HIV Protease Inhibitor

Lopinavir (Standard) is the analytical standard of Lopinavir. This product is intended for research and analytical applications. 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.

HIV-1 protease-IN-13 (compound 18d) is a potent HIV-1 protease inhibitor with an IC₅₀ value of 0.54 nM. HIV-1 protease-IN-13 also shows potent activity against HIV-1DRVRS (DRV-resistant mutation) and HIV-1NL4_3 variant (wild type).

JE-2178 is an orally available HIV-1 protease inhibitor with IC₅₀ and K_i values are 15 and 0.318 nM respectively. JE-2178 has antiviral activity.

HIV-1-IN-91 (Compound BAN) is a HIV-1 protease inhibitor.

HIV-1 protease-IN-7 (compound 16) is an orally active HIV-1 protease inhibitor (IC₅₀=3.52 nM, EC₅₀=37 nM).

Kynostatin 272 (KNI 272) is a potent HIV protease inhibitor. Kynostatin 272 inhibits the activity of the HIV protease by simulating the substrate transition state of the HIV protease, thus preventing a key step in the replication of the HIV virus. Kynostatin 272 provides an important research foundation for the development of drugs for HIV and AIDS.

Agaritine is a compound isolated from the commonly cultivated commercial mushroom Agaricus bisporus. Agaritine is hydrolyzed by an enzyme system present in the mushroom into 4-(hydroxymethyl)benzenediazonium ion, which is a carcinogen in mice. Agaritine is structurally similar to some known carcinogens and can be used for research in cancer and food safety.

Stercobilin hydrochloride (amixture of isomers) is a bile pigment metabolized by gut bacteria, and it's also an HIV protease inhibitor, with a K_i of 4 μM. Stercobilin hydrochloride (a mixture of isomers) can induce pro-inflammatory activity in mouse macrophage RAW264 cells, including the production of TNF-α and IL-1β. Stercobilin hydrochloride (a mixture of isomers) can be used in studies of inflammation and viral infections.

HIV-1 protease-IN-6 (compound 17d) is a potent HIV-1 protease inhibitor, with an IC₅₀ of 21 pM and a K_i of 4.7 pM, respectively. HIV-1 protease-IN-6 exhibits potent antiviral activity to DRV (darunavir)-resistant variant, even more than wild type virus.

GS-9770 is an orally active inhibitor for HIV protease with K_i of 0.16 nM. GS-9770 exhibits antiviral activity aginst HIV-1 strains and HIV-2 strains with EC₅₀ of 1.9-26 nM, and 26 nM. GS-9770 is metabolic stable in human liver microsomes. GS-9770 exhibits good pharmacokinetic characters in Sprague Dawley rats.

L 756423 is a potent HIV protease inhibitor. L 756423 has the potential for the research of HIV infection.

R-87366 is a water-soluble human immunodeficiency virus (HIV) protease inhibitor. R-87366 has potent inhibitory for HIV protease with a K_i value of 11 nM. R-87366 can be used for the research of anti-human immunodeficiency virus (HIV).

U-89360E is an inhibitor for HIV-1 protease. U-89360E inhibits the protease of HIV-1 wildtype, V82D mutant and V82N mutant with K_i of 20 nM, 560 nM and 2100 nM, respectively.

HIV-1-IN-84 (Compound 9) is a potent HIV-1 non-nucleoside reverse transcriptase (HIV-1 RT) inhibitor (IC₅₀=33.89 μM, EC₅₀=540 nM). HIV-1-IN-84 is promising for research of HIV infections.

L 694746 is the metabolite of L-689502 (HY-U00261). L 694746 is an inhibitor for HIV-1 protease with an IC₅₀ of 1 nM and a K_i of 0.34 nM.

Ritonavir-¹³C,d₃ is the ¹³C- and 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.

NNRT-IN-3 (compound 8) is an HIV-1 non-nucleoside reverse transcriptase inhibitor (EC₅₀=0.01 μM).

DMP-851 is a cyclic urea HIV protease inhibitor, with a K_i of 0.021 nM. DMP-851 shows antiviral activity against laboratory strains of HIV-l and HIV-2 as well as against primary clinical isolates derived from Zidovudine (HY-17413)-resistant samples (A018C, E, WR 10983).

Saquinavir-d₉ (Ro 31-8959-d₉) is the deuterium labeled Saquinavir (HY-17007). 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.

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.