HCV Protease Inhibitor

NS5A-IN-1 is a proagent of the HCV NS5A inhibitor Pibrentasvir (ABT-530).

Ac-DEMEEC-OH is a HCV NS3 protease competitive inhibitor (K_i: 0.6 µM).

Grazoprevir sodium salt (MK-5172 sodium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with K_is of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively. Grazoprevir sodium salt inhibits SARS-CoV-2 3CL^pro activity.

MK-2748 is a hepatitis C virus (HCV) NS3/4a protease inhibitor. MK-2748 exhibits broad-spectrum and potent antiviral activity, with nanomolar-level activity against all genotypes (gt1a-gt6) (IC₅₀ < 0.115 nM), showing only slightly weaker activity against gt3a (1.212 nM), and maintaining high inhibitory activity against drug-resistant mutant strains such as gt1b R155K (IC₅₀ = 0.032 nM) and D168Y (IC₅₀ = 0.057 nM). MK-2748 can be used in the research of HCV infection.

BMS-986144 non-deuterated is the non-tritium form of BMS-986144 (HY-131905S). 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.

Deldeprevir (ACH-2684; Neceprevir) sodium is a HCV NS3/4A protease inhibitor and resistance inhibitor. Deldeprevir sodium exhibits activity against wild-type genotype 1a and 1b HCV, including mutant strains resistant to other NS3 protease inhibitors. Deldeprevir sodium blocks the emergence of HCV mutant strains resistant to ACH-3422 in vitro, with enhanced efficacy when used in triple combination with ACH-3422 and ACH-3102 (HY-124182). Deldeprevir sodium shows additive antiviral potency when combined with ACH-3422, and exerts antiviral activity against HCV replicons carrying ACH-3102. Deldeprevir sodium is applicable to research related to hepatitis C.

Valopicitabine dihydrochloride (Standard) is the analytical standard of Valopicitabine (dihydrochloride) (HY-108060A). This product is intended for research and analytical applications. Valopicitabine (NM283) dihydrochloride 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.

Glecaprevir (Standard) is the analytical standard of Glecaprevir. This product is intended for research and analytical applications. Glecaprevir is a novel HCV NS3/4A protease inhibitor, with IC50 values ranging from 3.5 to 11.3 nM. Glecaprevir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 4.09 μM.

Deldeprevir (ACH-2684) is a HCV NS3 protease inhibitor. Deldeprevir has potent antiviral activities against different genotypes and against known resistant variants (such as R155, Al56 and D168) by the formation a highly stable complex with NS3 prolease. Deldeprevir can be used for Hepatitis C virus infection research.

Paritaprevir (Standard) is the analytical standard of Paritaprevir. This product is intended for research and analytical applications. Paritaprevir (ABT-450) 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 is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.31 μM. Paritaprevir is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir can be enhanced by Ritonavir (a CYP450 inhibitor).

Simeprevir (Standard) is the analytical standard of Simeprevir (HY-10241). This product is intended for research and analytical applications. Simeprevir (TMC435; TMC435350) 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-IN-50 (Compound 2) is a competitive and selective HCV NS5B RNA-dependent RNA polymerase inhibitor with an IC₅₀ of 0.3  μM for NS5B △C21 enzyme over △C55 enzyme. HCV-IN-50 has an antiviral activity and efficiently blocks replication of HCV subgenomic replicons especially mutant replicons.

Boceprevir (Standard) is the analytical standard of Boceprevir. This product is intended for research and analytical applications. 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 3CL^pro activity.

Vedroprevir (GS-9451) is an inhibitor for HCV NS3/4A protease with an IC₅₀ of 3.2 nM. Vedroprevir is also an inhibitor for breast cancer resistant protein (BCRP) with an IC₅₀ of 1.4 μM. Vedroprevir inhibits P-gp, MRP1 and MRP2 with IC₅₀ of 34, 14.9 and 12 μM, respectively. Vedroprevir exhibits good pharmacokinetic characteristics in rats and dogs.

CID-50930756 is an HCV NS3 helicase inhibitor with an IC₅₀ of 22 μM.CID-50930756 inhibits HCV NS3 helicase-catalyzed nucleic acid unwinding.CID-50930756 inhibits HCV replication in hepatoma cells harboring a stably transfected subgenomic HCV replicon.CID-50930756 does not exhibit toxicity to hepatoma cells at 10 μM.CID-50930756 shows weak DNA-binding activity, displacing less than 20% of SYBR Green I from DNA at 100 μM.CID-50930756 can be used for the research of hepatitis c.

BMS 605339 is a linear tetra-peptide α-ketoamide inhibitor of HCV NS3 protease. BMS 605339 can be used in research related to hepatitis C (HCV infection).

Narlaprevir (Standard) is the analytical standard of Narlaprevir. This product is intended for research and analytical applications. Narlaprevir (SCH 900518) is a selective and orally bioavailable NS3 protease inhibitor with a Ki value of 6 nM and an EC90 value of 40 nM. Narlaprevir also inhibits the HCV nonstructural protein 3 serine protease. Narlaprevir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 2.3 μM.

Danoprevir (Standard) is the analytical standard of Danoprevir (HY-10238). This product is intended for research and analytical applications. Danoprevir (ITMN-191) is an orally active NS3/4A protease inhibitor for hepatitis C virus (HCV) with an IC₅₀ of 0.29 nM and is selective for NS3/4A over a panel of 53 proteases (IC₅₀ higher than 10 μM). Danoprevir (ITMN-191) inhibits HCV genotypes 1a, 1b, 4, 5, and 6 (IC₅₀s=0.2-0.4 nM) as well as 2b and 3a (IC₅₀s=1.6, 3.5 nM). Danoprevir is also a SARS-CoV 3CLpro inhibitor with an IC₅₀ of 0.05 μM.

Asunaprevir (Standard) is the analytical standard of Asunaprevir. This product is intended for research and analytical applications. Asunaprevir (BMS-650032) is a potent and orally bioavailable hepatitis C virus (HCV) NS3 protease inhibitor, with IC50 of 0.2 nM-3.5 nM. Asunaprevir inhibits SARS-CoV-2 3CLpro activity.