Bictegravir (GS-9883) (Synonyms: GS-9883) |
| Catalog No.GC32060 |
빅테그라비르(GS-9883)(GS-9883)는 7.5nM의 IC50으로 HIV-1 인테그라제의 강력한 억제제입니다.
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Cas No.: 1611493-60-7
Sample solution is provided at 25 µL, 10mM.
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Bictegravir is a novel, potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.
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].
[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.
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