Shelf life (days): 1460.0
Formulation: A solid
Formal Name: (4R,12aS)-N-((2,4-difluorophenyl-3,5,6-d3)methyl-d2)-7-hydroxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxamide
Purity: ≥99% deuterated forms (d1-d5)
Formula Markup: C20H14D5F2N3O5
Formula Weight: 424.409186
Notes: Dolutegravir-d5 is intended for use as an internal standard for the quantification of dolutegravir (Item No. 22191) by GC- or LC-MS. Dolutegravir is a potent inhibitor of HIV integrase with an IC50 value of 2.7 nM for HIV-1 integrase-catalyzed strand transfer in vitro.{40090} It inhibits HIV-1 viral replication (EC50 = 0.51 nM) in peripheral blood mononuclear cells (PBMCs). The cytotoxic concentration (CC50) values for dolutegravir in unstimulated and stimulated PBMCs are 189 and 52 µM, respectively, resulting in a therapeutic index of at least 9,400. It prevents replication of several HIV-1 strains (EC50s = 0.36-2.1 nM) that are resistant to nucleoside reverse transcriptase inhibitors (NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), and protease inhibitors and impairs their ability to infect CIP4 cells.{40090,40091} Formulations containing dolutegravir have been used to treat HIV-1 infection in humans.{40092}
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