|Molecular Formula: C21H14D4F3N3O5|
|Molecular Weight: 453.40|
|Related CAS: 1611493-60-7 (unlabelled)|
|Description||Labelled analog of Bictegravir. Bictegravir is a novel, potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM for strand transfer activity. Bictegravir is a drug of the integrase inhibitor class that was copied from Dolutegravir by scientists at Gilead Sciences. Bictegravir also inhibits HIV-1 viral infection in MT-2 and MT-4 cells, CD4+ T cells, and macrophages (EC50s = 1.5, 2.5, 1.5, and 6.6 nM, respectively) without exhibiting cytotoxicity (CC50s = 10.3, 3.7, 13, and 29.8 μM, respectively). In 2016, bictegravir was in a Phase 3 trial as part of a single tablet regimen in combination with tenofovir alafenamide (TAF) and emtricitabine (FTC) for the treatment of HIV-1 infection.|
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