HIV Protease Inhibitor

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.

Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CL^pro inhibitor with an IC₅₀ of 1.61 μM. Ritonavir (ABT 538) can penetrate the blood brain barrier (BBB).

Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with K_is of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity. Lopinavir is also a SARS-CoV 3CL^pro inhibitor with an IC₅₀ of 14.2 μM.

Saquinavir (Ro 31-8959) is an orally active HIV protease inhibitor that can be used in the research of AIDS. Saquinavir also has anti-inflammatory activity and can induce apoptosis of human red blood cells.

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.

PAC-Phe-Val is a potent HIV-1 protease inhibitor with an IC₅₀ value of 33.10 nM. PAC-Phe-Val forms stable and strong interactions with critical active site residues, contributing to its high inhibitory potency. PAC-Phe-Val can be used for HIV/AIDS research.

BILA 1906 BS is a HIV protease inhibitor. BILA 1906 BS prevents HIV-1 replication via inhibition of viral protease-mediated cleavage of Gag and Gag-Pol polyprotein precursors during virion maturation. BILA 1906 BS blocks maturation of p24 proteins in wild-type HIV-1, impairing polyprotein processing and viral maturation. BILA 1906 BS can be used for the research of human immunodeficiency virus type 1 (HIV-1) infection.

Tipranavir-d₅ (PNU-140690-d₅) is the deuterium 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.

Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CL^pro inhibitor with an IC₅₀ of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death.

Darunavir (TMC114), an orally active next generation HIV protease inhibitor, has a similar antiviral activity against the mutant and the wild-type viruses. Darunavir (TMC114) is potent against laboratory HIV-1 strains and primary clinical isolates (IC₅₀ = 0.003 μM; IC₉₀ = 0.009 μM) with minimal cytotoxicity.

Nelfinavir Mesylate (AG 1343 Mesylate) is a potent and orally bioavailable HIV-1 protease inhibitor (K_i=2 nM) for HIV infection. Nelfinavir Mesylate (AG 1343 Mesylate) is a broad-spectrum, anticancer agent.

Indinavir sulfate (MK-639) is an orally active and selective HIV-1 protease inhibitor with a K_i of 0.54 nM for PR. Indinavir sulfate exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir sulfate is also a SARS-CoV 3CL^pro inhibitor.

Saquinavir (Ro 31-8959) mesylate is an orally active HIV protease inhibitor that can be used in the research of AIDS. Saquinavir mesylate also has anti-inflammatory activity and can induce apoptosis of human red blood cells.

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.

Pepstatin (Pepstatin A) Trifluoroacetate 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 Trifluoroacetate also inhibits HIV protease.

Atazanavir (BMS-232632) sulfate is a highly selective and orally active HIV-1 protease inhibitor with blood-brain barrier permeability. Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir sulfate is also a SARS-CoV 3CL^pro inhibitor with an IC₅₀ of 3.49 μM. Atazanavir sulfate inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death.

Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV 3CL^pro inhibitor with an IC₅₀ of 1.09 μM.

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.

Pepstatin (Pepstatin A) Ammonium 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 Ammonium also inhibits HIV protease.

Rosamultin is a 19 α-hydroxyursane-type triterpenoid isolated from Potentilla anserina?L. Rosamultin has inhibitory effects against HIV-1 protease. Rosamultin has the potential for treating H₂O₂-induced oxidative stress injury through its antioxidant and antiapoptosis effects.