1133378-37-6

Off-White Amorphous Solid

Labeled Darunavir, intended for use as an internal standard for the quantification of Darunavir by GC- or LC-mass spectrometry.

Second generation HIV-1-protease inhibitor; structurally similar to amprenavir. Antiviral

Darunavir-d₉ is intended for use as an internal standard for the quantification of darunavir (Item Nos. 15866 | 31083) by GC- or LC-MS. Darunavir is an HIV-1 protease inhibitor. It is active against HIV-1_LAI 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). Formulations containing darunavir have been used in combination therapy for the treatment of HIV.

[1] YASUHIRO KOH. Novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI) UIC-94017 (TMC114) with potent activity against multi-PI-resistant human immunodeficiency virus in vitro.[J]. Antimicrobial Agents and Chemotherapy, 2003: 3123-3129. DOI: 10.1128/aac.47.10.3123-3129.2003
[2] BOGHUMA KABISEN TITANJI. Protease inhibitors effectively block cell-to-cell spread of HIV-1 between T cells.[J]. Retrovirology, 2013, 10: 161. DOI: 10.1186/1742-4690-10-161