Indinavir (sulfate)

Indinavir is an HIV-1 protease inhibitor (Ki = 0.358 nM).1 It is selective for HIV-1 protease over HIV-2 protease (Ki = 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 (Kis = 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.WARNING This product is not for human or veterinary use.

An HIV-1 protease inhibitor

711.9

≥98%

Biochemicals/Antivirals/Protease Inhibitors/Small Molecule Inhibitors/Peptidases & Proteases

Formal_Name:2,3,5-trideoxy-N-[(1S,2R)-2,3-dihydro-2-hydroxy-1H-inden-1-yl]-5-[(2S)-2-[[(1,1-dimethylethyl)amino]carbonyl]-4-(3-pyridinylmethyl)-1-piperazinyl]-2-(phenylmethyl)-D-erythro-pentonamide, monosulfate;Synonyms:Crixivan L-735,524 MK-639

O=C([C@H](CC1=CC=CC=C1)C[C@H](O)CN2CCN(CC3=CN=CC=C3)C[C@H]2C(NC(C)(C)C)=O)N[C@@H]4[C@H](O)CC5=C4C=CC

C36H47N5O4 • H2SO4

157810-81-6

≥ 2 years

DMF: 14 mg/ml DMSO: 20 mg/ml PBS (pH 7.2): 10 mg/ml

1.Bavinger, C.,Bendavid, E.,Niehaus, K., et al. Risk of cardiovascular disease from antiretroviral therapy for HIV: A systematic review. PLoS One 8(3), e59551 (2013).
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 inhibitors. Journal of Medicinal Chemistry 43(18), 3386-3399 (2000).
3.Liu, F.,Boross, P.I.,Wang, Y.F., et al. Kinetic, stability, and structural changes in high-resolution crystal structures of HIV-1 protease with drug-resistant mutations L24I, I50V, and G73S. Journal of Molecular Biology 354(4), 789-800 (2005).