Bictegravir sodium 是一种有效的 HIV-1 整合酶抑制剂,其 IC50 值为 7.5 nM。Bictegravir sodium 表现出强大的选择性的抗 HIV 活性和低的细胞毒性。
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Bictegravir sodium is a potent inhibitor of HIV-1 integrase, with an IC50 of 7.5 nM. Bictegravir sodium exhibits potent and selective anti-HIV activity and low cytotoxicity[1].
Bictegravir sodium 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].
[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.
DMNPE-caged ATP diammonium salt
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