HIV Protease Inhibitor

Nelfinavir (Standard) is the analytical standard of Nelfinavir. This product is intended for research and analytical applications. Nelfinavir (AG-1341) is a potent and orally bioavailable HIV-1 protease inhibitor (K_i=2 nM) for HIV infection. Nelfinavir is a broad-spectrum, anticancer agent.

Ritonavir-d₆ is the deuterium labeled Ritonavir. Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CLpro inhibitor with an IC₅₀ of 1.61 μM.

Atazanavir-d₅ is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC₅₀ of 3.49 μM.

Atazanavir-d₉ is the deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC₅₀ of 3.49 μM.

Indinavir-d₆ is the deuterium labeled Indinavir. Indinavir (MK-639; L735524) is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability.

Amprenavir-d₄ is the deuterium labeled Amprenavir. Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV 3CLpro inhibitor with an IC₅₀ of 1.09 μM.

DPC 684 is a potent and selective HIV-1 protease inhibitor (IC₉₀ = 5.7-40 nM, Ki = 0.021 nM). DPC 684 competitively inhibits HIV-1 protease and blocks viral polyprotein cleavage. DPC 684 has low protein binding and broad-spectrum inhibition against a variety of wild-type and mutant HIV-1 proteases. DPC 684 has low protein binding and broad-spectrum inhibition (IC₉₀ = 1.9-6.3 nM). DPC 684 has research significance for HIV.

PNU-103017 is an HIV protease inhibitor.

Tipranavir-d₇ is deuterated labeled Tipranavir (HY-15148). Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC₅₀s of 66-410 nM. Tipranavir inhibits SARS-CoV-2 3CL^pro activity.

SKF107457 is an HIV-1 protease inhibitor that can be used in AIDS research.

HIV-1 protease-IN-14 (compound 5ae) is a potent HIV-1 protease inhibitor with K_i values of 0.28, 56.9 nM for WT HIV-1 PR, R41T HIV-1 PR, respectively. HIV-1 protease-IN-14 shows low cytotoxicity.

Droxinavir hydrochloride (SC-55389A) is an HIV-1 protease inhibitor. Droxinavir hydrochloride binds to the S2 and S2' subsites of HIV-1 protease, and this interaction is regulated by protease amino acid residue 88, where the N88S mutation confers viral resistance. Droxinavir hydrochloride can be used in studies related to human immunodeficiency virus type 1 infection.

MK-8718 is a potent and orally active HIV protease inhibitor containing a morpholine aspartate binding group. MK-8718 can be used for the research of infection.

HIV Protease Substrate IV is a substrate of HIV protease. HIV Protease Substrate IV can be used to measure the activity of HIV (human immunodeficiency virus) -1 protease.

NIT is an inhibitor of HIV-1 protease (HIV-1p) with K_i values of 96 and 91 μM for WT HIV-1p and MDR HIV-1p, respectively.

HIV-IN-11 is part of the hydroxylaminoglutaramide (HAPA) transition state isomeric series of HIV protease inhibitors and is a potent and selective inhibitor of HIV-1 protease. HIV-IN-11 competitively inhibits HIV-1 PR (Ki: 0.049 nM) and potently inhibits replication of HIV(IIIb)-infected MT4 lymphocytes at concentrations of 25.0-50.0 nM. HIV-IN-11 displays a longer half-life than indinavir sulfate in animal models and serves as a promising second-generation HIV protease inhibitor.

Fosamprenavir-d₄ is the Deuterium-labeled Fosamprenavir (HY-78726). Fosamprenavir is an orally active inhibitor targeting HIV-1 protease and is a prodrug of Amprenavir (HY-17430). Fosamprenavir is hydrolyzed into Amprenavir (VX-478) by cell phosphatases in the intestinal epithelium. Amprenavir binds to the active site of HIV-1 protease, preventing the processing of viral gag and gag-pol polyprotein precursors, thereby inhibiting the formation of mature infectious virus particles and exerting anti-HIV-1 infection activity. Fosamprenavir can be used for the study of human immunodeficiency virus (HIV-1) infection.

RK-682 hemicalcium is the hemicalcium salt form of RK-682 (HY-135564A). RK-682 hemicalcium is the inhibitor for protein tyrosine phosphatase (PTPase), heparanase, phospholipase A2 and HIV-1 protease. RK-682 hemicalcium inhibits the dephosphorylation of CD45 (IC₅₀ is 54 μM) and VHR (IC₅₀ is 2.0 μM), and thereby inhibits the ERK signaling pathway. RK-682 hemicalcium inhibits the cell viability of cancer cell MGH-U3, T24 and UROtsa with IC₅₀s of 78.2, 43.2 and 145 nM, respectively, arrests the cell cycle at G1/S phase, inhibits the cell migration and autophagy in MGH-U3 and T24[2].

Pepstatin (Standard) is the analytical standard of Pepstatin. This product is intended for research and analytical applications. Pepstatin (Pepstatin A) is a specific, orally active aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin also inhibits HIV protease[1][2].

L-738872 is an orally active HIV-l encoded protease inhibitor. L-738872 inhibits the spread of HIV-1 in infected cells.