Bictegravir

Modify Date: 2024-01-02 06:37:00

Bictegravir Structure
Bictegravir structure
 Common Name Bictegravir
CAS Number 1611493-60-7 Molecular Weight 449.380
Density 1.62±0.1 g/cm3 Boiling Point 682.5±55.0 °C at 760 mmHg
Molecular Formula C21H18F3N3O5 Melting Point N/A
MSDS N/A Flash Point 366.6±31.5 °C

 Use of Bictegravir


Bictegravir is a novel, potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.

 Names

Name Bictegravir
Synonym More Synonyms

 Bictegravir Biological Activity

Description Bictegravir is a novel, potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.
Related Catalog
Target

IC50: 7.5 nM (HIV-1 integrase)[1]
In Vitro Bictegravir (BIC) 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 IN, with an IC50 of 241±51 nM. Bictegravir enhances the accumulation of 2-LTR circles ~5-fold relative to the mock-treated control and reduces the amount of authentic integration products in infected cells by 100-fold. Bictegravir potently inhibits HIV-1 replication in both MT-2 and MT-4 cells with EC50s of 1.5 and 2.4 nM, respectively. Bictegravir exhibits potent antiviral effects in both primary CD4+ T lymphocytes and monocyte-derived macrophages, with EC50s of 1.5±0.3 nM and 6.6±4.1 nM, respectively, which are comparable to values obtained in T-cell lines[1].
Cell Assay MT-2 cells are infected in bulk culture with HIV-1 IIIb at a cell density of 2×106 cells/mL for 3 h at 37°C. Infected MT-2 cells receive either DMSO (mock-treated control) or Bictegravir (BIC) at a final concentration greater than or equal to 20 times their respective antiviral 50% effective concentration (EC50). These plates are incubated at 37°C for either 12 h (for late reverse transcription product quantification) or 24 h (for 2-LTR circle and Alu-LTR product quantification), after which time the cells are harvested for total DNA isolation. DNA is extracted from each well using the DNA minikit and collected as a 100-μL eluate. TaqMan real-time PCR-quantified 2-LTR junctions (2-LTR circles), late reverse transcription products, and integration junctions (Alu-LTR) are normalized to the level of host globin gene in each sample[1].
References

[1]. Tsiang M, et al. Antiviral Activity of Bictegravir (GS-9883), a Novel Potent HIV-1 Integrase Strand Transfer Inhibitor with an Improved Resistance Profile. Antimicrob Agents Chemother. 2016 Nov 21;60(12):7086-7097.

 Chemical & Physical Properties

Density 1.62±0.1 g/cm3
Boiling Point 682.5±55.0 °C at 760 mmHg
Molecular Formula C21H18F3N3O5
Molecular Weight 449.380
Flash Point 366.6±31.5 °C
Exact Mass 449.119843
LogP -1.26
Vapour Pressure 0.0±2.2 mmHg at 25°C
Index of Refraction 1.664
Storage condition 2-8℃
Water Solubility Very slightly soluble (0.17 g/L) (25 ºC)

 Synonyms

bictegravir
GS-9883-01
UNII:8GB79LOJ07
(1S,11R,13R)-5-Hydroxy-3,6-dioxo-N-(2,4,6-trifluorobenzyl)-12-oxa-2,9-diazatetracyclo[11.2.1.0.0]hexadeca-4,7-diene-7-carboxamide
GS-9883
(2R,5S,13aR)-8-hydroxy-7,9-dioxo-N-[(2,4,6-trifluorophenyl)methyl]-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide
2,5-Methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide, 2,3,4,5,7,9,13,13a-octahydro-8-hydroxy-7,9-dioxo-N-[(2,4,6-trifluorophenyl)methyl]-, (2R,5S,13aR)-
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Related Compounds: More...
Bictegravir Sodium
1807988-02-8
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