Dolutegravir-<wbr/>d<sub>5</sub>

Dolutegravir-d5

CAT N°: 25755
Price:

1,280.00 1,088.00

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}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • (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
  • Correlated keywords
    • deuterated deuterium GSK1349572 GSK-1349572 HIV1 CIP-4 sGSK1349572 sGSK-1349572
  • Product Overview:
    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}

We also advise you