Bictegravir

Catalog No.S5911 Synonyms: GS-9883

Bictegravir Chemical Structure

Molecular Weight(MW): 449.38

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

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Biological Activity

Description Bictegravir is a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase.
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

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 powder
in solvent
Synonyms GS-9883

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
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Molecular Weight Calculator

Molecular Weight Calculator

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Total Molecular Weight: g/mol

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03789968 Enrolling by invitation Drug: bictegravir/emtricitabine/tenofovir alafenamide HIV/AIDS Thomas Jefferson University|University of Maryland College Park|Indiana University Health|The Brooklyn Hospital Center|University of Illinois at Chicago|Nova Southeastern University|University of California San Francisco September 1 2019 --
NCT03858478 Not yet recruiting Drug: Biktarvy arm HIV Seropositivity Institut de Médecine et d''Epidémiologie Appliquée - Fondation Internationale Léon M''Ba March 10 2019 Phase 3
NCT02881320 Recruiting Drug: B/F/TAF (Adult Strength)|Drug: B/F/TAF (Low Dose) HIV-1 Infection Gilead Sciences September 21 2016 Phase 2|Phase 3
NCT02400307 Completed Drug: Bictegravir HIV Gilead Sciences April 17 2015 Phase 1
NCT02275065 Completed Drug: GS-9883|Drug: GS-9883 Placebo HIV-1 Infection Gilead Sciences October 2014 Phase 1

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

Tel: +1-832-582-8158 Ext:3

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Integrase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID