathway

Integrase Signaling Pathways

Integrase Signaling Pathway

Biological Activity

Description Bictegravir (GS-9883) is a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase.
Targets
HIV-1 integrase [1]
In vitro
In vitro Bictegravir exhibits potent and selective in vitro antiretroviral activity in both T-cell lines and primary human T lymphocytes, with 50% effective concentrations ranging from 1.5 to 2.4 nM and selectivity indices up to 8,700 relative to cytotoxicity. Bictegravir inhibits the strand transfer activity with an IC50 of 7.5 ± 0.3 nM. Relative to its inhibition of strand transfer activity, Bictegravir is a much weaker inhibitor of 3'-processing activity of HIV-1 integrase, with an IC50 of 241 ± 51 nM. Bictegravir potently inhibits HIV-1 replication in both MT-2 and MT-4 cells with EC50s of 1.5 and 2.4 nM, respectively, and selectivity indices (50% cytotoxic concentration [CC50]/EC50) of ∼6,800 in MT-2 cells and ∼1,500 in MT-4 cells[1].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06104306 Recruiting
HIV-1-infection
Gilead Sciences
 December 13 2023 Phase 4
NCT05602506 Active not recruiting
HIV Infections
Fundacion Clinic per a la Recerca Biomédica
 November 15 2022 Phase 4
NCT05222945 Unknown status
HIV-1-infection
ANRS Emerging Infectious Diseases|Gilead Sciences
 February 1 2022 Not Applicable

Chemical Information & Solubility

Molecular Weight 449.38 Formula

C21H18F3N3O5
CAS No. 1611493-60-7 SDF --
Smiles C1CC2CC1N3C(O2)CN4C=C(C(=O)C(=C4C3=O)O)C(=O)NCC5=C(C=C(C=C5F)F)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 90 mg/mL ( (200.27 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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