Bictegravir

Catalog No.S5911 Synonyms: GS-9883

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].

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

References

[1] Tsiang M, et al. Antimicrob Agents Chemother. 2016, 60(12):7086-7097.

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
Storage	2 years -80°C in solvent
Synonyms	GS-9883

Bio Calculators

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Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-03-27)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03789968	Not yet recruiting	HIV/AIDS	Thomas Jefferson University\|University of Maryland\|Indiana University Health\|The Brooklyn Hospital Center\|University of Illinois at Chicago\|Nova Southeastern University\|University of California San Francisco	March 1 2019	--
NCT03789968	Not yet recruiting	HIV/AIDS	Thomas Jefferson University\|University of Maryland\|Indiana University Health\|The Brooklyn Hospital Center\|University of Illinois at Chicago\|Nova Southeastern University\|University of California San Francisco	March 1 2019	--
NCT03711253	Not yet recruiting	Acute HIV Infection	University of Southern California	November 2018	Phase 4
NCT03711253	Not yet recruiting	Acute HIV Infection	University of Southern California	November 2018	Phase 4
NCT03499483	Not yet recruiting	HIV Prevention	Fenway Community Health	May 30 2018	Phase 4
NCT03499483	Not yet recruiting	HIV Prevention	Fenway Community Health	May 30 2018	Phase 4

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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Integrase Signaling Pathway Map

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Dilution Calculator

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The Serial Dilution Calculator Equation

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-03-27)

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Integrase Signaling Pathway Map

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By Signaling Pathways

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Bictegravir

Purity & Quality Control

Choose Selective Integrase Inhibitors

Biological Activity

Protocol

References

Solubility (25°C)

Chemical Information

Bio Calculators

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Dilution Calculator

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

The Serial Dilution Calculator Equation

Serial Dilutions

Computed Result

Molecular Weight Calculator

Total Molecular Weight: g/mol

Instructions to calculate molar mass (molecular weight) of a chemical compound:

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

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-03-27)

Tech Support

Integrase Signaling Pathway Map

Related Integrase Products0

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