HCV NS3-4A serine protease is a non-covalent heterodimer consisting of a catalytic subunit (the N-terminal one-third of NS3 protein) and an activating cofactor (NS4A protein), and is responsible for cleavage at four sites of the HCV polyprotein. HCV NS3-4A protease is essential for viral replication in cell culture and in chimpanzees, and has been considered as one of the most attractive targets for developing novel anti-HCV therapies. However, discovery of small-molecule, selective inhibitors against HCV NS3-4A protease as oral drug candidates has been hampered by its shallow substrate-binding groove and the lack of robust, reproducible viral replication models in cell culture or in small animals.


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Glecaprevir

Glecaprevir is a novel HCV NS3/4A protease inhibitor, with IC50 values ranging from 3.5 to 11.3 nM.

  • CAS Number: 1365970-03-1
  • MF: C38H46F4N6O9S
  • MW: 838.865
  • Catalog: HCV
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ac-Asp-D-Gla-Leu-Ile-β-cyclohexyl-Ala-Cys-OH

Ac-D-DGla-LI-Cha-C is a potent HCV protease inhibitor peptide. Ac-D-DGla-LI-Cha-C can be used for the research of cancer, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, lung diseases, heart and vascular diseases and metabolic diseases[1].

  • CAS Number: 208940-40-3
  • MF: C36H58N6O14S
  • MW: 830.94300
  • Catalog: HCV Protease
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Daclatasvir (BMS-790052)

Daclatasvir is a potent HCV NS5A protein inhibitor, with mean EC50 values of 50 and 9 pM against genotype 1a and 1b replicons, respectively.

  • CAS Number: 1009119-64-5
  • MF: C40H50N8O6
  • MW: 738.875
  • Catalog: HCV
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 1071.2±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 601.7±34.3 °C

ITMN 4077

ITMN 4077 is a macrocyclic inhibitor against Hepatitis C Virus (HCV) NS3 protease (EC50: 2131 nM)[1][2].

  • CAS Number: 790305-05-4
  • MF: C26H40N4O8S
  • MW: 568.6828
  • Catalog: HCV Protease
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Hepatitis Virus C NS3 Protease Inhibitor 2

Hepatitis Virus C NS3 Protease Inhibitor 2 is a product-based peptide inhibitor of hepatitis C virus (HCV) NS3 protease, with a Ki of 41 nM[1].

  • CAS Number: 208939-95-1
  • MF: C43H56N6O14S
  • MW: 913.10
  • Catalog: HCV
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Daclatasvir dihydrochloride

BMS-790052 is a highly selective inhibitor of HCV NS5A with EC50 of 9-50 pM, for a broad range of HCV replicon genotypes and the JFH-1 genotype 2a infectious virus in cell culture.IC50 Value: 9-50 pMTarget: HCV NS5ABMS-790052 has broad genotype coverage and exhibits picomolar in vitro potency against genotypes 1a (EC50 50pm) and 1b (EC50 9pm). BMS-790052 produces a robust decline in HCV RNA (-3.6 logs after 48 hours from a single 100 mg) dosefollowing a single dose in patients chronically infected with HCV genotype 1.

  • CAS Number: 1009119-65-6
  • MF: C40H52Cl2N8O6
  • MW: 811.797
  • Catalog: HCV
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Faldaprevir-d6

Faldaprevir-d6 is deuterium labeled Faldaprevir.

  • CAS Number: 2750534-88-2
  • MF: C40H43D6BrN6O9S
  • MW: 875.86
  • Catalog: HCV Protease
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Asunaprevir

Asunaprevir is a potent hepatitis C virus (HCV) NS3 protease inhibitor, with IC50 of 0.2 nM-3.5 nM.

  • CAS Number: 630420-16-5
  • MF: C35H46ClN5O9S
  • MW: 748.286
  • Catalog: HCV
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TMC435

Simeprevir (TMC435; TMC435350) sodium is an oral, potent and highly specific hepatitis C virus (HCV) NS3/4A protease inhibitor with a Ki 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 (Mpro) and the RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2, and also modulates host immune responses[1][4].

  • CAS Number: 1241946-89-3
  • MF: C38H46N5NaO7S2
  • MW: 771.92100
  • Catalog: HCV
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ombitasvir

Ombitasvir is a potent inhibitor of the hepatitis C virus protein NS5A, with EC50s of 0.82 to 19.3 pM against HCV genotypes 1 to 5, and 366 pM against genotype 6a.

  • CAS Number: 1258226-87-7
  • MF: C50H67N7O8
  • MW: 894.109
  • Catalog: HCV
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 1065.6±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 598.2±34.3 °C

Ledipasvir (acetone)

Ledipasvir acetone is the active pharmaceutical ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.

  • CAS Number: 1441674-54-9
  • MF: C52H60F2N8O7
  • MW: 947.079
  • Catalog: HCV
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Vaniprevir

Vaniprevir (MK-7009) is a non-covalent competitive inhibitor of the hepatitis C virus (HCV) NS3/4A protease.IC50 Value: Target: HCV NS3/4A Protease; HCVvaniprevir (MK-7009) is a macrocyclic hepatitis C virus NS3/4a protease inhibitor, is active against both the genotype 1 and genotype 2 NS3/4a protease enzymes. vaniprevir (MK-7009) has good plasma exposure and excellent liver exposure in multiple species.

  • CAS Number: 923590-37-8
  • MF: C38H55N5O9S
  • MW: 757.93600
  • Catalog: HCV
  • Density: 1.33g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Dehydrojuncusol

Dehydrojuncusol, a potent HCV inhibitor, targets HCV NS5A and is able to inhibit RNA replication of replicons harboring resistance mutations to anti-NS5A direct-acting antivirals. Dehydrojuncusol significantly inhibits HCV infection when added after virus inoculation of HCV genotype 2a (EC50=1.35 µM)[1].

  • CAS Number: 117824-04-1
  • MF: C18H16O2
  • MW: 264.31800
  • Catalog: HCV
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Clemizole hydrochloride

Clemizole hydrochloride is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication. The IC50 of Clemizole for RNA binding by NS4B is 24±1 nM, whereas its EC50 for viral replication is 8 µM.

  • CAS Number: 1163-36-6
  • MF: C19H21Cl2N3
  • MW: 362.296
  • Catalog: HCV
  • Density: 1.25 g/cm3
  • Boiling Point: 506.1ºC at 760 mmHg
  • Melting Point: 241 °C
  • Flash Point: 259.9ºC

Grazoprevir hydrate

Grazoprevir hydrate (MK-5172 hydrate) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.

  • CAS Number: 1350462-55-3
  • MF: C38H52N6O10S
  • MW: 784.91900
  • Catalog: HCV
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

velpatasvir

Velpatasvir (VEL, GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons.target: NS5A

  • CAS Number: 1377049-84-7
  • MF: C49H54N8O8
  • MW: 883.002
  • Catalog: HCV
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GSK2818713

GSK2818713 is a novel Hepatitis C NS5A replication complex inhibitor.

  • CAS Number: 1422484-32-9
  • MF: C46H56N8O8
  • MW: 848.99
  • Catalog: HCV Protease
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Narlaprevir

Narlaprevir is a potent, selective, orally bioavailable NS3 protease inhibitor(Ki=6 nM; EC90=40 nM)IC50 Value: 6 nM (Ki)Target: HCV NS3/4A Protease; HCVNarlaprevir (SCH 900518) is a potent inhibitor of the hepatitis C virus (HCV) nonstructural protein 3 serine protease that is primarily metabolized by the cytochrome P450-3A4 system. Narlaprevir administration resulted in a robust HCV-RNA decline and high SVR rates when followed by standard of care in both treatment-experienced and treatment-naive HCV genotype 1-infected patients.

  • CAS Number: 865466-24-6
  • MF: C36H61N5O7S
  • MW: 707.964
  • Catalog: HCV
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Beclabuvir

Beclabuvir is an allosteric inhibitor that binds to thumb site 1 of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase, and inhibits recombinant NS5B proteins from HCV genotypes 1, 3, 4, and 5 with IC50 of < 28 nM. 

  • CAS Number: 958002-33-0
  • MF: C36H45N5O5S
  • MW: 659.838
  • Catalog: HCV
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Boceprevir

Boceprevir is a novel, potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with Ki of 14 nM in both enzyme assay and EC90 of 350 nM in cell-based replicon assay.

  • CAS Number: 394730-60-0
  • MF: C27H45N5O5
  • MW: 519.677
  • Catalog: HCV
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MK-5172 (potassium salt)

Grazoprevir potassium salt (MK-5172 potassium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.

  • CAS Number: 1206524-86-8
  • MF: C38H49KN6O9S
  • MW: 804.994
  • Catalog: HCV
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ledipasvir

Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively.

  • CAS Number: 1256388-51-8
  • MF: C49H54F2N8O6
  • MW: 889.000
  • Catalog: HCV
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Valopicitabine dihydrochloride

Valopicitabine (NM283) dihydrochloride is a nucleoside analog and the orally bioavailable prodrug of the potent anti-HCV agent 2'-C-methylcytidine (NM107). NM107competitively inhibits NS5B polymerase, causing chain termination[1][2].

  • CAS Number: 640725-71-9
  • MF: C15H26Cl2N4O6
  • MW: 429.30
  • Catalog: HCV
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Samatasvir

Samatasvir (IDX719) is a highly potent, selective inhibitor of HCV NS5A that effectively inhibits HCV genotype 1-5 replicons with EC50 of 2-24 pM; also retains full activity in the presence of HIV and hepatitis B virus (HBV) antivirals; demonstrates an overall additive effect when combined with IFN-α, ribavirin, representative HCV protease, and nonnucleoside polymerase inhibitors or the nucleotide prodrug IDX184. HCV Infection Phase 2 Clinical

  • CAS Number: 1312547-19-5
  • MF: C47H48N8O6S2
  • MW: 885.064
  • Catalog: HCV
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Telaprevir (VX-950)

Telaprevir 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.

  • CAS Number: 402957-28-2
  • MF: C36H53N7O6
  • MW: 679.849
  • Catalog: HCV
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HZ-1157

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[1][2].

  • CAS Number: 1009734-33-1
  • MF: C12H16N4O
  • MW: 232.282
  • Catalog: HCV Protease
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 471.6±53.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 239.0±30.9 °C

VCH-916

VCH-916 is a novel nonnucleoside HCV NS5B polymerase inhibitor.IC50 Value: Target: HCVVCH-916 is a novel allosteric inhibitor of HCV NS5B polymerase. The RNA-dependent RNA polymerase (NS5B) of HCV is one of the attractive validated targets for development of new drugs to block HCV infection. VCH-916 is currently being evaluated for safety/tolerability, pharmacokinetics and anti-viral efficacy in chronically infected HCV patient.

  • CAS Number: 1200133-34-1
  • MF: C26H36KNO4S
  • MW: 497.732
  • Catalog: HCV
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MK-5172

Grazoprevir (MK-5172) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.

  • CAS Number: 1350514-68-9
  • MF: C38H50N6O9S
  • MW: 766.903
  • Catalog: HCV
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HCVP-IN-1

HCVP-IN-1 (compound 1) is a hepatitis C viral polymerase (HCVP) inhibitor[1].

  • CAS Number: 877225-09-7
  • MF: C30H34FN5O3
  • MW: 531.62100
  • Catalog: HCV Protease
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BI 653048

BI 653048 is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with anti-inflammatory effects[1]. BI 653048, compound 103 extracted from patent WO2005028501A1, is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus[2].

  • CAS Number: 1198784-72-3
  • MF: C23H25F4N3O4S
  • MW: 515.52
  • Catalog: Glucocorticoid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A