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Bictegravir

Catalog No. T4493 CAS 1611493-60-7

Synonyms: GS-9883

Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase (IC50: 7.5 nM).

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Bictegravir, CAS 1611493-60-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 43.00
5 mg	In stock	$ 61.00
10 mg	In stock	$ 97.00
25 mg	In stock	$ 195.00
50 mg	In stock	$ 328.00
100 mg	In stock	$ 493.00
500 mg	In stock	$ 1,120.00
1 mL * 10 mM (in DMSO)	In stock	$ 60.00

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Purity: 99.98%

Purity: 97.6%

Biological Description

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Description	Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase (IC50: 7.5 nM).
Targets&IC50	HIV-1 integrase:7.5 nM
In vitro	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 inhibits the strand transfer activity with an IC50 of 7.5 nM. Relative to its inhibition of strand transfer activity, Bictegravir is a much weaker inhibitor of the 3′-processing activity of HIV-1 IN, with an IC50 of 241 nM. Bictegravir enhances the accumulation of 2-LTR circles ~5-fold relative to the mock-treated control and reduces the number of authentic integration products in infected cells by 100-fold. Bictegravir exhibits potent antiviral effects in both primary CD4+ T lymphocytes and monocyte-derived macrophages, with EC50s of 1.5 nM and 6.6 nM, respectively, which are comparable to values obtained in T-cell lines[1].
Cell Research	MT-2 cells are infected in bulk culture with HIV-1 IIIb at a cell density of 2×10^6 cells/mL for 3 h at 37°C. Infected MT-2 cells receive either DMSO (mock-treated control) or Bictegravir at a final concentration greater than or equal to 20 times their respective antiviral 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, late reverse transcription products, and integration junctions (Alu-LTR) are normalized to the level of host globin gene in each sample[1].

Synonyms	GS-9883
Molecular Weight	449.38
Formula	C21H18F3N3O5
CAS No.	1611493-60-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 80 mg/mL

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

EMA Approved Drug Library Drug Repurposing Compound Library Inhibitor Library NO PAINS Compound Library PPI Inhibitor Library Orally Active Compound Library Approved Drug Library Drug-induced Liver Injury (DILI) Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

Bictegravir 1611493-60-7 Microbiology/Virology Proteases/Proteasome HIV Protease HIV Integrase Inhibitor GS9883 HIV Human immunodeficiency virus inhibit GS-9883 GS 9883 inhibitor

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