HCV Protease Inhibitor

Faldaprevir (BI 201335) is a potent, orally active and selective noncovalent inhibitor of NS3/4A protease of HCV (hepatitis C virus) genotypes 1a and 1b, with K_i values of 2.6 and 2.0 nM, respectively. Faldaprevir inhibits HCV RNA replication, with EC₅₀ values of 6.5 and 3.1 nM, respectively. Faldaprevir has potent antiviral activity against chronic HCV infection.

Samatasvir (IDX71) is a potent, orally active NS5A inhibitor of HCV replication. Samatasvir is effective and selective against infectious HCV and replicons, with EC₅₀s falling within a tight range of 2 to 24 pM in genotype 1 through 5 replicons.

HZ-1157 inhibits HCV NS3/4A protease with an IC₅₀ of 1.0 μmol/L. HZ-1157 (4a) has a high dengue virus inhibitory activity (EC₅₀ = 0.15 μM) and is a relatively nontoxic (CC₅₀ > 10 μM) dengue antiviral agent.

IDX184 is a potent and orally bioavailable inhibitor of HCV replication. IDX184 potently inhibits HCV polymerase (IC₅₀=0.31 μM, K_i=52.3 nM).

Vaniprevir (MK-7009) is a non-covalent competitive inhibitor of the hepatitis C virus (HCV) NS3/4A protease.

Simeprevir (TMC435; TMC435350) sodium is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a K_i of 0.36 nM. Simeprevir sodium inhibits HCV replication with an EC₅₀ of 7.8 nM. Simeprevir sodium also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir sodium inhibits the main protease (M^pro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses.

Valopicitabine (NM283) is a nucleoside analog and the orally bioavailable proagent of the potent anti-HCV agent 2'-C-methylcytidine (NM107). NM107competitively inhibits NS5B polymerase, causing chain termination.

Roseoside is an inhibitor of DNA gyrase and HAV 3C protease, and also inhibits HCV NS5A/B replicase in human systems with an IC₅₀ of 20 μM. Roseoside binds to the active site of enzymes and stabilizes the interaction by forming hydrogen bonds with key amino acid residues. Roseoside inhibits the growth of Gram-positive bacteria, Gram-negative bacteria, and Candida albicans, and interferes with HCV RNA replication in vitro by inhibiting HCV NS5A/B replicase (IC₅₀=20 μM). Roseoside shows no cytotoxicity and serves as a research tool for studies related to bacterial infections, candidiasis, HAV and HCV.

JTK-109 is a potent inhibitor of hepatitis C virus NS5B RNA-dependent RNA polymerase. JTK-109 has NS5B inhibitory activity with IC₅₀ value of 0.017μM. JTK-109 can be used for the research of hepatitis C virus (HCV) .

GSK2818713 is a novel Hepatitis C NS5A replication complex inhibitor.

BI-1230, a chemical probe, is potent and digit nanomolar inhibitor of HCV NS3 protease and of viral replication. BI-1230 is also highly selective against other serine/cysteine proteases. BI-1230 shows good Pharmacokinetic(PK) activity.

BMS-986144 is an orally active inhibitor of HCV NS3/4A protease. BMS-986144 binds to the active site of HCV NS3/4A protease and induces conformational changes in the protease. BMS-986144 reduces time-dependent CYP3A4 inhibition, exhibits hepatic microsomal metabolic stability, and undergoes oxidation of the macrocyclic linker chain. BMS-986144 can be used in studies related to hepatitis C virus infection.

Paritaprevir (ABT-450) dihydrate is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC₅₀s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir dihydrate is also a SARS-CoV 3CL^pro inhibitor with an IC₅₀ of 1.31 μM. Paritaprevir dihydrate is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir dihydrate can be enhanced by Ritonavir (a CYP450 inhibitor).

Coblopasvir (KW-136) is a pangenotypic non-structural protein 5A (NS5A) inhibitor. Coblopasvir can be used for research of chronic hepatitis C virus infection.

Hepatitis Virus C NS3 Protease Inhibitor 2 is a product-based peptide inhibitor of hepatitis C virus (HCV) NS3 protease, with a K_i of 41 nM.

Boceprevir-d₉ is the deuterium labeled Boceprevir. Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a K_i of 14 nM in both enzyme assay and an EC₉₀ of 350 nM in cell-based replicon assay. Boceprevir inhibits SARS-CoV-2 3CLpro activity.

MK-1220 is a covalently reversible inhibitor of the hepatitis C virus (HCV) NS3/4A protease (NS3/4A protease) with a K_i of 0.02 nM. MK-1220 in cell models simulating viral replication exhibits EC₅₀s of 4 (with 10% fetal bovine serum) and 11 nM (50% normal human serum). MK-1220 can be used for the study of chronic hepatitis C virus infection.

Telaprevir (Standard) is the analytical standard of Telaprevir. This product is intended for research and analytical applications. Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide. Telaprevir inhibits SARS-CoV-2 3CLpro activity.

Simeprevir-¹³C,d₃ is the ¹³C- and deuterium labeled Simeprevir. Simeprevir is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a K_i of 0.36 nM. Simeprevir inhibits HCV replication with an EC₅₀ of 7.8 nM. Simeprevir also potently suppresses SARS-CoV-2 replication and synergizes with Remdesivir. Simeprevir inhibits the main protease (Mpro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses.

HCV NS5B polymerase-IN-5 is a HCV NS5B polymerase inhibitor with an IC₅₀ value of 47.9 μM. HCV NS5B polymerase-IN-5 reduces the production of inorganic pyrophosphate and decreases the nucleoside triphosphate incorporation of HCV NS5B polymerase. HCV NS5B polymerase-IN-5 can be used in studies related to hepatitis C virus infection.