Indinavir-d6 (Synonyms: L-735,524-d6, MK-639-d6)

Indinavir-d₆ is intended for use as an internal standard for the quantification of indinavir by GC- or LC-MS. Indinavir is an HIV-1 protease inhibitor (K_i = 0.358 nM).¹ It is selective for HIV-1 protease over HIV-2 protease (K_i = 3.316 nM), as well as human cathepsin D, porcine pepsin, bovine chymosin, human plasma renin, Factor Xa, and elastase at 10 μM. It is also selective for wild-type HIV-1 protease over the protease inhibitor-resistant mutants A-44, K-60, and V-18 (K_is = 0.24, 15, 50, and 40 nM, respectively).² Indinavir is active against multiple HIV-1 variants in cell-based assays (IC₉₅s = 12-100 nM).¹ Formulations containing indinavir have been used in combination with antiretroviral agents in the treatment of HIV infection.

1.Vacca, J.P., Dorsey, B.D., Schleif, W.A., et al.L-735,524: An orally bioavailable human immunodeficiency virus type 1 protease inhibitorProc. Natl. Acad. Sci. U.S.A.91(9)4096-4100(1994) 2.Dorsey, B.D., McDonough, C., McDaniel, S.L., et al.Identification of MK-944a: A second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitorsJ. Med. Chem.43(18)3386-3399(2000)