HIV Protease Inhibitor

A-77003 is an inhibitor for HIV protease, with IC₅₀ of 0.1 to 0.2 μg/ml, for HIV-1 and HIV-2 protease. A-77003 exhibits high levels of antiretroviral activity and low cytotoxicity in vitro.

CGP-75355 is an inhibitor of HIV-1 protease with IC₅₀ of 26 nM. CGP-75355 is a bis(L-tert-leucine) derivative.

KNI-174 is a potent and selective HIV-1 protease inhibitor and antiviral agent. KNI-174 targets and inhibits HIV-1-specific aspartic protease, thereby blocking retroviral proliferation. KNI-174 can be used in research related to acquired immunodeficiency syndrome (AIDS).

CGP 57813 is a peptidomimetic inhibitor of HIV protease that can be encapsulated by nanoparticles composed of poly(D,L-lactic acid) (PLA) and pH-sensitive methacrylic acid copolymers and delivered into the body.

A 74704 is a pseudo C2-symmetric inhibitor of HIV-1 protease and its diester analog.

Ritonavir-¹³C₃ is ¹³C labeled Ritonavir. 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.

Lopinavir-d₈ (ABT-378-d₈) is the deuterium labeled Lopinavir. 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 3CLpro inhibitor with an IC₅₀ of 14.2 μM.

GRL-142 is a potent HIV-1 protease inhibitor capable of crossing the blood-brain barrier. GRL-142 exhibits extremely high inhibitory activity against both wild-type and multidrug-resistant strains (IC₅₀=0.0094 nM). GRL-142 acts synergistically with the P2/P2' segments via a unique scaffold binding mechanism, utilizes fluorine-mediated stable interactions to maintain its bioactive conformation, adapts to p51 HIV-1 protease mutants, and maintains the flap-closed state by directly acting on the flap tip residues. GRL-142 disrupts the flap-water hydrogen bond network of wild-type protease, thereby effectively blocking viral replication. GRL-142 can be used to study HIV-1 infection and the associated neurocognitive disorder (HAND).

TMC310911 (Standard) (ASC-09 (Standard)) is the analytical standard of TMC310911 (HY-107123). This product is intended for research and analytical applications. TMC310911 is a potent and orally active HIV type-1 (HIV-1) protease inhibitor with EC₅₀ values ranged from 2.2 nM to 14.2 nM for wild-type HIV-1. TMC310911 has potent activity against a wide spectrum of recombinant HIV-1 isolates. TMC310911 has strong antiviral activity.

MDL-104168 is a macrocyclic peptide mimetic HIV protease inhibitor (human IC₅₀: 2 nM; K_i: 20 nM). MDL-104168 can be used for the research of human immunodeficiency virus infection.

A-80987 is an inhibitor of human immunodeficiency virus type 1 (HIV-1) protease.

Rpi-856 A is a competitive inhibitor of HIV-1 protease and HTLV-I protease, with an IC₅₀ of 37 nM against HIV-1 protease and an IC₅₀ of 27 nM against HTLV-I protease. Rpi-856 A inhibits Pepsin with an IC₅₀ of 1.9 μM. Rpi-856 A does not inhibit chymosin, trypsin, chymotrypsin, papain, bromelain, thermolysin, prolyl endopeptidase, carboxypeptidase A or carboxypeptidase B. Rpi-856 A can be used in the research of acquired immunodeficiency syndrome (AIDS) and related diseases, as well as HIV infection.

Escin IA (Standard) is the analytical standard of Escin IA. This product is intended for research and analytical applications. Escin IA is a triterpene saponin isolated from Aesculus hippocastanum, which inhibits HIV-1 protease with IC50 values of 35 μM. Escin IA has anti-TNBC metastasis activity, and its action mechanisms involved inhibition of epithelial-mesenchymal transition process by down-regulating LOXL2 expression.

BMS 186318 is an HIV protease inhibitor. BMS 186318 exhibits better anti-HIV efficacy when used in combination with reverse transcriptase inhibitors such as Stavudine (HY-B0116) and other protease inhibitors such as Saquinavir (HY-17007). BMS 186318 can be used in antiviral research.

ddCTP tetrasodium is a type of chain-terminating deoxynucleotide. ddCTP tetrasodium can be incorporated into the extension primer chain that lacks the 3'-hydroxyl group, thereby terminating primer extension, viral genome replication, and DNA synthesis. ddCTP tetrasodium can distinguish almost identical RNA through distinguishable extension products in primer extension inhibition experiments. ddCTP tetrasodium is the active metabolite of Zalcitabine (HY-17392), which can competitively inhibit HIV reverse transcriptase, terminate the synthesis of viral DNA chains, and thereby inhibit HIV replication.

U 81749 is a competitive, reversible HIV-1 protease inhibitor with a K_i value of 70 nM. U 81749 inhibits HIV-1 protease within HIV-like particles, blocks the processing of the HIV-1 gag polyprotein p55 into the mature structural proteins p24 and p17, and thereby prevents viral maturation. U 81749 reduces HIV p24 and HIV RNA levels in acutely infected human lymphocytes, and shows no toxicity to lymphocyte proliferation at effective concentrations. U 81749 can be used in studies related to HIV-1 infection.

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

Opaviraline (GW420867X) is an anti-HIV-1 reverse transcriptase inhibitor.

Rpi-856 C is an Aspartic protease inhibitor, with an IC₅₀ of 5.5 nM against HIV-1 protease, 9.2 nM against HTLV-I protease, 2.0 μM against Cathepsin D, and 4.8 μM against Pepsin. Rpi-856 C is produced by the Streptomyces strain AL-322. Rpi-856 C does not inhibit chymosin, trypsin, chymotrypsin, papain, bromelain, thermolysin, prolyl endopeptidase, carboxypeptidase A or carboxypeptidase B. Rpi-856 C can be used in the research of acquired immunodeficiency syndrome (AIDS) and related diseases, as well as HIV infection.

Fosamprenavir-¹³C₆ is the ¹³C-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.