Bictegravir

Catalog No.S5911 Synonyms: GS-9883

For research use only.

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

Bictegravir Chemical Structure

CAS No. 1611493-60-7

Selleck's Bictegravir has been cited by 1 Publication

Purity & Quality Control

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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

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].

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 90 mg/mL
(200.27 mM)
Water Insoluble
Ethanol 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 449.38
Formula

C21H18F3N3O5

CAS No. 1611493-60-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC2CC1N3C(O2)CN4C=C(C(=O)C(=C4C3=O)O)C(=O)NCC5=C(C=C(C=C5F)F)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04551573 Withdrawn Drug: Rifapentine daily|Drug: Rifapentine weekly Tuberculosis|Hiv Yale University|Gilead Sciences May 2021 Phase 4
NCT04805944 Recruiting Drug: Dolutegravir|Drug: Bictegravir HIV Infections Cliniques universitaires Saint-Luc- Université Catholique de Louvain March 5 2021 --
NCT04530630 Recruiting Drug: BIKTARVY 50Mg-200Mg-25Mg Tablet HIV Infections|Renal Transplant Rejection Weill Medical College of Cornell University|Gilead Sciences November 9 2020 Phase 4
NCT03858478 Unknown status Drug: Biktarvy arm HIV Seropositivity Institut de Médecine et d''Epidémiologie Appliquée - Fondation Internationale Léon M''Ba November 18 2019 Phase 4

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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