An internal standard for the quantification of darunavir
Darunavir-d9 is intended for use as an internal standard for the quantification of darunavir by GC- or LC-MS. Darunavir is an HIV-1 protease inhibitor.1 It is active against HIV-1LAI in MT-2 cells (IC50 = 3 nM) with a cytotoxic concentration (CC50) of 74.4 μM. Darunavir is also active against wild-type and multidrug-resistant clinical isolates of HIV-1 in phytohemagglutinin-activated peripheral blood mononuclear cells (PHA-PBMCs; IC50s = 3 and 3-29 nM, respectively). It inhibits cell-free diffusion and cell-to-cell spread of HIV-1 in Jurkat cell populations (IC50s = 2.5 and 2.8 nM, respectively).2 Formulations containing darunavir have been used in combination therapy for the treatment of HIV.
1.Koh, Y., Nakata, H., Maeda, K., et al.Novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI) UIC-94017 (TMC114) with potent activity against multi-PI-resistant human immunodeficiency virus in vitroAntimicrob. Agents Chemother.47(10)3123-3129(2003) 2.Titanji, B.K., Aasa-Chapman, M., Pillay, D., et al.Protease inhibitors effectively block cell-to-cell spread of HIV-1 between T cellsRetrovirology10161(2013)
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